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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: karr c. 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.
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. Among authors: karr c. Cancer Res. 2017 Dec 15;77(24):6999-7013. doi: 10.1158/0008-5472.CAN-17-1865. Cancer Res. 2017. PMID: 29247039
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: karr c. 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
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: karr c. Genes Dev. 2018 Feb 1;32(3-4):309-320. doi: 10.1101/gad.311043.117. Genes Dev. 2018. PMID: 29491137 Free PMC article.
Biochemical and structural basis for the pharmacological inhibition of nuclear hormone receptor PPARγ by inverse agonists.
Irwin S, Karr C, Furman C, Tsai J, Gee P, Banka D, Wibowo AS, Dementiev AA, O'Shea M, Yang J, Lowe J, Mitchell L, Ruppel S, Fekkes P, Zhu P, Korpal M, Larsen NA. Irwin S, et al. Among authors: karr c. J Biol Chem. 2022 Nov;298(11):102539. doi: 10.1016/j.jbc.2022.102539. Epub 2022 Sep 28. J Biol Chem. 2022. PMID: 36179791 Free PMC article.
Total synthesis of 6-deoxypladienolide D and Assessment of Splicing Inhibitory Activity in a Mutant SF3B1 cancer cell line.
Arai K, Buonamici S, Chan B, Corson L, Endo A, Gerard B, Hao MH, Karr C, Kira K, Lee L, Liu X, Lowe JT, Luo T, Marcaurelle LA, Mizui Y, Nevalainen M, O'Shea MW, Park ES, Perino SA, Prajapati S, Shan M, Smith PG, Tivitmahaisoon P, Wang JY, Warmuth M, Wu KM, Yu L, Zhang H, Zheng GZ, Keaney GF. Arai K, et al. Among authors: karr c. Org Lett. 2014 Nov 7;16(21):5560-3. doi: 10.1021/ol502556c. Epub 2014 Oct 26. Org Lett. 2014. PMID: 25376106
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. Among authors: karr c. Nat Commun. 2017 May 25;8:15522. doi: 10.1038/ncomms15522. Nat Commun. 2017. PMID: 28541300 Free PMC article.
H3B-8800, an orally available small-molecule splicing modulator, induces lethality in spliceosome-mutant cancers.
Seiler M, Yoshimi A, Darman R, Chan B, Keaney G, Thomas M, Agrawal AA, Caleb B, Csibi A, Sean E, Fekkes P, Karr C, Klimek V, Lai G, Lee L, Kumar P, Lee SC, Liu X, Mackenzie C, Meeske C, Mizui Y, Padron E, Park E, Pazolli E, Peng S, Prajapati S, Taylor J, Teng T, Wang J, Warmuth M, Yao H, Yu L, Zhu P, Abdel-Wahab O, Smith PG, Buonamici S. Seiler M, et al. Among authors: karr c. Nat Med. 2018 May;24(4):497-504. doi: 10.1038/nm.4493. Epub 2018 Feb 19. Nat Med. 2018. PMID: 29457796 Free PMC article.
Sensitivity to splicing modulation of BCL2 family genes defines cancer therapeutic strategies for splicing modulators.
Aird D, Teng T, Huang CL, Pazolli E, Banka D, Cheung-Ong K, Eifert C, Furman C, Wu ZJ, Seiler M, Buonamici S, Fekkes P, Karr C, Palacino J, Park E, Smith PG, Yu L, Mizui Y, Warmuth M, Chicas A, Corson L, Zhu P. Aird D, et al. Among authors: karr c. Nat Commun. 2019 Jan 11;10(1):137. doi: 10.1038/s41467-018-08150-5. Nat Commun. 2019. PMID: 30635584 Free PMC article.
203 results