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Page 1
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: sawyer tk. 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.
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: sawyer tk. 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.
Discovery of 3-[2-(imidazo[1,2-b]pyridazin-3-yl)ethynyl]-4-methyl-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide (AP24534), a potent, orally active pan-inhibitor of breakpoint cluster region-abelson (BCR-ABL) kinase including the T315I gatekeeper mutant.
Huang WS, Metcalf CA, Sundaramoorthi R, Wang Y, Zou D, Thomas RM, Zhu X, Cai L, Wen D, Liu S, Romero J, Qi J, Chen I, Banda G, Lentini SP, Das S, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Zhou T, Commodore L, Narasimhan NI, Mohemmad QK, Iuliucci J, Rivera VM, Dalgarno DC, Sawyer TK, Clackson T, Shakespeare WC. Huang WS, et al. Among authors: sawyer tk. J Med Chem. 2010 Jun 24;53(12):4701-19. doi: 10.1021/jm100395q. J Med Chem. 2010. PMID: 20513156
In vitro and in vivo activity of ATP-based kinase inhibitors AP23464 and AP23848 against activation-loop mutants of Kit.
Corbin AS, Demehri S, Griswold IJ, Wang Y, Metcalf CA 3rd, Sundaramoorthi R, Shakespeare WC, Snodgrass J, Wardwell S, Dalgarno D, Iuliucci J, Sawyer TK, Heinrich MC, Druker BJ, Deininger MW. Corbin AS, et al. Among authors: sawyer tk. Blood. 2005 Jul 1;106(1):227-34. doi: 10.1182/blood-2004-12-4771. Epub 2005 Mar 3. Blood. 2005. PMID: 15746079 Free article.
AP23846, a novel and highly potent Src family kinase inhibitor, reduces vascular endothelial growth factor and interleukin-8 expression in human solid tumor cell lines and abrogates downstream angiogenic processes.
Summy JM, Trevino JG, Lesslie DP, Baker CH, Shakespeare WC, Wang Y, Sundaramoorthi R, Metcalf CA 3rd, Keats JA, Sawyer TK, Gallick GE. Summy JM, et al. Among authors: sawyer tk. Mol Cancer Ther. 2005 Dec;4(12):1900-11. doi: 10.1158/1535-7163.MCT-05-0171. Mol Cancer Ther. 2005. PMID: 16373705
Activity of dual SRC-ABL inhibitors highlights the role of BCR/ABL kinase dynamics in drug resistance.
Azam M, Nardi V, Shakespeare WC, Metcalf CA 3rd, Bohacek RS, Wang Y, Sundaramoorthi R, Sliz P, Veach DR, Bornmann WG, Clarkson B, Dalgarno DC, Sawyer TK, Daley GQ. Azam M, et al. Among authors: sawyer tk. Proc Natl Acad Sci U S A. 2006 Jun 13;103(24):9244-9. doi: 10.1073/pnas.0600001103. Epub 2006 Jun 5. Proc Natl Acad Sci U S A. 2006. PMID: 16754879 Free PMC article.
Antiangiogenic and antitumor effects of SRC inhibition in ovarian carcinoma.
Han LY, Landen CN, Trevino JG, Halder J, Lin YG, Kamat AA, Kim TJ, Merritt WM, Coleman RL, Gershenson DM, Shakespeare WC, Wang Y, Sundaramoorth R, Metcalf CA 3rd, Dalgarno DC, Sawyer TK, Gallick GE, Sood AK. Han LY, et al. Among authors: sawyer tk. Cancer Res. 2006 Sep 1;66(17):8633-9. doi: 10.1158/0008-5472.CAN-06-1410. Cancer Res. 2006. PMID: 16951177 Free PMC article.
Discovery of 5-(arenethynyl) hetero-monocyclic derivatives as potent inhibitors of BCR-ABL including the T315I gatekeeper mutant.
Thomas M, Huang WS, Wen D, Zhu X, Wang Y, Metcalf CA, Liu S, Chen I, Romero J, Zou D, Sundaramoorthi R, Li F, Qi J, Cai L, Zhou T, Commodore L, Xu Q, Keats J, Wang F, Wardwell S, Ning Y, Snodgrass JT, Broudy MI, Russian K, Iuliucci J, Rivera VM, Sawyer TK, Dalgarno DC, Clackson T, Shakespeare WC. Thomas M, et al. Among authors: sawyer tk. Bioorg Med Chem Lett. 2011 Jun 15;21(12):3743-8. doi: 10.1016/j.bmcl.2011.04.060. Epub 2011 Apr 22. Bioorg Med Chem Lett. 2011. PMID: 21561767
208 results