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Volumn 12, Issue 6, 2002, Pages 735-741

Protein tyrosine kinases: Autoregulation and small-molecule inhibition

Author keywords

[No Author keywords available]

Indexed keywords

PROTEIN TYROSINE KINASE;

EID: 0036909260     PISSN: 0959440X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0959-440X(02)00383-4     Document Type: Review
Times cited : (75)

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    • Crystal structures of the Abl kinase domain with bona fide STI571, as well as with an inhibitor of the pyrido-pyrimidine class, reveal different modes of interaction between the compounds and the unphosphorylated activation loop. The pyrido-pyrimidine compound inhibits both unphosphorylated and phosphorylated forms of Abl equally well, which might explain its tenfold higher potency over STI571.
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    • Nagar, B.1    Bornmann, W.G.2    Pellicena, P.3    Schindler, T.4    Veach, D.R.5    Miller, W.T.6    Clarkson, B.7    Kuriyan, J.8
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    • Inhibition of the Abl protein-tyrosine kinase in vitro and in vivo by a 2-phenylaminopyrimidine derivative
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    • Analysis of the structural basis of specificity of inhibition of the Abl kinase by STI571
    • This mutagenesis study tests the effects of various Abl mutations on inhibition by STI571 and ATP binding. The Thr315→Ile mutation found in relapsed CML patients shows a marked decrease in STI571 susceptibility without loss of ATP binding, as would be predicted. The study reveals additional mutations that confer STI571 insensitivity while maintaining Abl catalytic activity.
    • Corbin A.S., Buchdunger E., Pascal F., Druker B.J. Analysis of the structural basis of specificity of inhibition of the Abl kinase by STI571. J Biol Chem. 277:2002;32214-32219. This mutagenesis study tests the effects of various Abl mutations on inhibition by STI571 and ATP binding. The Thr315→Ile mutation found in relapsed CML patients shows a marked decrease in STI571 susceptibility without loss of ATP binding, as would be predicted. The study reveals additional mutations that confer STI571 insensitivity while maintaining Abl catalytic activity.
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    • Corbin, A.S.1    Buchdunger, E.2    Pascal, F.3    Druker, B.J.4
  • 48
    • 0035800507 scopus 로고    scopus 로고
    • Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification
    • Gorre M.E., Mohammed M., Ellwood K., Hsu N., Paquette R., Rao P.N., Sawyers C.L. Clinical resistance to STI-571 cancer therapy caused by BCR-ABL gene mutation or amplification. Science. 293:2001;876-880.
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    • Gorre, M.E.1    Mohammed, M.2    Ellwood, K.3    Hsu, N.4    Paquette, R.5    Rao, P.N.6    Sawyers, C.L.7


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.