3le6 | pdb_00003le6

The structure of cyclin dependent kinase 2 (CKD2) with a pyrazolobenzodiazepine inhibitor

spinqualitylabelsall models 3le6, resolution 2.00Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 3le6 is a 1 chain structure with sequence from Homo sapiens. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: 2BZ Gene: CDK2 (Homo sapiens) Activity: Cyclin-dependent kinase, with EC number 2.7.11.22 Resources: FirstGlance, OCA, RCSB, PDBsum Publication Abstract from PubMed A novel series of pyrazolobenzodiazepines 3 has been identified as potent inhibitors of cyclin-dependent kinase 2 (CDK2). Their synthesis and structure-activity relationships (SAR) are described. Representative compounds from this class reversibly inhibit CDK2 activity in vitro, and block cell cycle progression in human tumor cell lines. Further exploration has revealed that this class of compounds inhibits several kinases that play critical roles in cancer cell growth and division as well as tumor angiogenesis. Together, these properties suggest a compelling basis for their use as antitumor agents. Pyrazolobenzodiazepines: part I. Synthesis and SAR of a potent class of kinase inhibitors.,Liu JJ, Daniewski I, Ding Q, Higgins B, Ju G, Kolinsky K, Konzelmann F, Lukacs C, Pizzolato G, Rossman P, Swain A, Thakkar K, Wei CC, Miklowski D, Yang H, Yin X, Wovkulich PM Bioorg Med Chem Lett. 2010 Oct 15;20(20):5984-7. Epub 2010 Aug 21. PMID:20832307 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Cell division protein kinase 2

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