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Items: 1 to 20 of 162

1.

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.

J Med Chem. 2010 Jun 24;53(12):4701-19. doi: 10.1021/jm100395q.

PMID:
20513156
2.

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.

Cancer Cell. 2009 Nov 6;16(5):401-12. doi: 10.1016/j.ccr.2009.09.028.

3.

Structural mechanism of the Pan-BCR-ABL inhibitor ponatinib (AP24534): lessons for overcoming kinase inhibitor resistance.

Zhou T, Commodore L, Huang WS, Wang Y, Thomas M, Keats J, Xu Q, Rivera VM, Shakespeare WC, Clackson T, Dalgarno DC, Zhu X.

Chem Biol Drug Des. 2011 Jan;77(1):1-11. doi: 10.1111/j.1747-0285.2010.01054.x. Epub 2010 Nov 30.

PMID:
21118377
4.

Identification of GZD824 as an orally bioavailable inhibitor that targets phosphorylated and nonphosphorylated breakpoint cluster region-Abelson (Bcr-Abl) kinase and overcomes clinically acquired mutation-induced resistance against imatinib.

Ren X, Pan X, Zhang Z, Wang D, Lu X, Li Y, Wen D, Long H, Luo J, Feng Y, Zhuang X, Zhang F, Liu J, Leng F, Lang X, Bai Y, She M, Tu Z, Pan J, Ding K.

J Med Chem. 2013 Feb 14;56(3):879-94. doi: 10.1021/jm301581y. Epub 2013 Jan 28.

PMID:
23301703
5.

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.

Bioorg Med Chem Lett. 2011 Jun 15;21(12):3743-8. doi: 10.1016/j.bmcl.2011.04.060. Epub 2011 Apr 22.

PMID:
21561767
6.

New Bcr-Abl inhibitors in chronic myeloid leukemia: keeping resistance in check.

O'Hare T, Eide CA, Deininger MW.

Expert Opin Investig Drugs. 2008 Jun;17(6):865-78. doi: 10.1517/13543784.17.6.865 . Review.

PMID:
18491988
7.

Design, synthesis, and biological evaluation of 3-(1H-1,2,3-triazol-1-yl)benzamide derivatives as Potent Pan Bcr-Abl inhibitors including the threonine(315)→isoleucine(315) mutant.

Li Y, Shen M, Zhang Z, Luo J, Pan X, Lu X, Long H, Wen D, Zhang F, Leng F, Li Y, Tu Z, Ren X, Ding K.

J Med Chem. 2012 Nov 26;55(22):10033-46. doi: 10.1021/jm301188x. Epub 2012 Nov 1.

PMID:
23088644
8.

Overcoming Bcr-Abl T315I mutation by combination of GNF-2 and ATP competitors in an Abl-independent mechanism.

Khateb M, Ruimi N, Khamisie H, Najajreh Y, Mian A, Metodieva A, Ruthardt M, Mahajna J.

BMC Cancer. 2012 Nov 27;12:563. doi: 10.1186/1471-2407-12-563.

9.

PF-114, a potent and selective inhibitor of native and mutated BCR/ABL is active against Philadelphia chromosome-positive (Ph+) leukemias harboring the T315I mutation.

Mian AA, Rafiei A, Haberbosch I, Zeifman A, Titov I, Stroylov V, Metodieva A, Stroganov O, Novikov F, Brill B, Chilov G, Hoelzer D, Ottmann OG, Ruthardt M.

Leukemia. 2015 May;29(5):1104-14. doi: 10.1038/leu.2014.326. Epub 2014 Nov 14.

PMID:
25394714
10.

Enhanced ABL-inhibitor-induced MAPK-activation in T315I-BCR-ABL-expressing cells: a potential mechanism of altered leukemogenicity.

Härtel N, Klag T, Hanfstein B, Mueller MC, Schenk T, Erben P, Hochhaus A, La Rosée P.

J Cancer Res Clin Oncol. 2012 Feb;138(2):203-12. doi: 10.1007/s00432-011-1086-x. Epub 2011 Nov 17.

PMID:
22089930
11.

Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformation.

Pemovska T, Johnson E, Kontro M, Repasky GA, Chen J, Wells P, Cronin CN, McTigue M, Kallioniemi O, Porkka K, Murray BW, Wennerberg K.

Nature. 2015 Mar 5;519(7541):102-5. doi: 10.1038/nature14119. Epub 2015 Feb 9.

PMID:
25686603
12.

Ponatinib in refractory Philadelphia chromosome-positive leukemias.

Cortes JE, Kantarjian H, Shah NP, Bixby D, Mauro MJ, Flinn I, O'Hare T, Hu S, Narasimhan NI, Rivera VM, Clackson T, Turner CD, Haluska FG, Druker BJ, Deininger MW, Talpaz M.

N Engl J Med. 2012 Nov 29;367(22):2075-88. doi: 10.1056/NEJMoa1205127.

13.

A type-II kinase inhibitor capable of inhibiting the T315I "gatekeeper" mutant of Bcr-Abl.

Choi HG, Ren P, Adrian F, Sun F, Lee HS, Wang X, Ding Q, Zhang G, Xie Y, Zhang J, Liu Y, Tuntland T, Warmuth M, Manley PW, Mestan J, Gray NS, Sim T.

J Med Chem. 2010 Aug 12;53(15):5439-48. doi: 10.1021/jm901808w.

14.

Recent developments in the third generation inhibitors of Bcr-Abl for overriding T315I mutation.

Lu XY, Cai Q, Ding K.

Curr Med Chem. 2011;18(14):2146-57. Review.

PMID:
21517764
15.

Discovery of picomolar ABL kinase inhibitors equipotent for wild type and T315I mutant via structure-based de novo design.

Park H, Hong S, Kim J, Hong S.

J Am Chem Soc. 2013 Jun 5;135(22):8227-37. doi: 10.1021/ja311756u. Epub 2013 May 24.

PMID:
23679864
16.

Triptolide inhibits Bcr-Abl transcription and induces apoptosis in STI571-resistant chronic myelogenous leukemia cells harboring T315I mutation.

Shi X, Jin Y, Cheng C, Zhang H, Zou W, Zheng Q, Lu Z, Chen Q, Lai Y, Pan J.

Clin Cancer Res. 2009 Mar 1;15(5):1686-97. doi: 10.1158/1078-0432.CCR-08-2141. Epub 2009 Feb 24.

17.

Allosteric inhibition enhances the efficacy of ABL kinase inhibitors to target unmutated BCR-ABL and BCR-ABL-T315I.

Mian AA, Metodieva A, Badura S, Khateb M, Ruimi N, Najajreh Y, Ottmann OG, Mahajna J, Ruthardt M.

BMC Cancer. 2012 Sep 17;12:411. doi: 10.1186/1471-2407-12-411.

18.

Combining the ABL1 kinase inhibitor ponatinib and the histone deacetylase inhibitor vorinostat: a potential treatment for BCR-ABL-positive leukemia.

Okabe S, Tauchi T, Kimura S, Maekawa T, Kitahara T, Tanaka Y, Ohyashiki K.

PLoS One. 2014 Feb 28;9(2):e89080. doi: 10.1371/journal.pone.0089080. eCollection 2014.

19.

Discovery of 2-((3-Amino-4-methylphenyl)amino)-N-(2-methyl-5-(3-(trifluoromethyl)benzamido)phenyl)-4-(methylamino)pyrimidine-5-carboxamide (CHMFL-ABL-053) as a Potent, Selective, and Orally Available BCR-ABL/SRC/p38 Kinase Inhibitor for Chronic Myeloid Leukemia.

Liang X, Liu X, Wang B, Zou F, Wang A, Qi S, Chen C, Zhao Z, Wang W, Qi Z, Lv F, Hu Z, Wang L, Zhang S, Liu Q, Liu J.

J Med Chem. 2016 Mar 10;59(5):1984-2004. doi: 10.1021/acs.jmedchem.5b01618. Epub 2016 Feb 5.

PMID:
26789553
20.

Targeting the BCR-ABL signaling pathway in therapy-resistant Philadelphia chromosome-positive leukemia.

O'Hare T, Deininger MW, Eide CA, Clackson T, Druker BJ.

Clin Cancer Res. 2011 Jan 15;17(2):212-21. doi: 10.1158/1078-0432.CCR-09-3314. Epub 2010 Nov 22.

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