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Items: 1 to 20 of 172

1.

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.

2.

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.

3.

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
4.

The ABL switch control inhibitor DCC-2036 is active against the chronic myeloid leukemia mutant BCR-ABLT315I and exhibits a narrow resistance profile.

Eide CA, Adrian LT, Tyner JW, Mac Partlin M, Anderson DJ, Wise SC, Smith BD, Petillo PA, Flynn DL, Deininger MW, O'Hare T, Druker BJ.

Cancer Res. 2011 May 1;71(9):3189-95. doi: 10.1158/0008-5472.CAN-10-3224. Epub 2011 Apr 19.

5.

p185(BCR/ABL) has a lower sensitivity than p210(BCR/ABL) to the allosteric inhibitor GNF-2 in Philadelphia chromosome-positive acute lymphatic leukemia.

Mian AA, Metodieva A, Najajreh Y, Ottmann OG, Mahajna J, Ruthardt M.

Haematologica. 2012 Feb;97(2):251-7. doi: 10.3324/haematol.2011.047191. Epub 2011 Nov 4.

6.

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
7.

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
8.

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
9.

Dynamic change of T315I BCR-ABL kinase domain mutation in Korean chronic myeloid leukaemia patients during treatment with Abl tyrosine kinase inhibitors.

Kim WS, Kim D, Kim DW, Kweon IY, Kim SH, Goh HG, Park SH, Lee J.

Hematol Oncol. 2010 Jun;28(2):82-8. doi: 10.1002/hon.918.

PMID:
19768693
10.

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.

11.

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.

12.

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
13.
14.

Overcoming kinase resistance in chronic myeloid leukemia.

Lee F, Fandi A, Voi M.

Int J Biochem Cell Biol. 2008;40(3):334-43. Review.

PMID:
18401881
15.

Treatment of human pre-B acute lymphoblastic leukemia with the Aurora kinase inhibitor PHA-739358 (Danusertib).

Fei F, Lim M, Schmidhuber S, Moll J, Groffen J, Heisterkamp N.

Mol Cancer. 2012 Jun 21;11:42. doi: 10.1186/1476-4598-11-42.

16.

The gatekeeper mutation T315I confers resistance against small molecules by increasing or restoring the ABL-kinase activity accompanied by aberrant transphosphorylation of endogenous BCR, even in loss-of-function mutants of BCR/ABL.

Mian AA, Schüll M, Zhao Z, Oancea C, Hundertmark A, Beissert T, Ottmann OG, Ruthardt M.

Leukemia. 2009 Sep;23(9):1614-21. doi: 10.1038/leu.2009.69. Epub 2009 Apr 16.

PMID:
19369965
17.

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
18.

MK-0457, a novel kinase inhibitor, is active in patients with chronic myeloid leukemia or acute lymphocytic leukemia with the T315I BCR-ABL mutation.

Giles FJ, Cortes J, Jones D, Bergstrom D, Kantarjian H, Freedman SJ.

Blood. 2007 Jan 15;109(2):500-2. Epub 2006 Sep 21.

19.

The quantitative level of T315I mutated BCR-ABL predicts for major molecular response to second-line nilotinib or dasatinib treatment in patients with chronic myeloid leukemia.

Lange T, Ernst T, Gruber FX, Maier J, Cross M, Müller MC, Niederwieser D, Hochhaus A, Pfirrmann M.

Haematologica. 2013 May;98(5):714-7. doi: 10.3324/haematol.2012.068890. Epub 2012 Oct 12.

20.

SGX393 inhibits the CML mutant Bcr-AblT315I and preempts in vitro resistance when combined with nilotinib or dasatinib.

O'Hare T, Eide CA, Tyner JW, Corbin AS, Wong MJ, Buchanan S, Holme K, Jessen KA, Tang C, Lewis HA, Romero RD, Burley SK, Deininger MW.

Proc Natl Acad Sci U S A. 2008 Apr 8;105(14):5507-12. doi: 10.1073/pnas.0800587105. Epub 2008 Mar 26.

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