1ol2
From Proteopedia
(New page: 200px<br /> <applet load="1ol2" size="450" color="white" frame="true" align="right" spinBox="true" caption="1ol2, resolution 2.6Å" /> '''CYCLIN A BINDING GRO...) |
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==About this Structure== | ==About this Structure== | ||
| - | 1OL2 is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with NH2 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/ ]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]]. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1OL2 OCA]]. | + | 1OL2 is a [[http://en.wikipedia.org/wiki/Protein_complex Protein complex]] structure of sequences from [[http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]] with NH2 as [[http://en.wikipedia.org/wiki/ligand ligand]]. Active as [[http://en.wikipedia.org/wiki/Transferred_entry:_2.7.11.1 Transferred entry: 2.7.11.1]], with EC number [[http://www.brenda-enzymes.info/php/result_flat.php4?ecno=2.7.1.37 2.7.1.37]]. Structure known Active Site: CBB. Full crystallographic information is available from [[http://ispc.weizmann.ac.il/oca-bin/ocashort?id=1OL2 OCA]]. |
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Protein complex]] | [[Category: Protein complex]] | ||
| + | [[Category: Transferred entry: 2.7.11.1]] | ||
[[Category: Andrews, M.]] | [[Category: Andrews, M.]] | ||
[[Category: Cowan, A.]] | [[Category: Cowan, A.]] | ||
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[[Category: peptidomimetics]] | [[Category: peptidomimetics]] | ||
| - | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on | + | ''Page seeded by [http://ispc.weizmann.ac.il/oca OCA ] on Tue Oct 30 11:18:08 2007'' |
Revision as of 09:13, 30 October 2007
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CYCLIN A BINDING GROOVE INHIBITOR H-ARG-ARG-LEU-ASN-(P-F-PHE)-NH2
Overview
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 Structure
1OL2 is a [Protein complex] structure of sequences from [Homo sapiens] with NH2 as [ligand]. Active as [Transferred entry: 2.7.11.1], with EC number [2.7.1.37]. Structure known Active Site: CBB. 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
Page seeded by OCA on Tue Oct 30 11:18:08 2007
Categories: Homo sapiens | Protein complex | Transferred entry: 2.7.11.1 | Andrews, M. | Cowan, A. | Fischer, P. | Green, S. | Griffiths, G. | Innes, L. | Kontopidis, G. | Lane, D. | Mcinnes, C. | Paterson, D. | Plater, A. | Powers, H. | Walkinshaw, M. | Zheleva, D. | NH2 | Cyclin a | Drug design | Inhibitor | Kinase | Ligand exchange | Peptidomimetics
