1okw

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[[Image:1okw.gif|left|200px]]
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{{STRUCTURE_1okw| PDB=1okw | SCENE= }}
{{STRUCTURE_1okw| PDB=1okw | SCENE= }}
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'''CYCLIN A BINDING GROOVE INHIBITOR AC-ARG-ARG-LEU-ASN-(M-CL-PHE)-NH2'''
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===CYCLIN A BINDING GROOVE INHIBITOR AC-ARG-ARG-LEU-ASN-(M-CL-PHE)-NH2===
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==Overview==
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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), Ac-Arg-Arg-Leu-Asn-(m-Cl-Phe)-NH(2) (peptide 3), H-Arg-Arg-Leu-Asn-(p-F-Phe)-NH(2) (peptide 4), and H-Cit-Cit-Leu-Ile-(p-F-Phe)-NH(2) (peptide 5). Some of the peptide complexes presented here were obtained through the novel technique of ligand exchange within protein crystals. This method may find general application for obtaining complex structures of proteins with surface-bound ligands.
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The line below this paragraph, {{ABSTRACT_PUBMED_14656438}}, adds the Publication Abstract to the page
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(as it appears on PubMed at http://www.pubmed.gov), where 14656438 is the PubMed ID number.
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{{ABSTRACT_PUBMED_14656438}}
==About this Structure==
==About this Structure==
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[[Category: Ligand exchange]]
[[Category: Ligand exchange]]
[[Category: Peptidomimetic]]
[[Category: Peptidomimetic]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 03:58:57 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 01:56:54 2008''

Revision as of 22:56, 27 July 2008

Image:1okw.png

Template:STRUCTURE 1okw

CYCLIN A BINDING GROOVE INHIBITOR AC-ARG-ARG-LEU-ASN-(M-CL-PHE)-NH2

Template:ABSTRACT PUBMED 14656438

About this Structure

1OKW is a Protein complex structure of sequences from Homo sapiens. Full crystallographic information is available from OCA.

Reference

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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