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Small Molecule Inhibition of CPS1 Activity through an Allosteric Pocket.
Yao S, Nguyen TV, Rolfe A, Agrawal AA, Ke J, Peng S, Colombo F, Yu S, Bouchard P, Wu J, Huang KC, Bao X, Omoto K, Selvaraj A, Yu L, Ioannidis S, Vaillancourt FH, Zhu P, Larsen NA, Bolduc DM. Yao S, et al. Among authors: vaillancourt fh. Cell Chem Biol. 2020 Mar 19;27(3):259-268.e5. doi: 10.1016/j.chembiol.2020.01.009. Epub 2020 Feb 3. Cell Chem Biol. 2020. PMID: 32017919 Free article.
Discovery of 2,6-Dimethylpiperazines as Allosteric Inhibitors of CPS1.
Rolfe A, Yao S, Nguyen TV, Omoto K, Colombo F, Virrankoski M, Vaillancourt FH, Yu L, Cook A, Reynolds D, Ioannidis S, Zhu P, Larsen NA, Bolduc DM. Rolfe A, et al. Among authors: vaillancourt fh. ACS Med Chem Lett. 2020 May 26;11(6):1305-1309. doi: 10.1021/acsmedchemlett.0c00145. eCollection 2020 Jun 11. ACS Med Chem Lett. 2020. PMID: 32551016 Free PMC article.
The R882H DNMT3A hot spot mutation stabilizes the formation of large DNMT3A oligomers with low DNA methyltransferase activity.
Nguyen TV, Yao S, Wang Y, Rolfe A, Selvaraj A, Darman R, Ke J, Warmuth M, Smith PG, Larsen NA, Yu L, Zhu P, Fekkes P, Vaillancourt FH, Bolduc DM. Nguyen TV, et al. Among authors: vaillancourt fh. J Biol Chem. 2019 Nov 8;294(45):16966-16977. doi: 10.1074/jbc.RA119.010126. Epub 2019 Oct 3. J Biol Chem. 2019. PMID: 31582562 Free PMC article.
Discovery of Selective Estrogen Receptor Covalent Antagonists for the Treatment of ERαWT and ERαMUT Breast Cancer.
Puyang X, Furman C, Zheng GZ, Wu ZJ, Banka D, Aithal K, Agoulnik S, Bolduc DM, Buonamici S, Caleb B, Das S, Eckley S, Fekkes P, Hao MH, Hart A, Houtman R, Irwin S, Joshi JJ, Karr C, Kim A, Kumar N, Kumar P, Kuznetsov G, Lai WG, Larsen N, Mackenzie C, Martin LA, Melchers D, Moriarty A, Nguyen TV, Norris J, O'Shea M, Pancholi S, Prajapati S, Rajagopalan S, Reynolds DJ, Rimkunas V, Rioux N, Ribas R, Siu A, Sivakumar S, Subramanian V, Thomas M, Vaillancourt FH, Wang J, Wardell S, Wick MJ, Yao S, Yu L, Warmuth M, Smith PG, Zhu P, Korpal M. Puyang X, et al. Among authors: vaillancourt fh. Cancer Discov. 2018 Sep;8(9):1176-1193. doi: 10.1158/2159-8290.CD-17-1229. Epub 2018 Jul 10. Cancer Discov. 2018. PMID: 29991605
Covalent ERα Antagonist H3B-6545 Demonstrates Encouraging Preclinical Activity in Therapy-Resistant Breast Cancer.
Furman C, Puyang X, Zhang Z, Wu ZJ, Banka D, Aithal KB, Albacker LA, Hao MH, Irwin S, Kim A, Montesion M, Moriarty AD, Murugesan K, Nguyen TV, Rimkunas V, Sahmoud T, Wick MJ, Yao S, Zhang X, Zeng H, Vaillancourt FH, Bolduc DM, Larsen N, Zheng GZ, Prajapati S, Zhu P, Korpal M. Furman C, et al. Among authors: vaillancourt fh. Mol Cancer Ther. 2022 Jun 1;21(6):890-902. doi: 10.1158/1535-7163.MCT-21-0378. Mol Cancer Ther. 2022. PMID: 35642432 Free PMC article.
Reprogramming RNA processing: an emerging therapeutic landscape.
Neil CR, Seiler MW, Reynolds DJ, Smith JJ, Vaillancourt FH, Smith PG, Agrawal AA. Neil CR, et al. Among authors: vaillancourt fh. Trends Pharmacol Sci. 2022 May;43(5):437-454. doi: 10.1016/j.tips.2022.02.011. Epub 2022 Mar 21. Trends Pharmacol Sci. 2022. PMID: 35331569 Free article. Review.
Evaluation of phosphatidylinositol-4-kinase IIIα as a hepatitis C virus drug target.
Vaillancourt FH, Brault M, Pilote L, Uyttersprot N, Gaillard ET, Stoltz JH, Knight BL, Pantages L, McFarland M, Breitfelder S, Chiu TT, Mahrouche L, Faucher AM, Cartier M, Cordingley MG, Bethell RC, Jiang H, White PW, Kukolj G. Vaillancourt FH, et al. J Virol. 2012 Nov;86(21):11595-607. doi: 10.1128/JVI.01320-12. Epub 2012 Aug 15. J Virol. 2012. PMID: 22896614 Free PMC article.
33 results