2ayp | pdb_00002ayp
Crystal Structure of CHK1 with an Indol Inhibitor
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Overview
Chk1 inhibitors have emerged as a novel class of neoplastic agents for, abrogating the G2 DNA damage checkpoint arrest. Analogs of the Chk1, inhibitor, 3-ethylidene-1,3-dihydro-indol-2-one, were synthesized and, tested in vitro for their inhibitory activities. The most promising, compound identified from this series is analog 28, which possesses potent, enzymatic and cellular activities.
About this Structure
2AYP is a Single protein structure of sequence from Homo sapiens with 43A as ligand. Active as Non-specific serine/threonine protein kinase, with EC number 2.7.11.1 Full crystallographic information is available from OCA.
Reference
Synthesis and biological evaluation of 3-ethylidene-1,3-dihydro-indol-2-ones as novel checkpoint 1 inhibitors., Lin NH, Xia P, Kovar P, Park C, Chen Z, Zhang H, Rosenberg SH, Sham HL, Bioorg Med Chem Lett. 2006 Jan 15;16(2):421-6. Epub 2005 Oct 18. PMID:16242328
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