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Protein kinase inhibition by staurosporine revealed in details of the molecular interaction with CDK2.
Staurosporine exhibits nanomolar IC50 values against a wide range of protein kinases. The structure of a CDK2 staurosporine complex explains the tight binding of this inhibitor, and suggests features to be exploited in the design of specific inhibitors of CDKs.
PMID: 9334743 [PubMed - indexed for MEDLINE]
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Cited by 7 PubMed Central articles
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Crystal structures of the N-terminal kinase domain of human RSK1 bound to three different ligands: Implications for the design of RSK1 specific inhibitors.
Ikuta M, Kornienko M, Byrne N, Reid JC, Mizuarai S, Kotani H, Munshi SK.
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Structural and functional characterization of the human protein kinase ASK1.
Bunkoczi G, Salah E, Filippakopoulos P, Fedorov O, Müller S, Sobott F, Parker SA, Zhang H, Min W, Turk BE, et al.
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[Structure. 2007]
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Mitogen-activated protein kinases interacting kinases are autoinhibited by a reprogrammed activation segment.
Jauch R, Cho MK, Jäkel S, Netter C, Schreiter K, Aicher B, Zweckstetter M, Jäckle H, Wahl MC.
EMBO J. 2006 Sep 6; 25(17):4020-32. Epub 2006 Aug 17.
[EMBO J. 2006]
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Structures reported by this article