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Covalent Fragment Screening and Optimization Identifies the Chloroacetohydrazide Scaffold as Inhibitors for Ubiquitin C-terminal Hydrolase L1.
Imhoff RD, Patel R, Safdar MH, Jones HBL, Pinto-Fernandez A, Vendrell I, Chen H, Muli CS, Krabill AD, Kessler BM, Wendt MK, Das C, Flaherty DP. Imhoff RD, et al. Among authors: kessler bm. J Med Chem. 2024 Mar 28;67(6):4496-4524. doi: 10.1021/acs.jmedchem.3c01661. Epub 2024 Mar 15. J Med Chem. 2024. PMID: 38488146
Molecular basis of USP7 inhibition by selective small-molecule inhibitors.
Turnbull AP, Ioannidis S, Krajewski WW, Pinto-Fernandez A, Heride C, Martin ACL, Tonkin LM, Townsend EC, Buker SM, Lancia DR, Caravella JA, Toms AV, Charlton TM, Lahdenranta J, Wilker E, Follows BC, Evans NJ, Stead L, Alli C, Zarayskiy VV, Talbot AC, Buckmelter AJ, Wang M, McKinnon CL, Saab F, McGouran JF, Century H, Gersch M, Pittman MS, Marshall CG, Raynham TM, Simcox M, Stewart LMD, McLoughlin SB, Escobedo JA, Bair KW, Dinsmore CJ, Hammonds TR, Kim S, Urbé S, Clague MJ, Kessler BM, Komander D. Turnbull AP, et al. Among authors: kessler bm. Nature. 2017 Oct 26;550(7677):481-486. doi: 10.1038/nature24451. Epub 2017 Oct 18. Nature. 2017. PMID: 29045389 Free PMC article.
Human Platelet Protein Ubiquitylation and Changes following GPVI Activation.
Unsworth AJ, Bombik I, Pinto-Fernandez A, McGouran JF, Konietzny R, Zahedi RP, Watson SP, Kessler BM, Pears CJ. Unsworth AJ, et al. Among authors: kessler bm. Thromb Haemost. 2019 Jan;119(1):104-116. doi: 10.1055/s-0038-1676344. Epub 2018 Dec 31. Thromb Haemost. 2019. PMID: 30597505 Free PMC article.
Deacetylation Inhibition Reverses PABPN1-Dependent Muscle Wasting.
Olie CS, Riaz M, Konietzny R, Charles PD, Pinto-Fernandez A, Kiełbasa SM, Aartsma-Rus A, Goeman JJ, Kessler BM, Raz V. Olie CS, et al. Among authors: kessler bm. iScience. 2019 Feb 22;12:318-332. doi: 10.1016/j.isci.2019.01.024. Epub 2019 Jan 22. iScience. 2019. PMID: 30739015 Free PMC article.
Regulation of the endosomal SNX27-retromer by OTULIN.
Stangl A, Elliott PR, Pinto-Fernandez A, Bonham S, Harrison L, Schaub A, Kutzner K, Keusekotten K, Pfluger PT, El Oualid F, Kessler BM, Komander D, Krappmann D. Stangl A, et al. Among authors: kessler bm. Nat Commun. 2019 Sep 20;10(1):4320. doi: 10.1038/s41467-019-12309-z. Nat Commun. 2019. PMID: 31541095 Free PMC article.
Re-Evaluating the Mechanism of Action of α,β-Unsaturated Carbonyl DUB Inhibitors b-AP15 and VLX1570: A Paradigmatic Example of Unspecific Protein Cross-linking with Michael Acceptor Motif-Containing Drugs.
Ward JA, Pinto-Fernandez A, Cornelissen L, Bonham S, Díaz-Sáez L, Riant O, Huber KVM, Kessler BM, Feron O, Tate EW. Ward JA, et al. Among authors: kessler bm. J Med Chem. 2020 Apr 9;63(7):3756-3762. doi: 10.1021/acs.jmedchem.0c00144. Epub 2020 Mar 19. J Med Chem. 2020. PMID: 32109059 Free PMC article.
294 results