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Page 1
Potent and Selective SETDB1 Covalent Negative Allosteric Modulator Reduces Methyltransferase Activity in Cells.
Uguen M, Shell DJ, Silva M, Deng Y, Li F, Szewczyk MM, Yang K, Zhao Y, Stashko MA, Norris-Drouin JL, Waybright JM, Beldar S, Rectenwald JM, Mordant AL, Webb TS, Herring LE, Arrowsmith CH, Ackloo S, Gygi SP, McGinty RK, Barsyte-Lovejoy D, Liu P, Halabelian L, James LI, Pearce KH, Frye SV. Uguen M, et al. Among authors: szewczyk mm. bioRxiv [Preprint]. 2024 Sep 28:2024.09.27.615363. doi: 10.1101/2024.09.27.615363. bioRxiv. 2024. PMID: 39386588 Free PMC article. Preprint.
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: szewczyk mm. 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
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: szewczyk mm. PNAS Nexus. 2024 Apr 10;3(4):pgae153. doi: 10.1093/pnasnexus/pgae153. eCollection 2024 Apr. PNAS Nexus. 2024. PMID: 38665159 Free PMC article.
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: szewczyk mm. 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: szewczyk mm. 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 Free PMC article.
Epigenetic vulnerabilities of leukemia harboring inactivating EZH2 mutations.
Alqazzaz MA, Luciani GM, Vu V, Machado RAC, Szewczyk MM, Adamson EC, Cheon S, Li F, Arrowsmith CH, Minden MD, Barsyte-Lovejoy D. Alqazzaz MA, et al. Among authors: szewczyk mm. Exp Hematol. 2024 Feb;130:104135. doi: 10.1016/j.exphem.2023.11.009. Epub 2023 Dec 10. Exp Hematol. 2024. PMID: 38072134
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: szewczyk mm. 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.
Discovery of a Potent and Selective Targeted NSD2 Degrader for the Reduction of H3K36me2.
Hanley RP, Nie DY, Tabor JR, Li F, Sobh A, Xu C, Barker NK, Dilworth D, Hajian T, Gibson E, Szewczyk MM, Brown PJ, Barsyte-Lovejoy D, Herring LE, Wang GG, Licht JD, Vedadi M, Arrowsmith CH, James LI. Hanley RP, et al. Among authors: szewczyk mm. J Am Chem Soc. 2023 Apr 12;145(14):8176-8188. doi: 10.1021/jacs.3c01421. Epub 2023 Mar 28. J Am Chem Soc. 2023. PMID: 36976643 Free PMC article.
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: szewczyk mm. 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.
54 results