Publications | EUbOPEN

2024

Pahlevan Kakhki M, Giordano A, Starvaggi Cucuzza C, Venkata S Badam T, Samudyata S, Lemée MV, Stridh P, Gkogka A, Shchetynsky K, Harroud A, Gyllenberg A, Liu Y, Boddul S, James T, Sorosina M, Filippi M, Esposito F, Wermeling F, Gustafsson M, Casaccia P, Hillert J, Olsson T, Kockum I, Sellgren CM, Golzio C, Kular L, Jagodic M. (2024) A genetic-epigenetic interplay at 1q21.1 locus underlies CHD1L-mediated vulnerability to primary progressive multiple sclerosis. Nat Commun. 15(1):6419. doi: 10.1038/s41467-024-50794-z.

Nie DY, Tabor JR, Li J, Kutera M, St-Germain J, Hanley RP, Wolf E, Paulakonis E, Kenney TMG, Duan S, Shrestha S, Owens DDG, Maitland MER, Pon A, Szewczyk M, Lamberto AJ, Menes M, Li F, Penn LZ, Barsyte-Lovejoy D, Brown NG, Barsotti AM, Stamford AW, Collins JL, Wilson DJ, Raught B, Licht JD, James LI, Arrowsmith CH. (2024) Recruitment of FBXO22 for targeted degradation of NSD2. Nat Chem Biol. 2024 Jul 4. doi: 10.1038/s41589-024-01660-y

Monteil VM, Wright SC, Dyczynski M, Kellner MJ, Appelberg S, Platzer SW, Ibrahim A, Kwon H, Pittarokoilis I, Mirandola M, Michlits G, Devignot S, Elder E, Abdurahman S, Bereczky S, Bagci B, Youhanna S, Aastrup T, Lauschke VM, Salata C, Elaldi N, Weber F, Monserrat N, Hawman DW, Feldmann H, Horn M, Penninger JM, Mirazimi A. (2024) Crimean-Congo haemorrhagic fever virus uses LDLR to bind and enter host cells. Nat Microbiol. 9(6):1499-1512. doi: 10.1038/s41564-024-01672-3

Oliva-Vilarnau N, Beusch CM, Sabatier P, Sakaraki E, Tjaden A, Graetz L, Büttner FA, Dorotea D, Nguyen M, Bergqvist F, Sundström Y, Müller S, Zubarev RA, Schulte G, Tredup C, Gramignoli R, Tietge UJF, Lauschke VM. (2024) Wnt/β-catenin and NFκB signaling synergize to trigger growth factor-free regeneration of adult primary human hepatocytes. Hepatology. 2024 Jun 1;79(6):1337-1351. doi: 10.1097/HEP.0000000000000648

Taebnia N, Lauschke VM. (2024) Hepatic Inhibition of ANGPTL3 Mimics the Molecular Hallmarks of Hypothyroidism. Arterioscler Thromb Vasc Biol. 44(5):1098-1100. doi: 10.1161/ATVBAHA.124.320817

Righetto GL, Yin Y, Duda DM, Vu V, Szewczyk MM, Zeng H, Li Y, Loppnau P, Mei T, Li YY, Seitova A, Patrick AN, Brazeau JF, Chaudhry C, Barsyte-Lovejoy D, Santhakumar V, Halabelian L. (2024) Probing the CRL4^DCAF12 interactions with MAGEA3 and CCT5 di-Glu C-terminal degrons. PNAS Nexus. 3(4):pgae153. doi: 10.1093/pnasnexus/pgae153

Frommelt F, Fossati A, Uliana F, Wendt F, Xue P, Heusel M, Wollscheid B, Aebersold R, Ciuffa R, Gstaiger M. (2024) DIP-MS: ultra-deep interaction proteomics for the deconvolution of protein complexes. Nat Methods. 21(4):635-647. doi: 10.1038/s41592-024-02211-y

González-Álvarez H, Ensan D, Xin T, Wong JF, Zepeda-Velázquez CA, Cros J, Sweeney MN, Hoffer L, Kiyota T, Wilson BJ, Aman A, Roberts O, Isaac MB, Bullock AN, Smil D, Al-Awar R. (2024) Discovery of Conformationally Constrained ALK2 Inhibitors. J Med Chem. 67(6):4707-4725. doi: 10.1021/acs.jmedchem.3c02308.

Flax RG, Rosston P, Rocha C, Anderson B, Capener JL, Durcan TM, Drewry DH, Prinos P, Axtman AD. (2024) Illumination of understudied ciliary kinases. Front Mol Biosci. 2024 Mar 8;11:1352781. doi: 10.3389/fmolb.2024.1352781

Ipas H, Gouws EB, Abell NS, Chiou PC, Devanathan SK, Hervé S, Lee S, Mercado M, Reinsborough C, Halabelian L, Arrowsmith CH, Xhemalçe B. (2024) ChemRAP uncovers specific mRNA translation regulation via RNA 5' phospho-methylation. EMBO Rep. 2024 Mar;25(3):1570-1588. doi: 10.1038/s44319-024-00059-z

Koutsilieri S, Mickols E, Végvári Á, Lauschke VM. (2024) Proteomic workflows for deep phenotypic profiling of 3D organotypic liver models. Biotechnol J. 19(3):e2300684. doi: 10.1002/biot.202300684

Asressu KH, Smith JL, Dickmander RJ, Moorman NJ, Wellnitz J, Popov KI, Axtman AD, Willson TM. (2024) Synthesis of 5-Benzylamino and 5-Alkylamino-Substituted Pyrimido[4,5-c]quinoline Derivatives as CSNK2A Inhibitors with Antiviral Activity. Pharmaceuticals (Basel). 17(3):306. doi: 10.3390/ph17030306

Perveen S, Yazdi AK, Hajian T, Li F, Vedadi M. (2024) Kinetic characterization of human mRNA guanine-N7 methyltransferase. Sci Rep. 14(1):4509. doi: 10.1038/s41598-024-55184-5

Bauer N, Balourdas DI, Schneider JR, Zhang X, Berger LM, Berger BT, Schwalm MP, Klopp NA, Siveke JT, Knapp S, Joerger AC. (2024) Development of Potent Dual BET/HDAC Inhibitors via Pharmacophore Merging and Structure-Guided Optimization. ACS Chem Biol. 19(2):266-279. doi: 10.1021/acschembio.3c00427.

Zhang SM, Paulin CBJ, Shu H, Yagüe-Capilla M, Michel M, Marttila P, Ortis F, Bwanika HC, Dirks C, Venkatram RP, Wiita E, Jemth AS, Almlöf I, Loseva O, Hormann FM, Koolmeister T, Linde E, Lee S, Llona-Minguez S, Haraldsson M, Axelsson H, Strömberg K, Homan EJ, Scobie M, Lundbäck T, Helleday T, Rudd SG. (2024) Identification and evaluation of small-molecule inhibitors against the dNTPase SAMHD1 via a comprehensive screening funnel. iScience. 27(2):108907. doi: 10.1016/j.isci.2024.108907

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024) The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res. 52(D1):D1180-D1192. doi: 10.1093/nar/gkad1004

Alcober-Boquet L, Zang T, Pietsch L, Suess E, Hartmann M, Proschak E, Gross LZF, Sacerdoti M, Zeuzem S, Rogov VV, Leroux AE, Piiper A, Biondi RM. (2024) The PB1 and the ZZ domain of the autophagy receptor p62/SQSTM1 regulate the interaction of p62/SQSTM1 with the autophagosome protein LC3B. Protein Sci. 33(1):e4840. doi: 10.1002/pro.4840

Ren L, Charbord J, Chu L, Kemas AM, Bertuzzi M, Mi J, Xing C, Lauschke VM, Andersson O. (2024) Adjudin improves beta cell maturation, hepatic glucose uptake and glucose homeostasis. Diabetologia. 67(1):137-155. doi: 10.1007/s00125-023-06020-4

2023

Kimani SW, Perveen S, Szewezyk M, Zeng H, Dong A, Li F, Ghiabi P, Li Y, Chau I, Arrowsmith CH, Barsyte-Lovejoy D, Santhakumar V, Vedadi M, Halabelian L. (2023) The co-crystal structure of Cbl-b and a small-molecule inhibitor reveals the mechanism of Cbl-b inhibition. Commun Biol. 6(1):1272. doi: 10.1038/s42003-023-05655-8

Mann MK, Wolf E, Silva M, Kwak HA, Wilson B, Bolotokova A, Wilson DJ, Harding RJ, Schapira M. (2023) Small Molecule Screen Identifies Non-catalytic USP3 Chemical Handle. ACS Omega. 9(1):917-924. doi: 10.1021/acsomega.3c07070

Karelou M, Kampasis D, Kalampaliki AD, Persoons L, Krämer A, Schols D, Knapp S, De Jonghe S, Kostakis IK. (2023) Synthesis and Biological Evaluation of 2-Substituted Quinazolin-4(3H)-Ones with Antiproliferative Activities. Molecules. 28(23):7912. doi: 10.3390/molecules28237912

Velasco Cárdenas RM, Brandl SM, Meléndez AV, Schlaak AE, Buschky A, Peters T, Beier F, Serrels B, Taromi S, Raute K, Hauri S, Gstaiger M, Lassmann S, Huppa JB, Boerries M, Andrieux G, Bengsch B, Schamel WW, Minguet S. (2023) Harnessing CD3 diversity to optimize CAR T cells. Nat Immunol. 24(12):2135-2149. doi: 10.1038/s41590-023-01658-z

Ayoubi R, Ryan J, Biddle MS, Alshafie W, Fotouhi M, Bolivar SG, Ruiz Moleon V, Eckmann P, Worrall D, McDowell I, Southern K, Reintsch W, Durcan TM, Brown C, Bandrowski A, Virk H, Edwards AM, McPherson P, Laflamme C. (2023) Scaling of an antibody validation procedure enables quantification of antibody performance in major research applications. Elife. 12:RP91645. doi: 10.7554/eLife.91645

Simon IA, Homan EJ, Wijtmans M, Sundström M, Leurs R, De Esch IJP, Zarzycka BA. (2023) PSW-Designer: An Open-Source Computational Platform for the Design and Virtual Screening of Photopharmacological Ligands. J Chem Inf Model. 63(21):6696-6705. doi: 10.1021/acs.jcim.3c01050

Wesseler MF, Taebnia N, Harrison S, Youhanna S, Preiss LC, Kemas AM, Vegvari A, Mokry J, Sullivan GJ, Lauschke VM, Larsen NB. (2023) 3D microperfusion of mesoscale human microphysiological liver models improves functionality and recapitulates hepatic zonation. Acta Biomater. 171:336-349. doi: 10.1016/j.actbio.2023.09.022

Stanfill SB, Hecht SS, Joerger AC, González PJ, Maia LB, Rivas MG, Moura JJG, Gupta AK, Le Brun NE, Crack JC, Hainaut P, Sparacino-Watkins C, Tyx RE, Pillai SD, Zaatari GS, Henley SJ, Blount BC, Watson CH, Kaina B, Mehrotra R. (2023) From cultivation to cancer: formation of N-nitrosamines and other carcinogens in smokeless tobacco and their mutagenic implications. Crit Rev Toxicol. 53(10):658-701. doi: 10.1080/10408444.2023.2264327

Krishnan R, Lapierre M, Gautreau B, Nixon KCJ, El Ghamrasni S, Patel PS, Hao J, Yerlici VT, Guturi KKN, St-Germain J, Mateo F, Saad A, Algouneh A, Earnshaw R, Shili D, Seitova A, Miller J, Khosraviani N, Penn A, Ho B, Sanchez O, Hande MP, Masson JY, Brown GW, Alaoui-Jamali M, Reynolds JJ, Arrowsmith C, Raught B, Pujana MA, Mekhail K, Stewart GS, Hakem A, Hakem R. (2023) RNF8 ubiquitylation of XRN2 facilitates R-loop resolution and restrains genomic instability in BRCA1 mutant cells. Nucleic Acids Res. 51(19):10484-10505. doi: 10.1093/nar/gkad733

Strubel A, Münick P, Hartmann O, Chaikuad A, Dreier B, Schaefer JV, Gebel J, Osterburg C, Tuppi M, Schäfer B, Buck V, Rosenfeldt M, Knapp S, Plückthun A, Diefenbacher ME, Dötsch V. (2023) DARPins detect the formation of hetero-tetramers of p63 and p73 in epithelial tissues and in squamous cell carcinoma. Cell Death Dis. 14(10):674. doi: 10.1038/s41419-023-06213-0

Yang X, Ong HW, Dickmander RJ, Smith JL, Brown JW, Tao W, Chang E, Moorman NJ, Axtman AD, Willson TM. (2023) Optimization of 3-Cyano-7-cyclopropylamino-pyrazolo[1,5-a]pyrimidines toward the Development of an In Vivo Chemical Probe for CSNK2A. ACS Omega. 8(42):39546-39561. doi: 10.1021/acsomega.3c05377

Wright SC, Motso A, Koutsilieri S, Beusch CM, Sabatier P, Berghella A, Blondel-Tepaz É, Mangenot K, Pittarokoilis I, Sismanoglou DC, Le Gouill C, Olsen JV, Zubarev RA, Lambert NA, Hauser AS, Bouvier M, Lauschke VM. (2023) GLP-1R signaling neighborhoods associate with the susceptibility to adverse drug reactions of incretin mimetics. Nat Commun. 14(1):6243. doi: 10.1038/s41467-023-41893-4

Lauschke VM. Practice guidance documents for the diagnosis and management of non-alcoholic fatty liver disease-recent updates and open questions. Hepatobiliary Surg Nutr. 12(5):780-784. doi: 10.21037/hbsn-23-376

Patil PR, Burroughs AM, Misra M, Cerullo F, Costas-Insua C, Hung HC, Dikic I, Aravind L, Joazeiro CAP. (2023) Mechanism and evolutionary origins of alanine-tail C-degron recognition by E3 ligases Pirh2 and CRL2-KLHDC10. Cell Rep. 42(9):113100. doi: 10.1016/j.celrep.2023.113100

Yong D, Green SR, Ghiabi P, Santhakumar V, Vedadi M. (2023) Discovery of Nedd4 auto-ubiquitination inhibitors. Sci Rep. 13(1):16057. doi: 10.1038/s41598-023-42997-z

Gan J, de Vries J, Akkermans JJLL, Mohammed Y, Tjokrodirijo RTN, de Ru AH, Kim RQ, Vargas DA, Pol V, Fasan R, van Veelen PA, Neefjes J, van Dam H, Ovaa H, Sapmaz A, Geurink PP. (2023) Cellular Validation of a Chemically Improved Inhibitor Identifies Monoubiquitination on OTUB2. ACS Chem Biol. 18(9):2003-2013. doi: 10.1021/acschembio.3c00227

Tremmel R, Zhou Y, Schwab M, Lauschke VM. (2023) Structural variation of the coding and non-coding human pharmacogenome. NPJ Genom Med. 8(1):24. doi: 10.1038/s41525-023-00371-y

Pichon MM, Drelinkiewicz D, Lozano D, Moraru R, Hayward LJ, Jones M, McCoy MA, Allstrum-Graves S, Balourdas DI, Joerger AC, Whitby RJ, Goldup SM, Wells N, Langley GJ, Herniman JM, Baud MGJ. (2023) Structure-Reactivity Studies of 2-Sulfonylpyrimidines Allow Selective Protein Arylation. Bioconjug Chem. 34(9):1679-1687. doi: 10.1021/acs.bioconjchem.3c00322

Harding RJ, Franzoni I, Mann MK, Szewczyk MM, Mirabi B, Ferreira de Freitas R, Owens DDG, Ackloo S, Scheremetjew A, Juarez-Ornelas KA, Sanichar R, Baker RJ, Dank C, Brown PJ, Barsyte-Lovejoy D, Santhakumar V, Schapira M, Lautens M, Arrowsmith CH. (2023) Discovery and Characterization of a Chemical Probe Targeting the Zinc-Finger Ubiquitin-Binding Domain of HDAC6. J Med Chem. 66(15):10273-10288. doi: 10.1021/acs.jmedchem.3c00314

Pérez Berrocal DA, Vishwanatha TM, Horn-Ghetko D, Botsch JJ, Hehl LA, Kostrhon S, Misra M, Ðikić I, Geurink PP, van Dam H, Schulman BA, Mulder MPC. (2023) A Pro-Fluorescent Ubiquitin-Based Probe to Monitor Cysteine-Based E3 Ligase Activity. Angew Chem Int Ed Engl. 62(32):e202303319. doi:10.1002/anie.202303319

Grätz L, Kowalski-Jahn M, Scharf MM, Kozielewicz P, Jahn M, Bous J, Lambert NA, Gloriam DE, Schulte G. (2023) Pathway selectivity in Frizzleds is achieved by conserved micro-switches defining pathway-determining, active conformations. Nat Commun. 14(1):4573. Published 2023 Jul 29. doi:10.1038/s41467-023-40213-0

Lauschke VM, Zhou Y, Ingelman-Sundberg M. (2023) Pharmacogenomics Beyond Single Common Genetic Variants: The Way Forward [published online ahead of print, 2023 Jul 28]. Annu Rev Pharmacol Toxicol. 10.1146/annurev-pharmtox-051921-091209. doi:10.1146/annurev-pharmtox-051921-091209

Farin HF, Mosa MH, Ndreshkjana B, Grebbin BM, Ritter B, Menche C, Kennel KB, Ziegler PK, Szabo L, Bollrath J, Rieder D, Michels BE, Kress A, Bozlar M, Darvishi T, Stier S, Kur IM, Bankov K, Kesselring R, Fichtner-Feigl S, Brune B, Goetze TO, Al-Batran SE, Brandts CH, Bechstein WO, Wild PJ, Weigert A, Muller S, Knapp S, Trajanoski Z, Greten FR. (2023) Colorectal cancer organoid-stroma biobank allows subtype-specific assessment of individualized therapy responses. [published online ahead of print, 2023 Jul 25]. Cancer Discov. 2023;CD-23-0050. doi:10.1158/2159-8290.CD-23-0050

Castano A, Silvestre M, Wells CI, Sanderson JL, Ferrer CA, Ong HW, Lang Y, Richardson W, Silvaroli JA, Bashore FM, Smith JL, Genereux IM, Dempster K, Drewry DH, Pabla NS, Bullock AN, Benke TA, Ultanir SK, Axtman AD. (2023) Discovery and characterization of a specific inhibitor of serine-threonine kinase cyclin-dependent kinase-like 5 (CDKL5) demonstrates role in hippocampal CA1 physiology. Elife. 12:e88206. doi: 10.7554/eLife.88206

Chauhan C, Kraemer A, Knapp S, Windheim M, Kotlyarov A, Menon MB, Gaestel M. (2023) 5-Iodotubercidin sensitizes cells to RIPK1-dependent necroptosis by interfering with NFκB signaling. Cell Death Discov. 9(1):262. doi: 10.1038/s41420-023-01576-x

Schwalm MP, Krämer A, Dölle A, Weckesser J, Yu X, Jin J, Saxena K, Knapp S. (2023) Tracking the PROTAC degradation pathway in living cells highlights the importance of ternary complex measurement for PROTAC optimization. Cell Chem Biol. 30(7):753-765.e8. doi: 10.1016/j.chembiol.2023.06.002

Arifi S, Marschner JA, Pollinger J, Isigkeit L, Heitel P, Kaiser A, Obeser L, Höfner G, Proschak E, Knapp S, Chaikuad A, Heering J, Merk D. (2023) Targeting the Alternative Vitamin E Metabolite Binding Site Enables Noncanonical PPARγ Modulation. J Am Chem Soc. 145(27):14802-14810. doi: 10.1021/jacs.3c03417

Barreby E, Strunz B, Nock S, Naudet L, Shen JX, Johansson H, Sönnerborg I, Ma J, Urgard E, Pallett LJ, Hu Y, Fardellas A, Azzimato V, Vankova A, Levi L, Morgantini C, Maini MK, Stål P, Rosshart SP, Coquet JM, Nowak G, Näslund E, Lauschke VM, Ellis E, Björkström NK, Chen P, Aouadi M. (2023) Human resident liver myeloid cells protect against metabolic stress in obesity. Nat Metab. 5(7):1188-1203. doi:10.1038/s42255-023-00834-7

Choi JY, Noguchi Y, Alburger JM, Bayle S, Chung E, Grant W, Chaikuad A, Knapp S, Duckett DR, Roush WR. (2023) Structure-Based Development of Isoform-Selective Inhibitors of Casein Kinase 1ε vs Casein Kinase 1δ. J Med Chem. 66(11):7162-7178. doi: 10.1021/acs.jmedchem.2c01180

Novak L, Petrosino M, Pasquo A, Chaikuad A, Chiaraluce R, Knapp S, Consalvi V. (2023) Mutation in the Common Docking Domain Affects MAP Kinase ERK2 Catalysis and Stability. Cancers (Basel). 15(11):2938. doi: 10.3390/cancers15112938

Kimani S, Perveen S, Szewezyk M, Zeng H, Dong A, Li F, Ghiabi P, Li Y, Chau I, Arrowsmith CH, Barsyte-Lovejoy D, Santhakumar V, Vedadi M, Halabelian L. (2023) Probing the mechanism of Cbl-b inhibition by a small-molecule inhibitor. bioRxiv 2023.05.05.539612; doi: https://doi.org/10.1101/2023.05.05.539612

Ong HW, Liang Y, Richardson W, Lowry ER, Wells CI, Chen X, Silvestre M, Dempster K, Silvaroli JA, Smith JL, Wichterle H, Pabla NS, Ultanir SK, Bullock AN, Drewry DH, Axtman AD. (2023) Discovery of a Potent and Selective CDKL5/GSK3 Chemical Probe That Is Neuroprotective. ACS Chem Neurosci. 14(9):1672-1685. doi: 10.1021/acschemneuro.3c00135

Balıkçı E, Marques AMC, Hansen JS, Huber KVM. (2023) Open resources for chemical probes and their implications for future drug discovery. Expert Opin Drug Discov. 18(5):505-513. doi:10.1080/17460441.2023.2199979

Ni X, Joerger AC, Chaikuad A, Knapp S. (2023) Structural insights into a regulatory mechanism of FIR RRM1-FUSE interaction. Open Biol. 13(5):230031. doi: 10.1098/rsob.230031

Youhanna S, Bruton J, Jardemark K, Westerblad H, Lauschke VM. (2023) Calcium measurements in enzymatically dissociated or mechanically microdissected mouse primary skeletal muscle fibers. STAR Protoc. 4(2):102260. doi: 10.1016/j.xpro.2023.102260

Tredup C, Ndreshkjana B, Schneider NS, Tjaden A, Kemas AM, Youhanna S, Lauschke VM, Berger BT, Krämer A, Berger LM, Röhm S, Knapp S, Farin HF, Müller S. (2023) Deep Annotation of Donated Chemical Probes (DCP) in Organotypic Human Liver Cultures and Patient-Derived Organoids from Tumor and Normal Colorectum. ACS Chem Biol. 18(4):822-836. doi:10.1021/acschembio.2c00877

Bashore FM, Marquez AB, Chaikuad A, Howell S, Dunn AS, Beltran AA, Smith JL, Drewry DH, Beltran AS, Axtman AD. (2023) Modulation of tau tubulin kinases (TTBK1 and TTBK2) impacts ciliogenesis. Sci Rep. 13(1):6118. doi: 10.1038/s41598-023-32854-4

Durcan TM, Axtman AD. (2023) Editorial: The next generation of tools and technologies for studying human neurons in a dish. Front Cell Neurosci. 17:1196543. doi: 10.3389/fncel.2023.1196543

Li ASM, Kimani S, Wilson B, Noureldin M, González-Álvarez H, Mamai A, Hoffer L, Guilinger JP, Zhang Y, von Rechenberg M, Disch JS, Mulhern CJ, Slakman BL, Cuozzo JW, Dong A, Poda G, Mohammed M, Saraon P, Mittal M, Modh P, Rathod V, Patel B, Ackloo S, Santhakumar V, Szewczyk MM, Barsyte-Lovejoy D, Arrowsmith CH, Marcellus R, Guié MA, Keefe AD, Brown PJ, Halabelian L, Al-Awar R, Vedadi M. (2023) Discovery of Nanomolar DCAF1 Small Molecule Ligands. J Med Chem. 66(7):5041-5060. doi:10.1021/acs.jmedchem.2c02132

Uliana F, Ciuffa R, Mishra R, Fossati A, Frommelt F, Keller S, Mehnert M, Birkeland ES, van Drogen F, Srejic N, Peter M, Tapon N, Aebersold R, Gstaiger M. (2023) Phosphorylation-linked complex profiling identifies assemblies required for Hippo signal integration. Mol Syst Biol. 19(4):e11024. doi:10.15252/msb.202211024

Mons E, Kim RQ, Mulder MPC. (2023) Technologies for Direct Detection of Covalent Protein-Drug Adducts. Pharmaceuticals (Basel). 16(4):547. Published 2023 Apr 5. doi:10.3390/ph16040547

Wright SC, Lauschke VM. (2023) Rewiring of catecholamine-induced calcium signalling is an early event in non-alcoholic fatty liver disease. J Physiol. 601(8):1317-1318. doi:10.1113/JP284526

Li F, Ghiabi P, Hajian T, Klima M, Li ASM, Khalili Yazdi A, Chau I, Loppnau P, Kutera M, Seitova A, Bolotokova A, Hutchinson A, Perveen S, Boura E, Vedadi M. (2023) SS148 and WZ16 inhibit the activities of nsp10-nsp16 complexes from all seven human pathogenic coronaviruses. Biochim Biophys Acta Gen Subj. 1867(4):130319. doi:10.1016/j.bbagen.2023.130319

Haubrich K, Spiteri VA, Farnaby W, Sobott F, Ciulli A. (2023) Breaking free from the crystal lattice: Structural biology in solution to study protein degraders. Curr Opin Struct Biol. 79:102534. doi:10.1016/j.sbi.2023.102534

Ayoubi R, Fotouhi M, Southern K, Bhajiawala R, Fanti R, Prinos P, McPherson PS, Laflamme C; NeuroSGC/YCharOS/EDDU collaborative group; ABIF Consortium. (2023) The identification of high-performing antibodies for transmembrane protein 106B (TMEM106B) for use in Western blot, immunoprecipitation, and immunofluorescence. F1000Res. 12:308. doi: 10.12688/f1000research.131333.1

Rogov VV, Nezis IP, Tsapras P, Zhang H, Dagdas Y, Noda NN, Nakatogawa H, Wirth M, Mouilleron S, McEwan DG, Behrends C, Deretic V, Elazar Z, Tooze SA, Dikic I, Lamark T, Johansen T. Atg8 family proteins, LIR/AIM motifs and other interaction modes. Autophagy Rep. 2(1):27694127.2023.2188523. doi: 10.1080/27694127.2023.2188523

Ackloo S, Antolin AA, Bartolome JM, Beck H, Bullock A, Betz UAK, Böttcher J, Brown PJ, Chaturvedi M, Crisp A, Daniels D, Dreher J, Edfeldt K, Edwards AM, Egner U, Elkins J, Fischer C, Glendorf T, Goldberg S, Hartung IV, Hillisch A, Homan E, Knapp S, Köster M, Krämer O, Llaveria J, Lessel U, Lindemann S, Linderoth L, Matsui H, Michel M, Montel F, Mueller-Fahrnow A, Müller S, Owen DR, Saikatendu KS, Santhakumar V, Sanderson W, Scholten C, Schapira M, Sharma S, Shireman B, Sundström M, Todd MH, Tredup C, Venable J, Willson TM, Arrowsmith CH. (2023) Target 2035 - an update on private sector contributions. RSC Med Chem. 14(6):1002-1011. Published 2023 Mar 16. doi:10.1039/d2md00441k

Martinelli P, Schaaf O, Mantoulidis A, Martin LJ, Fuchs JE, Bader G, Gollner A, Wolkerstorfer B, Rogers C, Balıkçı E, Lipp JJ, Mischerikow N, Doebel S, Gerstberger T, Sommergruber W, Huber KVM, Böttcher J. (2023) Discovery of a Chemical Probe to Study Implications of BPTF Bromodomain Inhibition in Cellular and in vivo Experiments. ChemMedChem. 18(6):e202200686. doi:10.1002/cmdc.202200686

Göricke F, Vu V, Smith L, Scheib U, Böhm R, Akkilic N, Wohlfahrt G, Weiske J, Bömer U, Brzezinka K, Lindner N, Lienau P, Gradl S, Beck H, Brown PJ, Santhakumar V, Vedadi M, Barsyte-Lovejoy D, Arrowsmith CH, Schmees N, Petersen K. (2023) Discovery and Characterization of BAY-805, a Potent and Selective Inhibitor of Ubiquitin-Specific Protease USP21. J Med Chem. 66(5):3431-3447. doi:10.1021/acs.jmedchem.2c01933

Němec V, Khirsariya P, Janovská P, Moyano PM, Maier L, Procházková P, Kebková P, Gybel' T, Berger BT, Chaikuad A, Reinecke M, Kuster B, Knapp S, Bryja V, Paruch K. (2023) Discovery of Potent and Exquisitely Selective Inhibitors of Kinase CK1 with Tunable Isoform Selectivity. Angew Chem Int Ed Engl. 62(11):e202217532. doi:10.1002/anie.202217532

Ong HW, Truong A, Kwarcinski F, de Silva C, Avalani K, Havener TM, Chirgwin M, Galal KA, Willis C, Krämer A, Liu S, Knapp S, Derbyshire ER, Zutshi R, Drewry DH.(2023) Discovery of potent Plasmodium falciparum protein kinase 6 (PfPK6) inhibitors with a type II inhibitor pharmacophore. Eur J Med Chem. 249:115043. doi:10.1016/j.ejmech.2022.115043

Aakula A, Sharma M, Tabaro F, Nätkin R, Kamila J, Honkanen H, Schapira M, Arrowsmith C, Nykter M, Westermarck J. (2023) RAS and PP2A activities converge on epigenetic gene regulation. Life Sci Alliance. 6(5):e202301928. Published 2023 Mar 1. doi:10.26508/lsa.202301928

Schwalm MP, Knapp S, Rogov VV. (2023) Toward effective Atg8-based ATTECs: Approaches and perspectives. J Cell Biochem. 2023 Feb 13. doi: 10.1002/jcb.30380. Epub ahead of print.

MacDonald KM, Nicholson-Puthenveedu S, Tageldein MM, Khasnis S, Arrowsmith CH, Harding SM. (2023) Antecedent chromatin organization determines cGAS recruitment to ruptured micronuclei. Nat Commun. 14(1):556. Published 2023 Feb 2. doi:10.1038/s41467-023-36195-8

Denis HL, Alpaugh M, Alvarez CP, Fenyi A, Barker RA, Chouinard S, Arrowsmith CH, Melki R, Labib R, Harding RJ, Cicchetti F. (2023) Detection of antibodies against the huntingtin protein in human plasma. Cell Mol Life Sci. 80(2):45. Published 2023 Jan 18. doi:10.1007/s00018-023-04687-x

Zhou J, Horton JR, Menna M, Fiorentino F, Ren R, Yu D, Hajian T, Vedadi M, Mazzoccanti G, Ciogli A, Weinhold E, Hüben M, Blumenthal RM, Zhang X, Mai A, Rotili D, Cheng X. (2023) Systematic Design of Adenosine Analogs as Inhibitors of a Clostridioides difficile-Specific DNA Adenine Methyltransferase Required for Normal Sporulation and Persistence. J Med Chem. 66(1):934-950. doi:10.1021/acs.jmedchem.2c01789

Antolin, A. A., Sanfelice, D., Crisp, A., Villasclaras Fernandez, E., Mica, I. L., Chen, Y., Collins, I., Edwards, A., Müller, S., Al-Lazikani, B., & Workman, P. (2023). The Chemical Probes Portal: an expert review-based public resource to empower chemical probe assessment, selection and use. Nucleic acids research, 51(D1), D1492–D1502. https://doi.org/10.1093/nar/gkac909

Taebnia N, Römling U, Lauschke VM. (2023) In vitro and ex vivo modeling of enteric bacterial infections. Gut Microbes. 15(1):2158034. doi:10.1080/19490976.2022.2158034

2022

Tjaden, A., Giessmann, R. T., Knapp, S., Schröder, M., & Müller, S. (2022). High-content live-cell multiplex screen for chemogenomic compound annotation based on nuclear morphology. STAR protocols, 3(4), 101791. https://doi.org/10.1016/j.xpro.2022.101791

Zandi Shafagh R, Youhanna S, Keulen J, Shen JX, Taebnia N, Preiss LC, Klein K, Büttner FA, Bergqvist M, van der Wijngaart W, Lauschke VM. (2022) Bioengineered Pancreas-Liver Crosstalk in a Microfluidic Coculture Chip Identifies Human Metabolic Response Signatures in Prediabetic Hyperglycemia. Adv Sci (Weinh). 9(34):e2203368. doi:10.1002/advs.202203368

Zhou Y, Lauschke VM. (2022) The genetic landscape of major drug metabolizing cytochrome P450 genes-an updated analysis of population-scale sequencing data. Pharmacogenomics J. 22(5-6):284-293. doi:10.1038/s41397-022-00288-2

Amrhein JA, Berger LM, Tjaden A, Krämer A, Elson L, Tolvanen T, Martinez-Molina D, Kaiser A, Schubert-Zsilavecz M, Müller S, Knapp S, Hanke T. (2022) Discovery of 3-Amino-1H-pyrazole-Based Kinase Inhibitors to Illuminate the Understudied PCTAIRE Family. Int J Mol Sci. 23(23):14834. Published 2022 Nov 27. doi:10.3390/ijms232314834

Rovers E, Liu L, Schapira M. ProxyBind: A compendium of binding sites for proximity-induced pharmacology. Comput Struct Biotechnol J. 2022;20:6163-6171. Published 2022 Nov 8. doi:10.1016/j.csbj.2022.11.010

Voorneveld, J., Kloet, M. S., Wijngaarden, S., Kim, R. Q., Moutsiopoulou, A., Verdegaal, M., Misra, M., Đikić, I., van der Marel, G. A., Overkleeft, H. S., Filippov, D. V., & van der Heden van Noort, G. J. (2022). Arginine ADP-Ribosylation: Chemical Synthesis of Post-Translationally Modified Ubiquitin Proteins. Journal of the American Chemical Society, 144(45), 20582–20589. https://doi.org/10.1021/jacs.2c06249

Chaikuad, A., Zhubi, R., Tredup, C., & Knapp, S. (2022). Comparative structural analyses of the NHL domains from the human E3 ligase TRIM-NHL family. IUCrJ, 9(Pt 6), 720–727. https://doi.org/10.1107/S2052252522008582

Payliss BJ, Tse YWE, Reichheld SE, Lemak A, Yun HY, Houliston S, Patel A, Arrowsmith CH, Sharpe S, Wyatt HDM. (2022) Phosphorylation of the DNA repair scaffold SLX4 drives folding of the SAP domain and activation of the MUS81-EME1 endonuclease. Cell Rep. 41(4):111537. doi:10.1016/j.celrep.2022.111537

Ketley RF, Battistini F, Alagia A, Mondielli C, Iehl F, Balikçi E, Huber KVM, Orozco M, Gullerova M. (2022) DNA double-strand break-derived RNA drives TIRR/53BP1 complex dissociation. Cell Rep. 41(4):111526. doi:10.1016/j.celrep.2022.111526

Pentinmikko N, Lozano R, Scharaw S, Andersson S, Englund JI, Castillo-Azofeifa D, Gallagher A, Broberg M, Song KY, Sola Carvajal A, Speidel AT, Sundstrom M, Allbritton N, Stevens MM, Klein OD, Teixeira A, Katajisto P. (2022) Cellular shape reinforces niche to stem cell signaling in the small intestine. Sci Adv. 8(41):eabm1847. doi:10.1126/sciadv.abm1847

Hanke, T., Mathea, S., Woortman, J., Salah, E., Berger, B. T., Tumber, A., Kashima, R., Hata, A., Kuster, B., Müller, S., & Knapp, S. (2022). Development and Characterization of Type I, Type II, and Type III LIM-Kinase Chemical Probes. Journal of medicinal chemistry, 65(19), 13264–13287. https://doi.org/10.1021/acs.jmedchem.2c01106

Jia Y, Kim RQ, Kooij R, Ovaa H, Sapmaz A, Geurink PP. (2022) Chemical Toolkit for PARK7: Potent, Selective, and High-Throughput. J Med Chem. 65(19):13288-13304. doi:10.1021/acs.jmedchem.2c01113

Kim TE, Tsuboyama K, Houliston S, Martell CM, Phoumyvong CM, Lemak A, Haddox HK, Arrowsmith CH, Rocklin GJ. (2022) Dissecting the stability determinants of a challenging de novo protein fold using massively parallel design and experimentation. Proc Natl Acad Sci U S A. 119(41):e2122676119. doi:10.1073/pnas.2122676119

Lesbon, J. C. C., Garnica, T. K., Xavier, P. L. P., Rochetti, A. L., Reis, R. M., Müller, S., & Fukumasu, H. (2022). A Screening of Epigenetic Therapeutic Targets for Non-Small Cell Lung Cancer Reveals PADI4 and KDM6B as Promising Candidates. International journal of molecular sciences, 23(19), 11911. https://doi.org/10.3390/ijms231911911

Ciuffa R, Uliana F, Mannion J, Mehnert M, Tenev T, Marulli C, Satanowski A, Keller LML, Rodilla Ramírez PN, Ori A, Gstaiger M, Meier P, Aebersold R. (2022) Novel biochemical, structural, and systems insights into inflammatory signaling revealed by contextual interaction proteomics. Proc Natl Acad Sci U S A. 119(40):e2117175119. doi:10.1073/pnas.2117175119

Chidyausiku TM, Mendes SR, Klima JC, Nadal M, Eckhard U, Roel-Touris J, Houliston S, Guevara T, Haddox HK, Moyer A, Arrowsmith CH, Gomis-Rüth FX, Baker D, Marcos E. (2022) De novo design of immunoglobulin-like domains. Nat Commun. 13(1):5661. Published 2022 Oct 3. doi:10.1038/s41467-022-33004-6

Liu L, Rovers E, Schapira M. (2022) ChemBioPort: an online portal to navigate the structure, function and chemical inhibition of the human proteome. Database (Oxford). 2022:baac088. doi:10.1093/database/baac088

Wallner O, Cázares-Körner A, Scaletti ER, Masuyer G, Bekkhus T, Visnes T, Mamonov K, Ortis F, Lundbäck T, Volkova M, Koolmeister T, Wiita E, Loseva O, Pandey M, Homan E, Benítez-Buelga C, Davies J, Scobie M, Warpman Berglund U, Kalderén C, Stenmark P, Helleday T, Michel M. (2023) Optimization of N-Piperidinyl-Benzimidazolone Derivatives as Potent and Selective Inhibitors of 8-Oxo-Guanine DNA Glycosylase 1. ChemMedChem. 18(1):e202200310. doi:10.1002/cmdc.202200310

Liu Y, Iqbal A, Li W, Ni Z, Wang Y, Ramprasad J, Abraham KJ, Zhang M, Zhao DY, Qin S, Loppnau P, Jiang H, Guo X, Brown PJ, Zhen X, Xu G, Mekhail K, Ji X, Bedford MT, Greenblatt JF, Min J. (2022) A small molecule antagonist of SMN disrupts the interaction between SMN and RNAP II. Nat Commun. 13(1):5453. Published 2022 Sep 16. doi:10.1038/s41467-022-33229-5

Fraser BJ, Beldar S, Seitova A, Hutchinson A, Mannar D, Li Y, Kwon D, Tan R, Wilson RP, Leopold K, Subramaniam S, Halabelian L, Arrowsmith CH, Bénard F. (2022) Structure and activity of human TMPRSS2 protease implicated in SARS-CoV-2 activation. Nat Chem Biol. 18(9):963-971. doi:10.1038/s41589-022-01059-7

Liu, X., Kalogeropulou, A. F., Domingos, S., Makukhin, N., Nirujogi, R. S., Singh, F., Shpiro, N., Saalfrank, A., Sammler, E., Ganley, I. G., Moreira, R., Alessi, D. R., & Ciulli, A. (2022). Discovery of XL01126: A Potent, Fast, Cooperative, Selective, Orally Bioavailable, and Blood-Brain Barrier Penetrant PROTAC Degrader of Leucine-Rich Repeat Kinase 2. Journal of the American Chemical Society, 144(37), 16930–16952. https://doi.org/10.1021/jacs.2c05499

Wu Q, Nie DY, Ba-Alawi W, Ji Y, Zhang Z, Cruickshank J, Haight J, Ciamponi FE, Chen J, Duan S, Shen Y, Liu J, Marhon SA, Mehdipour P, Szewczyk MM, Dogan-Artun N, Chen W, Zhang LX, Deblois G, Prinos P, Massirer KB, Barsyte-Lovejoy D, Jin J, De Carvalho DD, Haibe-Kains B, Wang X, Cescon DW, Lupien M, Arrowsmith CH. (2022) PRMT inhibition induces a viral mimicry response in triple-negative breast cancer. Nat Chem Biol. 18(8):821-830. doi:10.1038/s41589-022-01024-4

Trush, V. V., Feller, C., Li, A. S. M., Allali-Hassani, A., Szewczyk, M. M., Chau, I., Eram, M. S., Jiang, B., Luu, R., Zhang, F., Barsyte-Lovejoy, D., Aebersold, R., Arrowsmith, C. H., & Vedadi, M. (2022). Enzymatic nucleosome acetylation selectively affects activity of histone methyltransferases in vitro. Biochimica et biophysica acta. Gene regulatory mechanisms, 1865(5), 194845. https://doi.org/10.1016/j.bbagrm.2022.194845

Tsika, A. C., Gallo, A., Fourkiotis, N. K., Argyriou, A. I., Sreeramulu, S., Löhr, F., Rogov, V. V., Richter, C., Linhard, V., Gande, S. L., Altincekic, N., Krishnathas, R., Elamri, I., Schwalbe, H., Wollenhaupt, J., Weiss, M. S., & Spyroulias, G. A. (2022). Binding Adaptation of GS-441524 Diversifies Macro Domains and Downregulates SARS-CoV-2 de-MARylation Capacity. Journal of molecular biology, 434(16), 167720. https://doi.org/10.1016/j.jmb.2022.167720

Michel M, Benítez-Buelga C, Calvo PA, Hanna BMF, Mortusewicz O, Masuyer G, Davies J, Wallner O, Sanjiv K, Albers JJ, Castañeda-Zegarra S, Jemth AS, Visnes T, Sastre-Perona A, Danda AN, Homan EJ, Marimuthu K, Zhenjun Z, Chi CN, Sarno A, Wiita E, von Nicolai C, Komor AJ, Rajagopal V, Müller S, Hank EC, Varga M, Scaletti ER, Pandey M, Karsten S, Haslene-Hox H, Loevenich S, Marttila P, Rasti A, Mamonov K, Ortis F, Schömberg F, Loseva O, Stewart J, D'Arcy-Evans N, Koolmeister T, Henriksson M, Michel D, de Ory A, Acero L, Calvete O, Scobie M, Hertweck C, Vilotijevic I, Kalderén C, Osorio A, Perona R, Stolz A, Stenmark P, Berglund UW, de Vega M, Helleday T. (2022) Small-molecule activation of OGG1 increases oxidative DNA damage repair by gaining a new function. Science. 376(6600):1471-1476. doi: 10.1126/science.abf8980

Jemth AS, Scaletti ER, Homan E, Stenmark P, Helleday T, Michel M. (2022) Nudix hydrolase 18 catalyzes the hydrolysis of active triphosphate metabolites of the antivirals remdesivir, ribavirin, and molnupiravir. J Biol Chem. 298(8):102169. doi:10.1016/j.jbc.2022.102169

Tolvanen TA. (2022) Current Advances in CETSA. Front Mol Biosci. 9:866764. Published 2022 Jun 9. doi:10.3389/fmolb.2022.866764

Zhou, Y., & Lauschke, V. M. (2022). Population pharmacogenomics: an update on ethnogeographic differences and opportunities for precision public health. Human genetics, 141(6), 1113–1136. https://doi.org/10.1007/s00439-021-02385-x

Schwalm, M. P., Berger, L. M., Meuter, M. N., Vasta, J. D., Corona, C. R., Röhm, S., Berger, B. T., Farges, F., Beinert, S. M., Preuss, F., Morasch, V., Rogov, V. V., Mathea, S., Saxena, K., Robers, M. B., Müller, S., & Knapp, S. (2022). A Toolbox for the Generation of Chemical Probes for Baculovirus IAP Repeat Containing Proteins. Frontiers in cell and developmental biology, 10, 886537. https://doi.org/10.3389/fcell.2022.886537

Cruz Walma, D. A., Chen, Z., Bullock, A. N., & Yamada, K. M. (2022). Ubiquitin ligases: guardians of mammalian development. Nature reviews. Molecular cell biology, 23(5), 350–367. https://doi.org/10.1038/s41580-021-00448-5

Stork, B. A., Dean, A., Ortiz, A. R., Saha, P., Putluri, N., Planas-Silva, M. D., Mahmud, I., Rajapakshe, K., Coarfa, C., Knapp, S., Lorenzi, P. L., Kemp, B. E., Turk, B. E., Scott, J. W., Means, A. R., & York, B. (2022). Calcium/calmodulin-dependent protein kinase kinase 2 regulates hepatic fuel metabolism. Molecular metabolism, 62, 101513. https://doi.org/10.1016/j.molmet.2022.101513

Willems, S., Marschner, J. A., Kilu, W., Faudone, G., Busch, R., Duensing-Kropp, S., Heering, J., & Merk, D. (2022). Nurr1 Modulation Mediates Neuroprotective Effects of Statins. Advanced science (Weinheim, Baden-Wurttemberg, Germany), e2104640. Advance online publication. https://doi.org/10.1002/advs.202104640

Willems, S., Müller, M., Ohrndorf, J., Heering, J., Proschak, E., & Merk, D. (2022). Scaffold Hopping from Amodiaquine to Novel Nurr1 Agonist Chemotypes via Microscale Analogue Libraries. ChemMedChem, 17(8), e202200026. https://doi.org/10.1002/cmdc.202200026

Isigkeit, L., Chaikuad, A., & Merk, D. (2022). A Consensus Compound/Bioactivity Dataset for Data-Driven Drug Design and Chemogenomics. Molecules (Basel, Switzerland), 27(8), 2513. https://doi.org/10.3390/molecules27082513

Borsari, C., Keles, E., McPhail, J. A., Schaefer, A., Sriramaratnam, R., Goch, W., Schaefer, T., De Pascale, M., Bal, W., Gstaiger, M., Burke, J. E., & Wymann, M. P. (2022). Covalent Proximity Scanning of a Distal Cysteine to Target PI3Kα. Journal of the American Chemical Society, 144(14), 6326–6342. https://doi.org/10.1021/jacs.1c13568

Sun, Z. W., Waybright, J. M., Beldar, S., Chen, L., Foley, C. A., Norris-Drouin, J. L., Lyu, T. J., Dong, A., Min, J., Wang, Y. P., James, L. I., & Wang, Y. (2022). Cdyl Deficiency Brakes Neuronal Excitability and Nociception through Promoting Kcnb1 Transcription in Peripheral Sensory Neurons. Advanced science (Weinheim, Baden-Wurttemberg, Germany), 9(10), e2104317. https://doi.org/10.1002/advs.202104317

Wei, Y., Redel, C., Ahlner, A., Lemak, A., Johansson-Åkhe, I., Houliston, S., Kenney, T., Tamachi, A., Morad, V., Duan, S., Andrews, D. W., Wallner, B., Sunnerhagen, M., Arrowsmith, C. H., & Penn, L. Z. (2022). The MYC oncoprotein directly interacts with its chromatin cofactor PNUTS to recruit PP1 phosphatase. Nucleic acids research, 50(6), 3505–3522. https://doi.org/10.1093/nar/gkac138

Chen, Z., Ioris, R. M., Richardson, S., Van Ess, A. N., Vendrell, I., Kessler, B. M., Buffa, F. M., Busino, L., Clifford, S. C., Bullock, A. N., & D'Angiolella, V. (2022). Disease-associated KBTBD4 mutations in medulloblastoma elicit neomorphic ubiquitylation activity to promote CoREST degradation. Cell death and differentiation, 10.1038/s41418-022-00983-4. Advance online publication. https://doi.org/10.1038/s41418-022-00983-4

Srour, N., Villarreal, O. D., Hardikar, S., Yu, Z., Preston, S., Miller, W. H., Jr, Szewczyk, M. M., Barsyte-Lovejoy, D., Xu, H., Chen, T., Del Rincón, S. V., & Richard, S. (2022). PRMT7 ablation stimulates anti-tumor immunity and sensitizes melanoma to immune checkpoint blockade. Cell reports, 38(13), 110582. https://doi.org/10.1016/j.celrep.2022.110582

Kemas, A. M., Youhanna, S., & Lauschke, V. M. (2022) Non-alcoholic fatty liver disease - opportunities for personalized treatment and drug development. Expert Review of Precision Medicine and Drug Development, 7(1), 39–49. https://doi.org/10.1080/23808993.2022.2053285

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Szewczyk, M. M., Luciani, G. M., Vu, V., Murison, A., Dilworth, D., Barghout, S. H., Lupien, M., Arrowsmith, C. H., Minden, M. D., & Barsyte-Lovejoy, D. (2022). PRMT5 regulates ATF4 transcript splicing and oxidative stress response. Redox biology, 51, 102282. https://doi.org/10.1016/j.redox.2022.102282

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2021

Delaney, K., Tan, M., Zhu, Z., Gao, J., Dai, L., Kim, S., Ding, J., He, M., Halabelian, L., Yang, L., Nagarajan, P., Parthun, M. R., Lee, S., Khochbin, S., Zheng, Y. G., & Zhao, Y. (2021). Histone lysine methacrylation is a dynamic post-translational modification regulated by HAT1 and SIRT2. Cell discovery, 7(1), 122. https://doi.org/10.1038/s41421-021-00344-4

Klein, V. G., Bond, A. G., Craigon, C., Lokey, R. S., & Ciulli, A. (2021). Amide-to-Ester Substitution as a Strategy for Optimizing PROTAC Permeability and Cellular Activity. Journal of medicinal chemistry, 64(24), 18082–18101. https://doi.org/10.1021/acs.jmedchem.1c01496

Harding, R. J., Deme, J. C., Hevler, J. F., Tamara, S., Lemak, A., Cantle, J. P., Szewczyk, M. M., Begeja, N., Goss, S., Zuo, X., Loppnau, P., Seitova, A., Hutchinson, A., Fan, L., Truant, R., Schapira, M., Carroll, J. B., Heck, A., Lea, S. M., & Arrowsmith, C. H. (2021). Huntingtin structure is orchestrated by HAP40 and shows a polyglutamine expansion-specific interaction with exon 1. Communications biology, 4(1), 1374. https://doi.org/10.1038/s42003-021-02895-4

Müller, S., Ackloo, S., Al Chawaf, A., Al-Lazikani, B., Antolin, A., Baell, J. B., Beck, H., Beedie, S., Betz, U., Bezerra, G. A., Brennan, P. E., Brown, D., Brown, P. J., Bullock, A. N., Carter, A. J., Chaikuad, A., Chaineau, M., Ciulli, A., Collins, I., Dreher, J., … Arrowsmith, C. H. (2021). Target 2035 - update on the quest for a probe for every protein. RSC medicinal chemistry, 13(1), 13–21. https://doi.org/10.1039/d1md00228g

Azzimato, V., Chen, P., Barreby, E., Morgantini, C., Levi, L., Vankova, A., Jager, J., Sulen, A., Diotallevi, M., Shen, J. X., Miller, A., Ellis, E., Rydén, M., Näslund, E., Thorell, A., Lauschke, V. M., Channon, K. M., Crabtree, M. J., Haschemi, A., Craige, S. M., … Aouadi, M. (2021). Hepatic miR-144 Drives Fumarase Activity Preventing NRF2 Activation During Obesity. Gastroenterology, 161(6), 1982–1997.e11. https://doi.org/10.1053/j.gastro.2021.08.030

Chen, S., Zhou, M., Dong, A., Loppnau, P., Wang, M., Min, J., & Liu, K. (2021). Structural basis of the TAM domain of BAZ2A in binding to DNA or RNA independent of methylation status. The Journal of biological chemistry, 297(6), 101351. https://doi.org/10.1016/j.jbc.2021.101351

Laveglia, V., Giachetti, A., Cerofolini, L., Haubrich, K., Fragai, M., Ciulli, A., & Rosato, A. (2021). Automated Determination of Nuclear Magnetic Resonance Chemical Shift Perturbations in Ligand Screening Experiments: The PICASSO Web Server. Journal of chemical information and modeling, 61(12), 5726–5733. https://doi.org/10.1021/acs.jcim.1c00871

Imaide, S., Riching, K. M., Makukhin, N., Vetma, V., Whitworth, C., Hughes, S. J., Trainor, N., Mahan, S. D., Murphy, N., Cowan, A. D., Chan, K. H., Craigon, C., Testa, A., Maniaci, C., Urh, M., Daniels, D. L., & Ciulli, A. (2021). Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity. Nature chemical biology, 17(11), 1157–1167. https://doi.org/10.1038/s41589-021-00878-4

Yu, D., Horton, J. R., Yang, J., Hajian, T., Vedadi, M., Sagum, C. A., Bedford, M. T., Blumenthal, R. M., Zhang, X., & Cheng, X. (2021). Human MettL3-MettL14 RNA adenine methyltransferase complex is active on double-stranded DNA containing lesions. Nucleic acids research, 49(20), 11629–11642. https://doi.org/10.1093/nar/gkab460

Guegueniat, J., Halabelian, L., Zeng, H., Dong, A., Li, Y., Wu, H., Arrowsmith, C. H., & Kothe, U. (2021). The human pseudouridine synthase PUS7 recognizes RNA with an extended multi-domain binding surface. Nucleic acids research, 49(20), 11810–11822. https://doi.org/10.1093/nar/gkab934

Lyczek, A., Berger, B. T., Rangwala, A. M., Paung, Y., Tom, J., Philipose, H., Guo, J., Albanese, S. K., Robers, M. B., Knapp, S., Chodera, J. D., & Seeliger, M. A. (2021). Mutation in Abl kinase with altered drug-binding kinetics indicates a novel mechanism of imatinib resistance. Proceedings of the National Academy of Sciences of the United States of America, 118(46), e2111451118. https://doi.org/10.1073/pnas.2111451118

Dilworth, D., Hanley, R. P., Ferreira de Freitas, R., Allali-Hassani, A., Zhou, M., Mehta, N., Marunde, M. R., Ackloo, S., Carvalho Machado, R. A., Khalili Yazdi, A., Owens, D., Vu, V., Nie, D. Y., Alqazzaz, M., Marcon, E., Li, F., Chau, I., Bolotokova, A., Qin, S., Lei, M., … Schapira, M. (2022). A chemical probe targeting the PWWP domain alters NSD2 nucleolar localization. Nature chemical biology, 18(1), 56–63. https://doi.org/10.1038/s41589-021-00898-0

Koromina, M., Pandi, M. T., van der Spek, P. J., Patrinos, G. P., & Lauschke, V. M. (2021). The ethnogeographic variability of genetic factors underlying G6PD deficiency. Pharmacological research, 173, 105904. https://doi.org/10.1016/j.phrs.2021.105904

Attwood, M. M., Fabbro, D., Sokolov, A. V., Knapp, S., & Schiöth, H. B. (2021). Trends in kinase drug discovery: targets, indications and inhibitor design. Nature reviews. Drug discovery, 20(11), 839–861. https://doi.org/10.1038/s41573-021-00252-y

Chen, S., Zhou, M., Dong, A., Loppnau, P., Wang, M., Min, J., & Liu, K. (2021). Structural basis of the TAM domain of BAZ2A in binding to DNA or RNA independent of methylation status. The Journal of biological chemistry, 297(6), 101351. https://doi.org/10.1016/j.jbc.2021.101351

Imaide, S., Riching, K. M., Makukhin, N., Vetma, V., Whitworth, C., Hughes, S. J., Trainor, N., Mahan, S. D., Murphy, N., Cowan, A. D., Chan, K. H., Craigon, C., Testa, A., Maniaci, C., Urh, M., Daniels, D. L., & Ciulli, A. (2021). Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity. Nature chemical biology, 17(11), 1157–1167. https://doi.org/10.1038/s41589-021-00878-4

Guo, Y., Liu, Q., Mallette, E., Caba, C., Hou, F., Fux, J., LaPlante, G., Dong, A., Zhang, Q., Zheng, H., Tong, Y., & Zhang, W. (2021). Structural and functional characterization of ubiquitin variant inhibitors for the JAMM-family deubiquitinases STAMBP and STAMBPL1. The Journal of biological chemistry, 297(4), 101107. https://doi.org/10.1016/j.jbc.2021.101107

Röhm, S., Berger, B. T., Schröder, M., Chatterjee, D., Mathea, S., Joerger, A. C., Pinkas, D. M., Bufton, J. C., Tjaden, A., Kovooru, L., Kudolo, M., Pohl, C., Bullock, A. N., Müller, S., Laufer, S., & Knapp, S. (2021). Development of a Selective Dual Discoidin Domain Receptor (DDR)/p38 Kinase Chemical Probe. Journal of medicinal chemistry, 64(18), 13451–13474. https://doi.org/10.1021/acs.jmedchem.1c00868

Robers, M. B., Wilkinson, J. M., Vasta, J. D., Berger, L. M., Berger, B. T., & Knapp, S. (2021). Single tracer-based protocol for broad-spectrum kinase profiling in live cells with NanoBRET. STAR protocols, 2(4), 100822. https://doi.org/10.1016/j.xpro.2021.100822

Zhou, Y., Arribas, G. H., Turku, A., Jürgenson, T., Mkrtchian, S., Krebs, K., Wang, Y., Svobodova, B., Milani, L., Schulte, G., Korabecny, J., Gastaldello, S., & Lauschke, V. M. (2021). Rare genetic variability in human drug target genes modulates drug response and can guide precision medicine. Science advances, 7(36), eabi6856. https://doi.org/10.1126/sciadv.abi6856

Ali, M., McAuley, M. M., Lüchow, S., Knapp, S., Joerger, A. C., & Ivarsson, Y. (2021). Integrated analysis of Shank1 PDZ interactions with C-terminal and internal binding motifs. Current research in structural biology, 3, 41–50. https://doi.org/10.1016/j.crstbi.2021.01.001

Otava, T., Šála, M., Li, F., Fanfrlík, J., Devkota, K., Perveen, S., Chau, I., Pakarian, P., Hobza, P., Vedadi, M., Boura, E., & Nencka, R. (2021). The Structure-Based Design of SARS-CoV-2 nsp14 Methyltransferase Ligands Yields Nanomolar Inhibitors. ACS infectious diseases, 7(8), 2214–2220. https://doi.org/10.1021/acsinfecdis.1c00131

Henderson, S. H., Sorrell, F., Bennett, J., Fedorov, O., Hanley, M. T., Godoi, P. H., Ruela de Sousa, R., Robinson, S., Ashall-Kelly, A., Hopkins Navratilova, I., Walter, D. S., Elkins, J. M., & Ward, S. E. (2021). Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors. Journal of medicinal chemistry, 64(15), 11709–11728. https://doi.org/10.1021/acs.jmedchem.1c01115

Schröder, M., & Chaikuad, A. (2021). Assessing reversible and irreversible binding effects of kinase covalent inhibitors through ADP-Glo assays. STAR protocols, 2(3), 100717. https://doi.org/10.1016/j.xpro.2021.100717

Reggio, A., Buonomo, V., Berkane, R., Bhaskara, R. M., Tellechea, M., Peluso, I., Polishchuk, E., Di Lorenzo, G., Cirillo, C., Esposito, M., Hussain, A., Huebner, A. K., Hübner, C. A., Settembre, C., Hummer, G., Grumati, P., & Stolz, A. (2021). Role of FAM134 paralogues in endoplasmic reticulum remodeling, ER-phagy, and Collagen quality control. EMBO reports, e52289. Advance online publication. https://doi.org/10.15252/embr.202052289

Drewry, D. H., Annor-Gyamfi, J. K., Wells, C. I., Pickett, J. E., Dederer, V., Preuss, F., Mathea, S., & Axtman, A. D. (2022). Identification of Pyrimidine-Based Lead Compounds for Understudied Kinases Implicated in Driving Neurodegeneration. Journal of medicinal chemistry, 65(2), 1313–1328. https://doi.org/10.1021/acs.jmedchem.1c00440

Youhanna, S., Wright, S. C., & Lauschke, V. M. (2021). Organotypic human ex vivo models for coronavirus disease 2019 research and drug development. Current opinion in pharmacology, 59, 11–18. https://doi.org/10.1016/j.coph.2021.04.006

Halabelian, L., & Barsyte-Lovejoy, D. (2021). Structure and Function of Protein Arginine Methyltransferase PRMT7. Life (Basel, Switzerland), 11(8), 768. https://doi.org/10.3390/life11080768

Edwards, A., & Hartung, I. V. (2021). No shortcuts to SARS-CoV-2 antivirals. Science (New York, N.Y.), 373(6554), 488–489. https://doi.org/10.1126/science.abj9488

Stebbing, J., & Lauschke, V. M. (2021). JAK Inhibitors - More Than Just Glucocorticoids. The New England journal of medicine, 385(5), 463–465. https://doi.org/10.1056/NEJMe2108667

Raab, M., Rak, M., Tesch, R., Gasimli, K., Becker, S., Knapp, S., Strebhardt, K., & Sanhaji, M. (2021). The Small-Molecule Inhibitor MRIA9 Reveals Novel Insights into the Cell Cycle Roles of SIK2 in Ovarian Cancer Cells. Cancers, 13(15), 3658. https://doi.org/10.3390/cancers13153658

Nonga, O. E., Lavogina, D., Enkvist, E., Kestav, K., Chaikuad, A., Dixon-Clarke, S. E., Bullock, A. N., Kopanchuk, S., Ivan, T., Ekambaram, R., Viht, K., Knapp, S., & Uri, A. (2021). Crystal Structure-Guided Design of Bisubstrate Inhibitors and Photoluminescent Probes for Protein Kinases of the PIM Family. Molecules (Basel, Switzerland), 26(14), 4353. https://doi.org/10.3390/molecules26144353

Wesch, N., Löhr, F., Rogova, N., Dötsch, V., & Rogov, V. V. (2021). A Concerted Action of UBA5 C-Terminal Unstructured Regions Is Important for Transfer of Activated UFM1 to UFC1. International journal of molecular sciences, 22(14), 7390. https://doi.org/10.3390/ijms22147390

Shen, J. X., Couchet, M., Dufau, J., de Castro Barbosa, T., Ulbrich, M. H., Helmstädter, M., Kemas, A. M., Zandi Shafagh, R., Marques, M. A., Hansen, J. B., Mejhert, N., Langin, D., Rydén, M., & Lauschke, V. M. (2021). 3D Adipose Tissue Culture Links the Organotypic Microenvironment to Improved Adipogenesis. Advanced science (Weinheim, Baden-Wurttemberg, Germany), 8(16), e2100106. https://doi.org/10.1002/advs.202100106

Pernaute-Lau, L., Adegnika, A. A., Zhou, Y., Zinsou, J. F., Gil, J. P., Krishna, S., Kremsner, P. G., Lauschke, V. M., & Velavan, T. P. (2021). Pharmacogene Sequencing of a Gabonese Population with Severe Plasmodium falciparum Malaria Reveals Multiple Novel Variants with Putative Relevance for Antimalarial Treatment. Antimicrobial agents and chemotherapy, 65(7), e0027521. https://doi.org/10.1128/AAC.00275-21

Schmidt, S. H., Weng, J. H., Aoto, P. C., Boassa, D., Mathea, S., Silletti, S., Hu, J., Wallbott, M., Komives, E. A., Knapp, S., Herberg, F. W., & Taylor, S. S. (2021). Conformation and dynamics of the kinase domain drive subcellular location and activation of LRRK2. Proceedings of the National Academy of Sciences of the United States of America, 118(23), e2100844118. https://doi.org/10.1073/pnas.2100844118

Wallner, O., Mamonov, K., Ortis, F., Michel, D., Michel, M. (2021). Assembly and Application of a Low Budget Photoreactor. Chemistry – Methods 1(5), 240-244. https://doi.org/10.1002/cmtd.202100022

Russell, L. E., Zhou, Y., Almousa, A. A., Sodhi, J. K., Nwabufo, C. K., & Lauschke, V. M. (2021). Pharmacogenomics in the era of next generation sequencing - from byte to bedside. Drug metabolism reviews, 53(2), 253–278. https://doi.org/10.1080/03602532.2021.1909613

Zhou, Y., & Lauschke, V. M. (2021). Computational Tools to Assess the Functional Consequences of Rare and Noncoding Pharmacogenetic Variability. Clinical pharmacology and therapeutics, 10.1002/cpt.2289. Advance online publication. https://doi.org/10.1002/cpt.2289

Dölle, A., Adhikari, B., Krämer, A., Weckesser, J., Berner, N., Berger, L. M., Diebold, M., Szewczyk, M. M., Barsyte-Lovejoy, D., Arrowsmith, C. H., Gebel, J., Löhr, F., Dötsch, V., Eilers, M., Heinzlmeir, S., Kuster, B., Sotriffer, C., Wolf, E., & Knapp, S. (2021). Design, Synthesis, and Evaluation of WD-Repeat-Containing Protein 5 (WDR5) Degraders. Journal of medicinal chemistry, 64(15), 10682–10710. https://doi.org/10.1021/acs.jmedchem.1c00146

Gama-Brambila, R. A., Chen, J., Dabiri, Y., Tascher, G., Němec, V., Münch, C., Song, G., Knapp, S., & Cheng, X. (2021). A Chemical Toolbox for Labeling and Degrading Engineered Cas Proteins. JACS Au, 1(6), 777–785. https://doi.org/10.1021/jacsau.1c00007

Wanior, M., Krämer, A., Knapp, S., & Joerger, A. C. (2021). Exploiting vulnerabilities of SWI/SNF chromatin remodelling complexes for cancer therapy. Oncogene, 40(21), 3637–3654. https://doi.org/10.1038/s41388-021-01781-x

Ma, T., Hu, C., Lal, B., Zhou, W., Ma, Y., Ying, M., Prinos, P., Quiñones-Hinojosa, A., Lim, M., Laterra, J., & Li, Y. (2021). Reprogramming Transcription Factors Oct4 and Sox2 Induce a BRD-Dependent Immunosuppressive Transcriptome in GBM-Propagating Cells. Cancer research, 81(9), 2457–2469. https://doi.org/10.1158/0008-5472.CAN-20-2489

Yadav, J., El Hassani, M., Sodhi, J., Lauschke, V. M., Hartman, J. H., & Russell, L. E. (2021). Recent developments in in vitro and in vivo models for improved translation of preclinical pharmacokinetics and pharmacodynamics data. Drug metabolism reviews, 53(2), 207–233. https://doi.org/10.1080/03602532.2021.1922435

Ingelman-Sundberg, M., & Lauschke, V. M. (2021). 3D human liver spheroids for translational pharmacology and toxicology. Basic & clinical pharmacology & toxicology, 10.1111/bcpt.13587. Advance online publication. https://doi.org/10.1111/bcpt.13587

Luparello, C., Cruciata, I., Joerger, A. C., Ocasio, C. A., Jones, R., Tareque, R. K., Bagley, M. C., Spencer, J., Walker, M., Austin, C., Ferrara, T., D Oca, P., Bellina, R., Branni, R., & Caradonna, F. (2021). Genotoxicity and Epigenotoxicity of Carbazole-Derived Molecules on MCF-7 Breast Cancer Cells. International journal of molecular sciences, 22(7), 3410. https://doi.org/10.3390/ijms22073410

Ni, X., Londregan, A. T., Owen, D. R., Knapp, S., & Chaikuad, A. (2021). Structure and Inhibitor Binding Characterization of Oncogenic MLLT1 Mutants. ACS chemical biology, 16(4), 571–578. https://doi.org/10.1021/acschembio.0c00960

Karatas, M., Chaikuad, A., Berger, B., Kubbutat, M., Totzke, F., Knapp, S., & Kunick, C. (2021). 7-(2-Anilinopyrimidin-4-yl)-1-benzazepin-2-ones Designed by a "Cut and Glue" Strategy Are Dual Aurora A/VEGF-R Kinase Inhibitors. Molecules (Basel, Switzerland), 26(6), 1611. https://doi.org/10.3390/molecules26061611

Lauschke V. M. (2021). Toxicogenomics of drug induced liver injury - from mechanistic understanding to early prediction. Drug metabolism reviews, 53(2), 245–252. https://doi.org/10.1080/03602532.2021.1894571

Kemas, A. M., Youhanna, S., Zandi Shafagh, R., & Lauschke, V. M. (2021). Insulin-dependent glucose consumption dynamics in 3D primary human liver cultures measured by a sensitive and specific glucose sensor with nanoliter input volume. FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 35(3), e21305. https://doi.org/10.1096/fj.202001989RR

Santhakumar, V., Sutherland, M., Li, A., Kaghad, A., Panagopoulos, D., Li, F., Szewczyk, M., Smil, D., Scholten, C., Bouché, L., Stellfeld, T., Arrowsmith, C. H., Barsyte, D., Vedadi, M., Hartung, I. V., Steuber, H., & Britton, R. (2021). Rational Design and Synthesis of Selective PRMT4 Inhibitors: a New Chemotype for Development of Cancer Therapeutics. ChemMedChem, 10.1002/cmdc.202100018. Advance online publication. https://doi.org/10.1002/cmdc.202100018

Williams, E., Riesebos, E., Kerr, G., & Bullock, A. N. (2021). ALK2 Receptor Kinase Association with FKBP12.6 Is Structurally Conserved with the ALK2-FKBP12 Complex. Biomedicines, 9(2), 129. https://doi.org/10.3390/biomedicines9020129

Berger, B. T., Amaral, M., Kokh, D. B., Nunes-Alves, A., Musil, D., Heinrich, T., Schröder, M., Neil, R., Wang, J., Navratilova, I., Bomke, J., Elkins, J. M., Müller, S., Frech, M., Wade, R. C., & Knapp, S. (2021). Structure-kinetic relationship reveals the mechanism of selectivity of FAK inhibitors over PYK2. Cell chemical biology, S2451-9456(21)00003-9. Advance online publication. https://doi.org/10.1016/j.chembiol.2021.01.003

Lemos, C., Schulze, V. K., Baumgart, S. J., Nevedomskaya, E., Heinrich, T., Lefranc, J., Bader, B., Christ, C. D., Briem, H., Kuhnke, L. P., Holton, S. J., Bömer, U., Lienau, P., von Nussbaum, F., Nising, C. F., Bauser, M., Hägebarth, A., Mumberg, D., & Haendler, B. (2021). The potent AMPK inhibitor BAY-3827 shows strong efficacy in androgen-dependent prostate cancer models. Cellular oncology (Dordrecht), 10.1007/s13402-020-00584-8. Advance online publication. https://doi.org/10.1007/s13402-020-00584-8

D'Amico, F., Mukhopadhyay, R., Ovaa, H., & Mulder, M. (2021). Targeting TRIM Proteins: A quest towards drugging an emerging protein class. Chembiochem : a European journal of chemical biology, 10.1002/cbic.202000787. Advance online publication. https://doi.org/10.1002/cbic.202000787

Desta, Z., El-Boraie, A., Gong, L., Somogyi, A. A., Lauschke, V. M., Dandara, C., Klein, K., Miller, N. A., Klein, T. E., Tyndale, R. F., Whirl-Carrillo, M., & Gaedigk, A. (2021). PharmVar GeneFocus: CYP2B6. Clinical pharmacology and therapeutics, 110(1), 82–97. https://doi.org/10.1002/cpt.2166

Wells, C. I., Al-Ali, H., Andrews, D. M., Asquith, C., Axtman, A. D., Dikic, I., Ebner, D., Ettmayer, P., Fischer, C., Frederiksen, M., Futrell, R. E., Gray, N. S., Hatch, S. B., Knapp, S., Lücking, U., Michaelides, M., Mills, C. E., Müller, S., Owen, D., Picado, A., … Drewry, D. H. (2021). The Kinase Chemogenomic Set (KCGS): An Open Science Resource for Kinase Vulnerability Identification. International journal of molecular sciences, 22(2), 566. https://doi.org/10.3390/ijms22020566

Stebbing, J., Sánchez Nievas, G., Falcone, M., Youhanna, S., Richardson, P., Ottaviani, S., Shen, J. X., Sommerauer, C., Tiseo, G., Ghiadoni, L., Virdis, A., Monzani, F., Rizos, L. R., Forfori, F., Avendaño Céspedes, A., De Marco, S., Carrozzi, L., Lena, F., Sánchez-Jurado, P. M., Lacerenza, L. G., … Lauschke, V. M. (2021). JAK inhibition reduces SARS-CoV-2 liver infectivity and modulates inflammatory responses to reduce morbidity and mortality. Science advances, 7(1), eabe4724. https://doi.org/10.1126/sciadv.abe4724

2020

Forster, M., Liang, X. J., Schröder, M., Gerstenecker, S., Chaikuad, A., Knapp, S., Laufer, S., & Gehringer, M. (2020). Discovery of a Novel Class of Covalent Dual Inhibitors Targeting the Protein Kinases BMX and BTK. International journal of molecular sciences, 21(23), 9269. https://doi.org/10.3390/ijms21239269

Ramachandran, S., & Ciulli, A. (2020). Building ubiquitination machineries: E3 ligase multi-subunit assembly and substrate targeting by PROTACs and molecular glues. Current opinion in structural biology, 67, 110–119. Advance online publication. https://doi.org/10.1016/j.sbi.2020.10.009

Preuss, F., Chatterjee, D., Mathea, S., Shrestha, S., St-Germain, J., Saha, M., Kannan, N., Raught, B., Rottapel, R., & Knapp, S. (2020). Nucleotide Binding, Evolutionary Insights, and Interaction Partners of the Pseudokinase Unc-51-like Kinase 4. Structure (London, England : 1993), 28(11), 1184–1196.e6. https://doi.org/10.1016/j.str.2020.07.016

Ishida, T., & Ciulli, A. (2020). E3 Ligase Ligands for PROTACs: How They Were Found and How to Discover New Ones. SLAS discovery : advancing life sciences R & D, 2472555220965528. Advance online publication. https://doi.org/10.1177/2472555220965528

Youhanna, S., & Lauschke, V. M. (2021). The Past, Present and Future of Intestinal In Vitro Cell Systems for Drug Absorption Studies. Journal of pharmaceutical sciences, 110(1), 50–65. https://doi.org/10.1016/j.xphs.2020.07.001

Meijer, I., Willems, S., Ni, X., Heering, J., Chaikuad, A., & Merk, D. (2020). Chemical Starting Matter for HNF4α Ligand Discovery and Chemogenomics. International journal of molecular sciences, 21(21), 7895. https://doi.org/10.3390/ijms21217895

Zhou, Y., Dagli Hernandez, C., & Lauschke, V. M. (2020). Population-scale predictions of DPD and TPMT phenotypes using a quantitative pharmacogene-specific ensemble classifier. British journal of cancer, 123(12), 1782–1789. https://doi.org/10.1038/s41416-020-01084-0

Schröder, M., Bullock, A. N., Fedorov, O., Bracher, F., Chaikuad, A., & Knapp, S. (2020). DFG-1 Residue Controls Inhibitor Binding Mode and Affinity, Providing a Basis for Rational Design of Kinase Inhibitor Selectivity. Journal of medicinal chemistry, 63(18), 10224–10234. https://doi.org/10.1021/acs.jmedchem.0c00898

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