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Molecular mechanisms of drug resistance in tyrosine kinases cAbl and cKit.

DiNitto JP, Wu JC.

Crit Rev Biochem Mol Biol. 2011 Aug;46(4):295-309. doi: 10.3109/10409238.2011.578612. Epub 2011 May 4. Review.


Flumatinib, a selective inhibitor of BCR-ABL/PDGFR/KIT, effectively overcomes drug resistance of certain KIT mutants.

Zhao J, Quan H, Xu Y, Kong X, Jin L, Lou L.

Cancer Sci. 2014 Jan;105(1):117-25. doi: 10.1111/cas.12320. Epub 2014 Jan 4.


Selecting tyrosine kinase inhibitors for gastrointestinal stromal tumor with secondary KIT activation-loop domain mutations.

Hsueh YS, Lin CL, Chiang NJ, Yen CC, Li CF, Shan YS, Ko CH, Shih NY, Wang LM, Chen TS, Chen LT.

PLoS One. 2013 Jun 20;8(6):e65762. doi: 10.1371/journal.pone.0065762. Print 2013.


A cell-based screen for resistance of Bcr-Abl-positive leukemia identifies the mutation pattern for PD166326, an alternative Abl kinase inhibitor.

von Bubnoff N, Veach DR, van der Kuip H, Aulitzky WE, Sänger J, Seipel P, Bornmann WG, Peschel C, Clarkson B, Duyster J.

Blood. 2005 Feb 15;105(4):1652-9. Epub 2004 Sep 30.


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.


Discovery of a small-molecule type II inhibitor of wild-type and gatekeeper mutants of BCR-ABL, PDGFRalpha, Kit, and Src kinases: novel type II inhibitor of gatekeeper mutants.

Weisberg E, Choi HG, Ray A, Barrett R, Zhang J, Sim T, Zhou W, Seeliger M, Cameron M, Azam M, Fletcher JA, Debiec-Rychter M, Mayeda M, Moreno D, Kung AL, Janne PA, Khosravi-Far R, Melo JV, Manley PW, Adamia S, Wu C, Gray N, Griffin JD.

Blood. 2010 May 27;115(21):4206-16. doi: 10.1182/blood-2009-11-251751. Epub 2010 Mar 18.


KIT signaling governs differential sensitivity of mature and primitive CML progenitors to tyrosine kinase inhibitors.

Corbin AS, O'Hare T, Gu Z, Kraft IL, Eiring AM, Khorashad JS, Pomicter AD, Zhang TY, Eide CA, Manley PW, Cortes JE, Druker BJ, Deininger MW.

Cancer Res. 2013 Sep 15;73(18):5775-86. doi: 10.1158/0008-5472.CAN-13-1318. Epub 2013 Jul 25.


Synergistic interactions between imatinib mesylate and the novel phosphoinositide-dependent kinase-1 inhibitor OSU-03012 in overcoming imatinib mesylate resistance.

Tseng PH, Lin HP, Zhu J, Chen KF, Hade EM, Young DC, Byrd JC, Grever M, Johnson K, Druker BJ, Chen CS.

Blood. 2005 May 15;105(10):4021-7. Epub 2005 Jan 21.


[STI571: a summary of targeted therapy].

Czyz M, Jakubowska J.

Postepy Hig Med Dosw (Online). 2006;60:677-96. Review. Polish.


Resistance to c-KIT kinase inhibitors conferred by V654A mutation.

Roberts KG, Odell AF, Byrnes EM, Baleato RM, Griffith R, Lyons AB, Ashman LK.

Mol Cancer Ther. 2007 Mar;6(3):1159-66.


Treatment of gastrointestinal stromal tumor after imatinib and sunitinib.

Montemurro M, Bauer S.

Curr Opin Oncol. 2011 Jul;23(4):367-72. doi: 10.1097/CCO.0b013e3283477ac2.


Association between imatinib-resistant BCR-ABL mutation-negative leukemia and persistent activation of LYN kinase.

Wu J, Meng F, Kong LY, Peng Z, Ying Y, Bornmann WG, Darnay BG, Lamothe B, Sun H, Talpaz M, Donato NJ.

J Natl Cancer Inst. 2008 Jul 2;100(13):926-39. doi: 10.1093/jnci/djn188. Epub 2008 Jun 24.


Lyn regulates BCR-ABL and Gab2 tyrosine phosphorylation and c-Cbl protein stability in imatinib-resistant chronic myelogenous leukemia cells.

Wu J, Meng F, Lu H, Kong L, Bornmann W, Peng Z, Talpaz M, Donato NJ.

Blood. 2008 Apr 1;111(7):3821-9. doi: 10.1182/blood-2007-08-109330. Epub 2008 Jan 30.


Mechanisms of resistance to tyrosine kinase inhibitors in chronic myeloid leukemia and recent therapeutic strategies to overcome resistance.

Bixby D, Talpaz M.

Hematology Am Soc Hematol Educ Program. 2009:461-76. doi: 10.1182/asheducation-2009.1.461. Review.


Mutated tyrosine kinases as therapeutic targets in myeloid leukemias.

Sattler M, Scheijen B, Weisberg E, Griffin JD.

Adv Exp Med Biol. 2003;532:121-40. Review.


Efficacy of dual-specific Bcr-Abl and Src-family kinase inhibitors in cells sensitive and resistant to imatinib mesylate.

Tipping AJ, Baluch S, Barnes DJ, Veach DR, Clarkson BM, Bornmann WG, Mahon FX, Goldman JM, Melo JV.

Leukemia. 2004 Aug;18(8):1352-6.


Long-term outcome of patients with chronic myeloid leukemia treated with second-generation tyrosine kinase inhibitors after imatinib failure is predicted by the in vitro sensitivity of BCR-ABL kinase domain mutations.

Jabbour E, Jones D, Kantarjian HM, O'Brien S, Tam C, Koller C, Burger JA, Borthakur G, Wierda WG, Cortes J.

Blood. 2009 Sep 3;114(10):2037-43. doi: 10.1182/blood-2009-01-197715. Epub 2009 Jun 30.


Function of activation loop tyrosine phosphorylation in the mechanism of c-Kit auto-activation and its implication in sunitinib resistance.

DiNitto JP, Deshmukh GD, Zhang Y, Jacques SL, Coli R, Worrall JW, Diehl W, English JM, Wu JC.

J Biochem. 2010 Apr;147(4):601-9. doi: 10.1093/jb/mvq015. Epub 2010 Feb 10.


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