6hj2

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'''Unreleased structure'''
 
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The entry 6hj2 is ON HOLD until Mar 02 2021
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==Crystal structure of hPXR in complex with dabrafenib==
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<StructureSection load='6hj2' size='340' side='right'caption='[[6hj2]], [[Resolution|resolution]] 2.28&Aring;' scene=''>
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Authors: Granell, M., Delfosse, V., Bourguet, W.
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== Structural highlights ==
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<table><tr><td colspan='2'>[[6hj2]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6HJ2 OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6HJ2 FirstGlance]. <br>
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Description: Crystal structure of hPXR in complex with dabrafenib
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=IPA:ISOPROPYL+ALCOHOL'>IPA</scene>, <scene name='pdbligand=P06:DABRAFENIB'>P06</scene></td></tr>
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[[Category: Unreleased Structures]]
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=6hj2 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6hj2 OCA], [http://pdbe.org/6hj2 PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=6hj2 RCSB], [http://www.ebi.ac.uk/pdbsum/6hj2 PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=6hj2 ProSAT]</span></td></tr>
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[[Category: Granell, M]]
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</table>
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== Function ==
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[[http://www.uniprot.org/uniprot/NR1I2_HUMAN NR1I2_HUMAN]] Nuclear receptor that binds and is activated by variety of endogenous and xenobiotic compounds. Transcription factor that activates the transcription of multiple genes involved in the metabolism and secretion of potentially harmful xenobiotics, drugs and endogenous compounds. Activated by the antibiotic rifampicin and various plant metabolites, such as hyperforin, guggulipid, colupulone, and isoflavones. Response to specific ligands is species-specific. Activated by naturally occurring steroids, such as pregnenolone and progesterone. Binds to a response element in the promoters of the CYP3A4 and ABCB1/MDR1 genes.<ref>PMID:9727070</ref> <ref>PMID:11668216</ref> <ref>PMID:11297522</ref> <ref>PMID:19297428</ref> <ref>PMID:12578355</ref> <ref>PMID:18768384</ref>
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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: Large Structures]]
[[Category: Bourguet, W]]
[[Category: Bourguet, W]]
[[Category: Delfosse, V]]
[[Category: Delfosse, V]]
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[[Category: Granell, M]]
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[[Category: Nuclear protein]]
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[[Category: Pregnane x receptor anti-cancer drug endocrine disruptor nuclear receptor]]

Revision as of 10:02, 27 March 2020

Crystal structure of hPXR in complex with dabrafenib

PDB ID 6hj2

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