1rv1

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{{STRUCTURE_1rv1| PDB=1rv1 | SCENE= }}
{{STRUCTURE_1rv1| PDB=1rv1 | SCENE= }}
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'''CRYSTAL STRUCTURE OF HUMAN MDM2 WITH AN IMIDAZOLINE INHIBITOR'''
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===CRYSTAL STRUCTURE OF HUMAN MDM2 WITH AN IMIDAZOLINE INHIBITOR===
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==Overview==
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MDM2 binds the p53 tumor suppressor protein with high affinity and negatively modulates its transcriptional activity and stability. Overexpression of MDM2, found in many human tumors, effectively impairs p53 function. Inhibition of MDM2-p53 interaction can stabilize p53 and may offer a novel strategy for cancer therapy. Here, we identify potent and selective small-molecule antagonists of MDM2 and confirm their mode of action through the crystal structures of complexes. These compounds bind MDM2 in the p53-binding pocket and activate the p53 pathway in cancer cells, leading to cell cycle arrest, apoptosis, and growth inhibition of human tumor xenografts in nude mice.
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(as it appears on PubMed at http://www.pubmed.gov), where 14704432 is the PubMed ID number.
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{{ABSTRACT_PUBMED_14704432}}
==About this Structure==
==About this Structure==
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[[Category: P53]]
[[Category: P53]]
[[Category: Protein-protein interaction]]
[[Category: Protein-protein interaction]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 07:56:41 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Jul 27 21:12:44 2008''

Revision as of 18:12, 27 July 2008

Image:1rv1.png

Template:STRUCTURE 1rv1

CRYSTAL STRUCTURE OF HUMAN MDM2 WITH AN IMIDAZOLINE INHIBITOR

Template:ABSTRACT PUBMED 14704432

About this Structure

1RV1 is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

In vivo activation of the p53 pathway by small-molecule antagonists of MDM2., Vassilev LT, Vu BT, Graves B, Carvajal D, Podlaski F, Filipovic Z, Kong N, Kammlott U, Lukacs C, Klein C, Fotouhi N, Liu EA, Science. 2004 Feb 6;303(5659):844-8. Epub 2004 Jan 2. PMID:14704432

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