Warianty tytułu
Języki publikacji
Abstrakty
An active form of an insulin receptor tyrosine kinase (IRK) catalytic core was modelled based on its experimentally known inactive form and the active form of a serine/threonine kinase, protein kinase A (PKA). This theoretical model was compared with the crystallographic structure of the active form of IRK reported later. The structures are very similar, which shows that all the most important features and interactions have been taken into account in the modelling procedure. The elaborated procedure can be applied to other tyrosine kinases. This would allow designing of a wide class of tyrosine kinase inhibitors, very important potential anti-cancer and/or anti-viral drugs.
Wydawca
Czasopismo
Rocznik
Tom
Numer
Opis fizyczny
p.601-607,fig.
Twórcy
autor
- Warsaw University, S.Zwirki i F.Wigury 93, 02-089 Warsaw, Poland
autor
autor
Bibliografia
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- 6. Wei, L.. Hubbard, S.R., Hendrickson, W.A. & Ellis, L. (1995) Expression, characterization, and crystallization of the catalytic core of the human insulin receptor protein-tyrosine kinase domain. J. Biol Chem. 270, 8122-8130.
- 7. Rosen, O.M., Herrera, R., Olowe, Y., Petruzzelli, L.M. & Cobb, M.H. (1983) Phosphorylation activates the insulin receptor tyrosine protein kinase. Proc. Natl Acad. Sci. U.S.A. 80, 3237-3240.
- 8. Ellis, L., Clauser, E., Morgan, D.O., Edery, M., Roth, R.A. & Rutter, W.J. (1986) Replacement of insulin receptor tyrosine residues 1162 and 1163 compromises insulin-stimulated kinase activity and uptake of 2-deoxyglucose. Cell 45, 721-732.
- 9. Hubbard, S.R., Wei, L., Ellis, L. &. Hendrickson, W.A. (1994) Crystal structure of the tyrosine kinase domain of the human insulin receptor. Nature 372, 746-754.
- 10. Ginalski, K., Lesyng, B., Sowadski, J. & Wojciechowski, M. (1997) Modelling of active forms of protein kinases: p38 — A case study. Acta Biochim. Poloru 44, 557-564.
- 11. Miller, M., Zbar, B., Ginalski, K. & Lesyng, B. (1998) Structural basis of oncogenesis caused by point mutations in the kinase domain of the MET proto-oncogene. Cell Mol Biol Lett 3, 273-274.
- 12. Hubbard, S.R. (1997) Crystal structure of the activated insulin receptor tyrosine kinase in complex with peptide substrate and ATP analog. EMBOJ. IB, 5572-5581.
- 13. Zheng, J., Trafny, E.A., Knighton, D.R., Xuong, N.-H., Taylor, S.S., Ten Eyck, L.F. & Sowadski, J.M. (1993) 2.2 A refined crystal structure of the catalytic subunit of cAMP-dependent protein kinase complexed with MnATP and peptide inhibitor. Acta Crystallog. D 49, 362-365.
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- 15. Zhou, S., Carraway III, K.L., Eck, M.J., Harrison, S.C., Feldman, R.A., Mohammadi, M., Schlessinger, J., Hubbard, S.R., Smith, D.P., Eng, C., Lorenzo, M.J., Ponder, B.A.J., Mayer, B.J. & Cantley, L.C. (1995) Catalytic specificity of protein-tyrosine kinases is critical for selective signalling. Nature 373, 536- 539.
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Typ dokumentu
Bibliografia
Identyfikatory
Identyfikator YADDA
bwmeta1.element.agro-article-76c3b8a4-dd58-463c-ba7b-b844952ec803