1t4e

From Proteopedia

(Difference between revisions)
Jump to: navigation, search
Line 1: Line 1:
[[Image:1t4e.gif|left|200px]]
[[Image:1t4e.gif|left|200px]]
-
{{Structure
+
<!--
-
|PDB= 1t4e |SIZE=350|CAPTION= <scene name='initialview01'>1t4e</scene>, resolution 2.60&Aring;
+
The line below this paragraph, containing "STRUCTURE_1t4e", creates the "Structure Box" on the page.
-
|SITE=
+
You may change the PDB parameter (which sets the PDB file loaded into the applet)
-
|LIGAND= <scene name='pdbligand=DIZ:(4-CHLOROPHENYL)[3-(4-CHLOROPHENYL)-7-IODO-2,5-DIOXO-1,2,3,5-TETRAHYDRO-4H-1,4-BENZODIAZEPIN-4-YL]ACETIC+ACID'>DIZ</scene>
+
or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
-
|ACTIVITY=
+
or leave the SCENE parameter empty for the default display.
-
|GENE= MDM2 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
+
-->
-
|DOMAIN=
+
{{STRUCTURE_1t4e| PDB=1t4e | SCENE= }}
-
|RELATEDENTRY=[[1rv1|1RV1]], [[1ycr|1YCR]], [[1t4f|1T4F]]
+
-
|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1t4e FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1t4e OCA], [http://www.ebi.ac.uk/pdbsum/1t4e PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1t4e RCSB]</span>
+
-
}}
+
'''Structure of Human MDM2 in complex with a Benzodiazepine Inhibitor'''
'''Structure of Human MDM2 in complex with a Benzodiazepine Inhibitor'''
Line 34: Line 31:
[[Category: Schubert, C.]]
[[Category: Schubert, C.]]
[[Category: Zhao, S Y.]]
[[Category: Zhao, S Y.]]
-
[[Category: mdm2-inhibitor complex]]
+
[[Category: Mdm2-inhibitor complex]]
-
 
+
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 09:30:40 2008''
-
''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Mar 30 23:51:08 2008''
+

Revision as of 06:30, 3 May 2008

Image:1t4e.gif

Template:STRUCTURE 1t4e

Structure of Human MDM2 in complex with a Benzodiazepine Inhibitor


Overview

HDM2 binds to an alpha-helical transactivation domain of p53, inhibiting its tumor suppressive functions. A miniaturized thermal denaturation assay was used to screen chemical libraries, resulting in the discovery of a novel series of benzodiazepinedione antagonists of the HDM2-p53 interaction. The X-ray crystal structure of improved antagonists bound to HDM2 reveals their alpha-helix mimetic properties. These optimized molecules increase the transcription of p53 target genes and decrease proliferation of tumor cells expressing wild-type p53.

About this Structure

1T4E is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Discovery and cocrystal structure of benzodiazepinedione HDM2 antagonists that activate p53 in cells., Grasberger BL, Lu T, Schubert C, Parks DJ, Carver TE, Koblish HK, Cummings MD, LaFrance LV, Milkiewicz KL, Calvo RR, Maguire D, Lattanze J, Franks CF, Zhao S, Ramachandren K, Bylebyl GR, Zhang M, Manthey CL, Petrella EC, Pantoliano MW, Deckman IC, Spurlino JC, Maroney AC, Tomczuk BE, Molloy CJ, Bone RF, J Med Chem. 2005 Feb 24;48(4):909-12. PMID:15715460 Page seeded by OCA on Sat May 3 09:30:40 2008

Proteopedia Page Contributors and Editors (what is this?)

OCA

Retrieved from "http://52.214.119.220/wiki/index.php/1t4e"
Personal tools