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Page 1
Crystal structures of DCAF1-PROTAC-WDR5 ternary complexes provide insight into DCAF1 substrate specificity.
Mabanglo MF, Wilson B, Noureldin M, Kimani SW, Mamai A, Krausser C, González-Álvarez H, Srivastava S, Mohammed M, Hoffer L, Chan M, Avrumutsoae J, Li ASM, Hajian T, Tucker S, Green S, Szewczyk M, Barsyte-Lovejoy D, Santhakumar V, Ackloo S, Loppnau P, Li Y, Seitova A, Kiyota T, Wang JG, Privé GG, Kuntz DA, Patel B, Rathod V, Vala A, Rout B, Aman A, Poda G, Uehling D, Ramnauth J, Halabelian L, Marcellus R, Al-Awar R, Vedadi M. Mabanglo MF, et al. Among authors: vedadi m. Nat Commun. 2024 Nov 23;15(1):10165. doi: 10.1038/s41467-024-54500-x. Nat Commun. 2024. PMID: 39580491 Free article.
A chemical probe to modulate human GID4 Pro/N-degron interactions.
Owens DDG, Maitland MER, Khalili Yazdi A, Song X, Reber V, Schwalm MP, Machado RAC, Bauer N, Wang X, Szewczyk MM, Dong C, Dong A, Loppnau P, Calabrese MF, Dowling MS, Lee J, Montgomery JI, O'Connell TN, Subramanyam C, Wang F, Adamson EC, Schapira M, Gstaiger M, Knapp S, Vedadi M, Min J, Lajoie GA, Barsyte-Lovejoy D, Owen DR, Schild-Poulter C, Arrowsmith CH. Owens DDG, et al. Among authors: vedadi m. Nat Chem Biol. 2024 Sep;20(9):1164-1175. doi: 10.1038/s41589-024-01618-0. Epub 2024 May 21. Nat Chem Biol. 2024. PMID: 38773330
Discovery of a Potent, Selective, and Cell-Active SPIN1 Inhibitor.
Xiong Y, Greschik H, Johansson C, Seifert L, Gamble V, Park KS, Fagan V, Li F, Chau I, Vedadi M, Arrowsmith CH, Brennan P, Fedorov O, Jung M, Farnie G, Liu J, Oppermann U, Schüle R, Jin J. Xiong Y, et al. Among authors: vedadi m. J Med Chem. 2024 Apr 11;67(7):5837-5853. doi: 10.1021/acs.jmedchem.4c00121. Epub 2024 Mar 27. J Med Chem. 2024. PMID: 38533580
Chemical tools for the Gid4 subunit of the human E3 ligase C-terminal to LisH (CTLH) degradation complex.
Yazdi AK, Perveen S, Dong C, Song X, Dong A, Szewczyk MM, Calabrese MF, Casimiro-Garcia A, Chakrapani S, Dowling MS, Ficici E, Lee J, Montgomery JI, O'Connell TN, Skrzypek GJ, Tran TP, Troutman MD, Wang F, Young JA, Min J, Barsyte-Lovejoy D, Brown PJ, Santhakumar V, Arrowsmith CH, Vedadi M, Owen DR. Yazdi AK, et al. Among authors: vedadi m. RSC Med Chem. 2024 Mar 5;15(3):1066-1071. doi: 10.1039/d3md00633f. eCollection 2024 Mar 20. RSC Med Chem. 2024. PMID: 38516600
Development of HC-258, a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration.
Fnaiche A, Chan HC, Paquin A, González Suárez N, Vu V, Li F, Allali-Hassani A, Cao MA, Szewczyk MM, Bolotokova A, Allemand F, Gelin M, Barsyte-Lovejoy D, Santhakumar V, Vedadi M, Guichou JF, Annabi B, Gagnon A. Fnaiche A, et al. Among authors: vedadi m. ACS Med Chem Lett. 2023 Nov 30;14(12):1746-1753. doi: 10.1021/acsmedchemlett.3c00386. eCollection 2023 Dec 14. ACS Med Chem Lett. 2023. PMID: 38116405
Drug Discovery in Low Data Regimes: Leveraging a Computational Pipeline for the Discovery of Novel SARS-CoV-2 Nsp14-MTase Inhibitors.
Nigam A, Hurley MFD, Li F, Konkoľová E, Klíma M, Trylčová J, Pollice R, Çinaroğlu SS, Levin-Konigsberg R, Handjaya J, Schapira M, Chau I, Perveen S, Ng HL, Ümit Kaniskan H, Han Y, Singh S, Gorgulla C, Kundaje A, Jin J, Voelz VA, Weber J, Nencka R, Boura E, Vedadi M, Aspuru-Guzik A. Nigam A, et al. Among authors: vedadi m. bioRxiv [Preprint]. 2024 Jan 13:2023.10.03.560722. doi: 10.1101/2023.10.03.560722. bioRxiv. 2024. PMID: 37873443 Free PMC article. Preprint.
Development of LM-41 and AF-2112, two flufenamic acid-derived TEAD inhibitors obtained through the replacement of the trifluoromethyl group by aryl rings.
Fnaiche A, Mélin L, Suárez NG, Paquin A, Vu V, Li F, Allali-Hassani A, Bolotokova A, Allemand F, Gelin M, Cotelle P, Woo S, LaPlante SR, Barsyte-Lovejoy D, Santhakumar V, Vedadi M, Guichou JF, Annabi B, Gagnon A. Fnaiche A, et al. Among authors: vedadi m. Bioorg Med Chem Lett. 2023 Oct 15;95:129488. doi: 10.1016/j.bmcl.2023.129488. Epub 2023 Sep 27. Bioorg Med Chem Lett. 2023. PMID: 37770003
193 results