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Page 1
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: larsen na. 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: larsen na. 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: larsen na. 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 Aminopyrazole Derivatives as Potent Inhibitors of Wild-Type and Gatekeeper Mutant FGFR2 and 3.
Brawn RA, Cook A, Omoto K, Ke J, Karr C, Colombo F, Virrankoski M, Prajapati S, Reynolds D, Bolduc DM, Nguyen TV, Gee P, Borrelli D, Caleb B, Yao S, Irwin S, Larsen NA, Selvaraj A, Zhao X, Ioannidis S. Brawn RA, et al. Among authors: larsen na. ACS Med Chem Lett. 2020 Dec 2;12(1):93-98. doi: 10.1021/acsmedchemlett.0c00517. eCollection 2021 Jan 14. ACS Med Chem Lett. 2020. PMID: 33488969 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. 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. 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.
The cryo-EM structure of the SF3b spliceosome complex bound to a splicing modulator reveals a pre-mRNA substrate competitive mechanism of action.
Finci LI, Zhang X, Huang X, Zhou Q, Tsai J, Teng T, Agrawal A, Chan B, Irwin S, Karr C, Cook A, Zhu P, Reynolds D, Smith PG, Fekkes P, Buonamici S, Larsen NA. Finci LI, et al. Among authors: larsen na. Genes Dev. 2018 Feb 1;32(3-4):309-320. doi: 10.1101/gad.311043.117. Genes Dev. 2018. PMID: 29491137 Free PMC article.
Splicing modulators act at the branch point adenosine binding pocket defined by the PHF5A-SF3b complex.
Teng T, Tsai JH, Puyang X, Seiler M, Peng S, Prajapati S, Aird D, Buonamici S, Caleb B, Chan B, Corson L, Feala J, Fekkes P, Gerard B, Karr C, Korpal M, Liu X, T Lowe J, Mizui Y, Palacino J, Park E, Smith PG, Subramanian V, Wu ZJ, Zou J, Yu L, Chicas A, Warmuth M, Larsen N, Zhu P. Teng T, et al. Nat Commun. 2017 May 25;8:15522. doi: 10.1038/ncomms15522. Nat Commun. 2017. PMID: 28541300 Free PMC article.
H3B-6527 Is a Potent and Selective Inhibitor of FGFR4 in FGF19-Driven Hepatocellular Carcinoma.
Joshi JJ, Coffey H, Corcoran E, Tsai J, Huang CL, Ichikawa K, Prajapati S, Hao MH, Bailey S, Wu J, Rimkunas V, Karr C, Subramanian V, Kumar P, MacKenzie C, Hurley R, Satoh T, Yu K, Park E, Rioux N, Kim A, Lai WG, Yu L, Zhu P, Buonamici S, Larsen N, Fekkes P, Wang J, Warmuth M, Reynolds DJ, Smith PG, Selvaraj A. Joshi JJ, et al. Cancer Res. 2017 Dec 15;77(24):6999-7013. doi: 10.1158/0008-5472.CAN-17-1865. Cancer Res. 2017. PMID: 29247039
82 results