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Covalent Inhibitors of KEAP1 with Exquisite Selectivity.
Fejes I, Markacz P, Tatai J, Rudas M, Dunkel P, Gyuris M, Nyerges M, Provost N, Duvivier V, Delerive P, Martiny V, Bristiel A, Vidal B, Richardson W, Rothweiler EM, Tranberg-Jensen J, Manning CE, Sweeney MN, Chalk R, Huber KVM, Bullock AN, Herner A, Seedorf K, Vinson C, Weber C, Kotschy A. Fejes I, et al. Among authors: huber kvm. J Med Chem. 2024 Nov 21. doi: 10.1021/acs.jmedchem.4c02019. Online ahead of print. J Med Chem. 2024. PMID: 39572012
Paralogue-Selective Degradation of the Lysine Acetyltransferase EP300.
Chen X, Crawford MC, Xiong Y, Shaik AB, Suazo KF, Bauer LG, Penikalapati MS, Williams JH, Huber KVM, Andressen T, Swenson RE, Meier JL. Chen X, et al. Among authors: huber kvm. JACS Au. 2024 Jul 29;4(8):3094-3103. doi: 10.1021/jacsau.4c00442. eCollection 2024 Aug 26. JACS Au. 2024. PMID: 39211607 Free PMC article.
Advancing drug discovery through assay development: a survey of tool compounds within the human solute carrier superfamily.
Digles D, Ingles-Prieto A, Dvorak V, Mocking TAM, Goldmann U, Garofoli A, Homan EJ, Di Silvio A, Azzollini L, Sassone F, Fogazza M, Bärenz F, Pommereau A, Zuschlag Y, Ooms JF, Tranberg-Jensen J, Hansen JS, Stanka J, Sijben HJ, Batoulis H, Bender E, Martini R, IJzerman AP, Sauer DB, Heitman LH, Manolova V, Reinhardt J, Ehrmann A, Leippe P, Ecker GF, Huber KVM, Licher T, Scarabottolo L, Wiedmer T, Superti-Furga G. Digles D, et al. Among authors: huber kvm. Front Pharmacol. 2024 Jul 9;15:1401599. doi: 10.3389/fphar.2024.1401599. eCollection 2024. Front Pharmacol. 2024. PMID: 39050757 Free PMC article.
Unexpected Noncovalent Off-Target Activity of Clinical BTK Inhibitors Leads to Discovery of a Dual NUDT5/14 Antagonist.
Balıkçı E, Marques AMC, Bauer LG, Seupel R, Bennett J, Raux B, Buchan K, Simelis K, Singh U, Rogers C, Ward J, Cheng C, Szommer T, Schützenhofer K, Elkins JM, Sloman DL, Ahel I, Fedorov O, Brennan PE, Huber KVM. Balıkçı E, et al. Among authors: huber kvm. J Med Chem. 2024 May 9;67(9):7245-7259. doi: 10.1021/acs.jmedchem.4c00072. Epub 2024 Apr 18. J Med Chem. 2024. PMID: 38635563 Free PMC article.
Discovery of PFI-6, a small-molecule chemical probe for the YEATS domain of MLLT1 and MLLT3.
Raux B, Buchan KA, Bennett J, Christott T, Dowling MS, Farnie G, Fedorov O, Gamble V, Gileadi C, Giroud C, Huber KVM, Korczynska M, Limberakis C, Narayanan A, Owen DR, Sáez LD, Stock IA, Londregan AT. Raux B, et al. Among authors: huber kvm. Bioorg Med Chem Lett. 2024 Jan 15;98:129546. doi: 10.1016/j.bmcl.2023.129546. Epub 2023 Nov 7. Bioorg Med Chem Lett. 2024. PMID: 37944866
Cyclic peptides target the aromatic cage of a PHD-finger reader domain to modulate epigenetic protein function.
Coleman OD, Macdonald J, Thomson B, Ward JA, Stubbs CJ, McAllister TE, Clark S, Amin S, Cao Y, Abboud MI, Zhang Y, Sanganee H, Huber KVM, Claridge TDW, Kawamura A. Coleman OD, et al. Among authors: huber kvm. Chem Sci. 2023 Apr 17;14(26):7136-7146. doi: 10.1039/d2sc05944d. eCollection 2023 Jul 5. Chem Sci. 2023. PMID: 37416723 Free PMC article.
Discovery of a Chemical Probe to Study Implications of BPTF Bromodomain Inhibition in Cellular and in vivo Experiments.
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. Martinelli P, et al. Among authors: huber kvm. ChemMedChem. 2023 Mar 14;18(6):e202200686. doi: 10.1002/cmdc.202200686. Epub 2023 Feb 6. ChemMedChem. 2023. PMID: 36649575
52 results