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Page 1
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: fekkes p. 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: fekkes p. 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.
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: fekkes p. Genes Dev. 2018 Feb 1;32(3-4):309-320. doi: 10.1101/gad.311043.117. Genes Dev. 2018. PMID: 29491137 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: fekkes p. Nat Commun. 2019 Jan 11;10(1):137. doi: 10.1038/s41467-018-08150-5. Nat Commun. 2019. PMID: 30635584 Free PMC article.
Cancer-Associated SF3B1 Hotspot Mutations Induce Cryptic 3' Splice Site Selection through Use of a Different Branch Point.
Darman RB, Seiler M, Agrawal AA, Lim KH, Peng S, Aird D, Bailey SL, Bhavsar EB, Chan B, Colla S, Corson L, Feala J, Fekkes P, Ichikawa K, Keaney GF, Lee L, Kumar P, Kunii K, MacKenzie C, Matijevic M, Mizui Y, Myint K, Park ES, Puyang X, Selvaraj A, Thomas MP, Tsai J, Wang JY, Warmuth M, Yang H, Zhu P, Garcia-Manero G, Furman RR, Yu L, Smith PG, Buonamici S. Darman RB, et al. Among authors: fekkes p. Cell Rep. 2015 Nov 3;13(5):1033-45. doi: 10.1016/j.celrep.2015.09.053. Epub 2015 Oct 22. Cell Rep. 2015. PMID: 26565915 Free article.
Evasion of immunosurveillance by genomic alterations of PPARγ/RXRα in bladder cancer.
Korpal M, Puyang X, Jeremy Wu Z, Seiler R, Furman C, Oo HZ, Seiler M, Irwin S, Subramanian V, Julie Joshi J, Wang CK, Rimkunas V, Tortora D, Yang H, Kumar N, Kuznetsov G, Matijevic M, Chow J, Kumar P, Zou J, Feala J, Corson L, Henry R, Selvaraj A, Davis A, Bloudoff K, Douglas J, Kiss B, Roberts M, Fazli L, Black PC, Fekkes P, Smith PG, Warmuth M, Yu L, Hao MH, Larsen N, Daugaard M, Zhu P. Korpal M, et al. Among authors: fekkes p. Nat Commun. 2017 Jul 24;8(1):103. doi: 10.1038/s41467-017-00147-w. Nat Commun. 2017. PMID: 28740126 Free PMC article.
Structural Basis of Splicing Modulation by Antitumor Macrolide Compounds.
Cretu C, Agrawal AA, Cook A, Will CL, Fekkes P, Smith PG, Lührmann R, Larsen N, Buonamici S, Pena V. Cretu C, et al. Among authors: fekkes p. Mol Cell. 2018 Apr 19;70(2):265-273.e8. doi: 10.1016/j.molcel.2018.03.011. Epub 2018 Apr 12. Mol Cell. 2018. PMID: 29656923 Free article.
Author Correction: Evasion of immunosurveillance by genomic alterations of PPARγ/RXRα in bladder cancer.
Korpal M, Puyang X, Wu ZJ, Seiler R, Furman C, Oo HZ, Seiler M, Irwin S, Subramanian V, Joshi JJ, Wang CK, Rimkunas V, Tortora D, Yang H, Kumar N, Kuznetsov G, Matijevic M, Chow J, Kumar P, Zou J, Feala J, Corson L, Henry R, Selvaraj A, Davis A, Bloudoff K, Douglas J, Kiss B, Roberts M, Fazli L, Black PC, Fekkes P, Smith PG, Warmuth M, Yu L, Hao MH, Larsen N, Daugaard M, Zhu P. Korpal M, et al. Among authors: fekkes p. Nat Commun. 2019 Jun 4;10(1):2527. doi: 10.1038/s41467-019-10666-3. Nat Commun. 2019. PMID: 31164653 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: fekkes p. 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
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: fekkes p. Cancer Res. 2017 Dec 15;77(24):6999-7013. doi: 10.1158/0008-5472.CAN-17-1865. Cancer Res. 2017. PMID: 29247039
29 results