1urc

From Proteopedia

Revision as of 11:19, 30 October 2007

CYCLIN A BINDING GROOVE INHIBITOR ACE-ARG-LYS-LEU-PHE-GLY

Overview

Inhibition of cyclin A- and cyclin E-associated cyclin-dependent kinase-2, (CDK2) activities is an effective way of selective induction of apoptotic, cell death via the E2F pathway in tumour cells. The cyclin groove, recognition motif (CRM) in the natural CDK-inhibitory (CDKI) tumour, suppressor protein p27KIP1 was used as the basis for the design and, synthesis of a series of cyclic peptides whose biological activity and, structural characterisation by NMR and X-ray crystallography is reported., Whereas linear p27KIP1 sequence peptides were comparatively ineffective, introduction of side chain-to-tail constraints was found to be productive., An optimal macrocyclic ring size for the conformational constraint was, determined, mimicking the intramolecular H-bonding system of p27., Molecular ... [(full description)]

About this Structure

1URC is a [Protein complex] structure of sequences from [Homo sapiens] with ACE as [ligand]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: CBG. Full crystallographic information is available from [OCA].

Reference

Design, synthesis, biological activity and structural analysis of cyclic peptide inhibitors targeting the substrate recruitment site of cyclin-dependent kinase complexes., Andrews MJ, McInnes C, Kontopidis G, Innes L, Cowan A, Plater A, Fischer PM, Org Biomol Chem. 2004 Oct 7;2(19):2735-41. Epub 2004 Sep 9. PMID:15455144

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