3zrb
From Proteopedia
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| - | [[ | + | ==STRUCTURAL BASIS FOR AGONISM AND ANTAGONISM FOR A SET OF CHEMICALLY RELATED PROGESTERONE RECEPTOR MODULATORS== |
| + | <StructureSection load='3zrb' size='340' side='right' caption='[[3zrb]], [[Resolution|resolution]] 1.80Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[3zrb]] is a 2 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ZRB OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ZRB FirstGlance]. <br> | ||
| + | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=OR8:2-CHLORO-N-[[4-(3,5-DIMETHYLISOXAZOL-4-YL)PHENYL]METHYL]-1,4-DIMETHYL-1H-PYRAZOLE-4-SULFONAMIDE'>OR8</scene>, <scene name='pdbligand=ORC:(R)-N-[1-[4-(3,5-DIMETHYLISOXAZOL-4-YL)PHENYL]ETHYL]-3,5-DIMETHYLISOXAZOLE-4-SULFONAMIDE'>ORC</scene>, <scene name='pdbligand=SO4:SULFATE+ION'>SO4</scene><br> | ||
| + | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[2c7a|2c7a]], [[2w8y|2w8y]], [[1a28|1a28]], [[1zuc|1zuc]], [[3zr7|3zr7]], [[1sqn|1sqn]], [[1sr7|1sr7]], [[1e3k|1e3k]], [[3zra|3zra]]</td></tr> | ||
| + | <tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3zrb FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3zrb OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3zrb RCSB], [http://www.ebi.ac.uk/pdbsum/3zrb PDBsum]</span></td></tr> | ||
| + | <table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | The progesterone receptor is able to bind to a large number and variety of ligands that elicit a broad range of transcriptional responses ranging from full agonism to full antagonism and numerous mixed profiles inbetween. We describe here two new progesterone receptor ligand binding domain x-ray structures bound to compounds from a structurally related but functionally divergent series, which show different binding modes corresponding to their agonistic or antagonistic nature. In addition, we present a third progesterone receptor ligand binding domain dimer bound to an agonist in monomer A and an antagonist in monomer B, which display binding modes in agreement with the earlier observation that agonists and antagonists from this series adopt different binding modes. | ||
| - | + | Structural basis for agonism and antagonism for a set of chemically related progesterone receptor modulators.,Lusher SJ, Raaijmakers HC, Vu-Pham D, Dechering K, Lam TW, Brown AR, Hamilton NM, Nimz O, Bosch R, McGuire R, Oubrie A, de Vlieg J J Biol Chem. 2011 Oct 7;286(40):35079-86. Epub 2011 Aug 17. PMID:21849509<ref>PMID:21849509</ref> | |
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| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | + | </div> | |
| - | + | == References == | |
| - | + | <references/> | |
| - | + | __TOC__ | |
| - | + | </StructureSection> | |
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[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: Azevedo, R.]] | [[Category: Azevedo, R.]] | ||
Revision as of 08:32, 5 June 2014
STRUCTURAL BASIS FOR AGONISM AND ANTAGONISM FOR A SET OF CHEMICALLY RELATED PROGESTERONE RECEPTOR MODULATORS
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