1ol2
CYCLIN A BINDING GROOVE INHIBITOR H-ARG-ARG-LEU-ASN-(P-F-PHE)-NH2
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OverviewOverview
Inhibition of CDK2/CA (cyclin-dependent kinase 2/cyclin A complex), activity through blocking of the substrate recognition site in the cyclin, A subunit has been demonstrated to be an effective method for inducing, apoptosis in tumor cells. We have used the cyclin binding motif (CBM), present in the tumor suppressor proteins p21(WAF1) and p27(KIP1) as a, template to optimize the minimal sequence necessary for CDK2/CA, inhibition. A series of peptides were prepared, containing nonnatural, amino acids, which possess nano- to micromolar CDK2-inhibitory activity., Here we present X-ray structures of the protein complex CDK2/CA, together, with the cyclin groove-bound peptides, H-Ala-Ala-Abu-Arg-Ser-Leu-Ile-(p-F-Phe)-NH(2) (peptide 1), H-Arg-Arg-Leu-Ile-Phe-NH(2) (peptide 2), ... [(full description)]
About this StructureAbout this Structure
1OL2 is a [Protein complex] structure of sequences from [Homo sapiens] with NH2 as [ligand]. Active as [[1]], with EC number [2.7.1.37]. Full crystallographic information is available from [OCA].
ReferenceReference
Insights into cyclin groove recognition: complex crystal structures and inhibitor design through ligand exchange., Kontopidis G, Andrews MJ, McInnes C, Cowan A, Powers H, Innes L, Plater A, Griffiths G, Paterson D, Zheleva DI, Lane DP, Green S, Walkinshaw MD, Fischer PM, Structure. 2003 Dec;11(12):1537-46. PMID:14656438
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