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Probing the CRL4DCAF12 interactions with MAGEA3 and CCT5 di-Glu C-terminal degrons.
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. Righetto GL, et al. Among authors: santhakumar v. PNAS Nexus. 2024 Apr 10;3(4):pgae153. doi: 10.1093/pnasnexus/pgae153. eCollection 2024 Apr. PNAS Nexus. 2024. PMID: 38665159 Free PMC article.
Discovery of a First-in-Class Small-Molecule Ligand for WDR91 Using DNA-Encoded Chemical Library Selection Followed by Machine Learning.
Ahmad S, Xu J, Feng JA, Hutchinson A, Zeng H, Ghiabi P, Dong A, Centrella PA, Clark MA, Guié MA, Guilinger JP, Keefe AD, Zhang Y, Cerruti T, Cuozzo JW, von Rechenberg M, Bolotokova A, Li Y, Loppnau P, Seitova A, Li YY, Santhakumar V, Brown PJ, Ackloo S, Halabelian L. Ahmad S, et al. Among authors: santhakumar v. J Med Chem. 2023 Dec 14;66(23):16051-16061. doi: 10.1021/acs.jmedchem.3c01471. Epub 2023 Nov 23. J Med Chem. 2023. PMID: 37996079
Development of LM98, a Small-Molecule TEAD Inhibitor Derived from Flufenamic Acid.
Mélin L, Abdullayev S, Fnaiche A, Vu V, González Suárez N, Zeng H, Szewczyk MM, Li F, Senisterra G, Allali-Hassani A, Chau I, Dong A, Woo S, Annabi B, Halabelian L, LaPlante SR, Vedadi M, Barsyte-Lovejoy D, Santhakumar V, Gagnon A. Mélin L, et al. Among authors: santhakumar v. ChemMedChem. 2021 Oct 6;16(19):2982-3002. doi: 10.1002/cmdc.202100432. Epub 2021 Jul 28. ChemMedChem. 2021. PMID: 34164919
Discovery of Nanomolar DCAF1 Small Molecule Ligands.
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. Li ASM, et al. Among authors: santhakumar v. J Med Chem. 2023 Apr 13;66(7):5041-5060. doi: 10.1021/acs.jmedchem.2c02132. Epub 2023 Mar 22. J Med Chem. 2023. PMID: 36948210 Free PMC article.
Discovery and Characterization of a Chemical Probe Targeting the Zinc-Finger Ubiquitin-Binding Domain of HDAC6.
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. Harding RJ, et al. Among authors: santhakumar v. J Med Chem. 2023 Aug 10;66(15):10273-10288. doi: 10.1021/acs.jmedchem.3c00314. Epub 2023 Jul 27. J Med Chem. 2023. PMID: 37499118 Free PMC article.
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: santhakumar v. 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
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: santhakumar v. RSC Med Chem. 2024 Mar 5;15(3):1066-1071. doi: 10.1039/d3md00633f. eCollection 2024 Mar 20. RSC Med Chem. 2024. PMID: 38516600
Discovery and Characterization of BAY-805, a Potent and Selective Inhibitor of Ubiquitin-Specific Protease USP21.
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. Göricke F, et al. Among authors: santhakumar v. J Med Chem. 2023 Mar 9;66(5):3431-3447. doi: 10.1021/acs.jmedchem.2c01933. Epub 2023 Feb 20. J Med Chem. 2023. PMID: 36802665 Free PMC article.
Discovery of a Potent and Selective Coactivator Associated Arginine Methyltransferase 1 (CARM1) Inhibitor by Virtual Screening.
Ferreira de Freitas R, Eram MS, Smil D, Szewczyk MM, Kennedy S, Brown PJ, Santhakumar V, Barsyte-Lovejoy D, Arrowsmith CH, Vedadi M, Schapira M. Ferreira de Freitas R, et al. Among authors: santhakumar v. J Med Chem. 2016 Jul 28;59(14):6838-47. doi: 10.1021/acs.jmedchem.6b00668. Epub 2016 Jul 8. J Med Chem. 2016. PMID: 27390919
114 results