1rv1

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[[Image:1rv1.gif|left|200px]]
[[Image:1rv1.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 1rv1 |SIZE=350|CAPTION= <scene name='initialview01'>1rv1</scene>, resolution 2.30&Aring;
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The line below this paragraph, containing "STRUCTURE_1rv1", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=IMZ:CIS-[4,5-BIS-(4-BROMOPHENYL)-2-(2-ETHOXY-4-METHOXYPHENYL)-4,5-DIHYDROIMIDAZOL-1-YL]-[4-(2-HYDROXYETHYL)PIPERAZIN-1-YL]METHANONE'>IMZ</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= MDM2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_1rv1| PDB=1rv1 | SCENE= }}
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|RELATEDENTRY=[[1ycr|1YCR]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1rv1 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1rv1 OCA], [http://www.ebi.ac.uk/pdbsum/1rv1 PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1rv1 RCSB]</span>
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}}
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'''CRYSTAL STRUCTURE OF HUMAN MDM2 WITH AN IMIDAZOLINE INHIBITOR'''
'''CRYSTAL STRUCTURE OF HUMAN MDM2 WITH AN IMIDAZOLINE INHIBITOR'''
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[[Category: Kammlott, U.]]
[[Category: Kammlott, U.]]
[[Category: Lukacs, C.]]
[[Category: Lukacs, C.]]
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[[Category: mdm2]]
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[[Category: Mdm2]]
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[[Category: p53]]
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[[Category: P53]]
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[[Category: protein-protein interaction]]
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[[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 Mar 30 23:33:23 2008''
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Revision as of 04:56, 3 May 2008

Image:1rv1.gif

Template:STRUCTURE 1rv1

CRYSTAL STRUCTURE OF HUMAN MDM2 WITH AN IMIDAZOLINE INHIBITOR


Overview

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.

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 Page seeded by OCA on Sat May 3 07:56:41 2008

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