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Discovery of Brigatinib (AP26113), a Phosphine Oxide-Containing, Potent, Orally Active Inhibitor of Anaplastic Lymphoma Kinase.
Huang WS, Liu S, Zou D, Thomas M, Wang Y, Zhou T, Romero J, Kohlmann A, Li F, Qi J, Cai L, Dwight TA, Xu Y, Xu R, Dodd R, Toms A, Parillon L, Lu X, Anjum R, Zhang S, Wang F, Keats J, Wardwell SD, Ning Y, Xu Q, Moran LE, Mohemmad QK, Jang HG, Clackson T, Narasimhan NI, Rivera VM, Zhu X, Dalgarno D, Shakespeare WC. Huang WS, et al. Among authors: rivera vm. J Med Chem. 2016 May 26;59(10):4948-64. doi: 10.1021/acs.jmedchem.6b00306. Epub 2016 May 12. J Med Chem. 2016. PMID: 27144831
A humanized system for pharmacologic control of gene expression.
Rivera VM, Clackson T, Natesan S, Pollock R, Amara JF, Keenan T, Magari SR, Phillips T, Courage NL, Cerasoli F Jr, Holt DA, Gilman M. Rivera VM, et al. Nat Med. 1996 Sep;2(9):1028-32. doi: 10.1038/nm0996-1028. Nat Med. 1996. PMID: 8782462
A versatile synthetic dimerizer for the regulation of protein-protein interactions.
Amara JF, Clackson T, Rivera VM, Guo T, Keenan T, Natesan S, Pollock R, Yang W, Courage NL, Holt DA, Gilman M. Amara JF, et al. Among authors: rivera vm. Proc Natl Acad Sci U S A. 1997 Sep 30;94(20):10618-23. doi: 10.1073/pnas.94.20.10618. Proc Natl Acad Sci U S A. 1997. PMID: 9380684 Free PMC article.
Inhibition of wild-type and mutant Bcr-Abl by AP23464, a potent ATP-based oncogenic protein kinase inhibitor: implications for CML.
O'Hare T, Pollock R, Stoffregen EP, Keats JA, Abdullah OM, Moseson EM, Rivera VM, Tang H, Metcalf CA 3rd, Bohacek RS, Wang Y, Sundaramoorthi R, Shakespeare WC, Dalgarno D, Clackson T, Sawyer TK, Deininger MW, Druker BJ. O'Hare T, et al. Among authors: rivera vm. Blood. 2004 Oct 15;104(8):2532-9. doi: 10.1182/blood-2004-05-1851. Epub 2004 Jul 15. Blood. 2004. PMID: 15256422 Free article.
AP24534, a pan-BCR-ABL inhibitor for chronic myeloid leukemia, potently inhibits the T315I mutant and overcomes mutation-based resistance.
O'Hare T, Shakespeare WC, Zhu X, Eide CA, Rivera VM, Wang F, Adrian LT, Zhou T, Huang WS, Xu Q, Metcalf CA 3rd, Tyner JW, Loriaux MM, Corbin AS, Wardwell S, Ning Y, Keats JA, Wang Y, Sundaramoorthi R, Thomas M, Zhou D, Snodgrass J, Commodore L, Sawyer TK, Dalgarno DC, Deininger MW, Druker BJ, Clackson T. O'Hare T, et al. Among authors: rivera vm. Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028. Cancer Cell. 2009. PMID: 19878872 Free PMC article.
183 results