1t4f: Difference between revisions
New page: left|200px<br /> <applet load="1t4f" size="450" color="white" frame="true" align="right" spinBox="true" caption="1t4f, resolution 1.90Å" /> '''Structure of human ... |
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[[Image:1t4f.gif|left|200px]]<br /> | [[Image:1t4f.gif|left|200px]]<br /><applet load="1t4f" size="350" color="white" frame="true" align="right" spinBox="true" | ||
<applet load="1t4f" size=" | |||
caption="1t4f, resolution 1.90Å" /> | caption="1t4f, resolution 1.90Å" /> | ||
'''Structure of human MDM2 in complex with an optimized p53 peptide'''<br /> | '''Structure of human MDM2 in complex with an optimized p53 peptide'''<br /> | ||
==Overview== | ==Overview== | ||
HDM2 binds to an alpha-helical transactivation domain of p53, inhibiting | 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== | ==About this Structure== | ||
1T4F is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with SO4 as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | 1T4F is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=SO4:'>SO4</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1T4F OCA]. | ||
==Reference== | ==Reference== | ||
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Single protein]] | [[Category: Single protein]] | ||
[[Category: Carver, T | [[Category: Carver, T E.]] | ||
[[Category: Franks, C | [[Category: Franks, C F.]] | ||
[[Category: Grasberger, B | [[Category: Grasberger, B L.]] | ||
[[Category: Koblish, H | [[Category: Koblish, H K.]] | ||
[[Category: LaFrance, L | [[Category: LaFrance, L V.]] | ||
[[Category: Lu, T.]] | [[Category: Lu, T.]] | ||
[[Category: Parks, D | [[Category: Parks, D J.]] | ||
[[Category: Schubert, C.]] | [[Category: Schubert, C.]] | ||
[[Category: Zhao, S | [[Category: Zhao, S Y.]] | ||
[[Category: SO4]] | [[Category: SO4]] | ||
[[Category: mdm2-p53 peptide complex]] | [[Category: mdm2-p53 peptide complex]] | ||
[[Category: p53-binding protein mdm2 oncoprotein mdm2 double minute 2 protein hdm2]] | [[Category: p53-binding protein mdm2 oncoprotein mdm2 double minute 2 protein hdm2]] | ||
''Page seeded by [http:// | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 15:09:45 2008'' | ||
