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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: li f. 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
Small-molecule inhibition of MLL activity by disruption of its interaction with WDR5.
Senisterra G, Wu H, Allali-Hassani A, Wasney GA, Barsyte-Lovejoy D, Dombrovski L, Dong A, Nguyen KT, Smil D, Bolshan Y, Hajian T, He H, Seitova A, Chau I, Li F, Poda G, Couture JF, Brown PJ, Al-Awar R, Schapira M, Arrowsmith CH, Vedadi M. Senisterra G, et al. Among authors: li f. Biochem J. 2013 Jan 1;449(1):151-9. doi: 10.1042/BJ20121280. Biochem J. 2013. PMID: 22989411 Free PMC article.
SS148 and WZ16 inhibit the activities of nsp10-nsp16 complexes from all seven human pathogenic coronaviruses.
Li F, Ghiabi P, Hajian T, Klima M, Li ASM, Khalili Yazdi A, Chau I, Loppnau P, Kutera M, Seitova A, Bolotokova A, Hutchinson A, Perveen S, Boura E, Vedadi M. Li F, et al. Among authors: li asm. Biochim Biophys Acta Gen Subj. 2023 Apr;1867(4):130319. doi: 10.1016/j.bbagen.2023.130319. Epub 2023 Feb 9. Biochim Biophys Acta Gen Subj. 2023. PMID: 36764586 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: li f. 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.
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: li f. Exp Hematol. 2024 Feb;130:104135. doi: 10.1016/j.exphem.2023.11.009. Epub 2023 Dec 10. Exp Hematol. 2024. PMID: 38072134
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: li f. 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
Discovery of hit compounds for methyl-lysine reader proteins from a target class DNA-encoded library.
Shell DJ, Rectenwald JM, Buttery PH, Johnson RL, Foley CA, Guduru SKR, Uguen M, Rubiano JS, Zhang X, Li F, Norris-Drouin JL, Axtman M, Brian Hardy P, Vedadi M, Frye SV, James LI, Pearce KH. Shell DJ, et al. Among authors: li f. SLAS Discov. 2022 Dec;27(8):428-439. doi: 10.1016/j.slasd.2022.10.003. Epub 2022 Oct 19. SLAS Discov. 2022. PMID: 36272689 Free article.
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