3zrb

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(New page: '''Unreleased structure''' The entry 3zrb is ON HOLD Authors: Lusher, S.J., raaijmakers, H.C.A., Vu-Pham, D., Dechering, K., Wai Lam, T., Brown, A.R., Hamilton, N.M., Nimz, O., Azevedo,...)
Current revision (10:42, 9 May 2024) (edit) (undo)
 
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'''Unreleased structure'''
 
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The entry 3zrb is ON HOLD
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==Structural basis for agonism and antagonism for a set of chemically related progesterone receptor modulators==
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<StructureSection load='3zrb' size='340' side='right'caption='[[3zrb]], [[Resolution|resolution]] 1.80&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[3zrb]] is a 2 chain structure with sequence from [https://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 [https://proteopedia.org/fgij/fg.htm?mol=3ZRB FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.8&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><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></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=3zrb FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3zrb OCA], [https://pdbe.org/3zrb PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3zrb RCSB], [https://www.ebi.ac.uk/pdbsum/3zrb PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3zrb ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/PRGR_HUMAN PRGR_HUMAN] The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. Progesterone receptor isoform B (PRB) is involved activation of c-SRC/MAPK signaling on hormone stimulation.<ref>PMID:15572662</ref> <ref>PMID:15798179</ref> <ref>PMID:17020914</ref> <ref>PMID:17347654</ref> <ref>PMID:17717077</ref> <ref>PMID:17173941</ref> <ref>PMID:18202149</ref> Isoform A is inactive in stimulating c-Src/MAPK signaling on hormone stimulation.<ref>PMID:15572662</ref> <ref>PMID:15798179</ref> <ref>PMID:17020914</ref> <ref>PMID:17347654</ref> <ref>PMID:17717077</ref> <ref>PMID:17173941</ref> <ref>PMID:18202149</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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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.
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Authors: Lusher, S.J., raaijmakers, H.C.A., Vu-Pham, D., Dechering, K., Wai Lam, T., Brown, A.R., Hamilton, N.M., Nimz, O., Azevedo, R., Mcguire, R., Oubrie, A., de vlieg, J.
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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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Description: Structural basis for agonism and antagonism for a set of chemically related progesterone receptor modulators
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 3zrb" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Progesterone receptor|Progesterone receptor]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Azevedo R]]
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[[Category: Brown AR]]
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[[Category: Dechering K]]
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[[Category: Hamilton NM]]
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[[Category: Lusher SJ]]
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[[Category: Mcguire R]]
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[[Category: Nimz O]]
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[[Category: Oubrie A]]
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[[Category: Raaijmakers HCA]]
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[[Category: Vu-Pham D]]
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[[Category: Wai Lam T]]
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[[Category: De Vlieg J]]

Current revision

Structural basis for agonism and antagonism for a set of chemically related progesterone receptor modulators

PDB ID 3zrb

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