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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: zhu 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.
NAMPT is the cellular target of STF-31-like small-molecule probes.
Adams DJ, Ito D, Rees MG, Seashore-Ludlow B, Puyang X, Ramos AH, Cheah JH, Clemons PA, Warmuth M, Zhu P, Shamji AF, Schreiber SL. Adams DJ, et al. Among authors: zhu p. ACS Chem Biol. 2014 Oct 17;9(10):2247-54. doi: 10.1021/cb500347p. Epub 2014 Aug 7. ACS Chem Biol. 2014. PMID: 25058389 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: zhu 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.
Allosteric inhibition of SHP2 phosphatase inhibits cancers driven by receptor tyrosine kinases.
Chen YN, LaMarche MJ, Chan HM, Fekkes P, Garcia-Fortanet J, Acker MG, Antonakos B, Chen CH, Chen Z, Cooke VG, Dobson JR, Deng Z, Fei F, Firestone B, Fodor M, Fridrich C, Gao H, Grunenfelder D, Hao HX, Jacob J, Ho S, Hsiao K, Kang ZB, Karki R, Kato M, Larrow J, La Bonte LR, Lenoir F, Liu G, Liu S, Majumdar D, Meyer MJ, Palermo M, Perez L, Pu M, Price E, Quinn C, Shakya S, Shultz MD, Slisz J, Venkatesan K, Wang P, Warmuth M, Williams S, Yang G, Yuan J, Zhang JH, Zhu P, Ramsey T, Keen NJ, Sellers WR, Stams T, Fortin PD. Chen YN, et al. Among authors: zhu p. Nature. 2016 Jul 7;535(7610):148-52. doi: 10.1038/nature18621. Epub 2016 Jun 29. Nature. 2016. PMID: 27362227
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: zhu p. Nat Commun. 2017 May 25;8:15522. doi: 10.1038/ncomms15522. Nat Commun. 2017. PMID: 28541300 Free PMC 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: zhu p. Nat Commun. 2017 Jul 24;8(1):103. doi: 10.1038/s41467-017-00147-w. Nat Commun. 2017. PMID: 28740126 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: zhu p. Cancer Res. 2017 Dec 15;77(24):6999-7013. doi: 10.1158/0008-5472.CAN-17-1865. Cancer Res. 2017. PMID: 29247039
Novel SF3B1 in-frame deletions result in aberrant RNA splicing in CLL patients.
Agrawal AA, Seiler M, Brinton LT, Mantel R, Lapalombella R, Woyach JA, Johnson AJ, Zhu P, Warmuth M, Yu L, Byrd JC, Smith PG, Blachly JS, Buonamici S. Agrawal AA, et al. Among authors: zhu p. Blood Adv. 2017 Jun 14;1(15):995-1000. doi: 10.1182/bloodadvances.2017007062. eCollection 2017 Jun 27. Blood Adv. 2017. PMID: 29296742 Free PMC article.
5,414 results