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Structure paper

TitleX-ray structures of progesterone receptor ligand binding domain in its agonist state reveal differing mechanisms for mixed profiles of 11 beta-substituted steroids.
Journal, issue, pagesJ. Biol. Chem., Vol. 287, Page 20333-20343, Year 2012
Publish dateSep 27, 2011 (structure data deposition date)
AuthorsLusher, S.J. / Raaijmakers, H.C. / Vu-Pham, D. / Kazemier, B. / Bosch, R. / McGuire, R. / Azevedo, R. / Hamersma, H. / Dechering, K. / Oubrie, A. ...Lusher, S.J. / Raaijmakers, H.C. / Vu-Pham, D. / Kazemier, B. / Bosch, R. / McGuire, R. / Azevedo, R. / Hamersma, H. / Dechering, K. / Oubrie, A. / van Duin, M. / de Vlieg, J.
External linksJ. Biol. Chem. / PubMed:22535964
MethodsX-ray diffraction
Resolution1.9 - 2 Å
Structure data

PDB-4a2j:
PR X-Ray structures in agonist conformations reveal two different mechanisms for partial agonism in 11beta-substituted steroids
Method: X-RAY DIFFRACTION / Resolution: 2 Å

PDB-4apu:
PR X-Ray structures in agonist conformations reveal two different mechanisms for partial agonism in 11beta-substituted steroids
Method: X-RAY DIFFRACTION / Resolution: 1.9 Å

Chemicals

ChemComp-AS0:
4-[(11BETA,17BETA)-17-METHOXY-17-(METHOXYMETHYL)-3-OXOESTRA-4,9-DIEN-11-YL]BENZALDEHYDE OXIME

ChemComp-SO4:
SULFATE ION

ChemComp-HOH:
WATER

ChemComp-OR8:
2-CHLORO-N-[[4-(3,5-DIMETHYLISOXAZOL-4-YL)PHENYL]METHYL]-1,4-DIMETHYL-1H-PYRAZOLE-4-SULFONAMIDE

ChemComp-A2K:
(8S,11R,13S,14S,16S,17S)-17-cyclopropylcarbonyl-16-ethenyl-13-methyl-11-(4-pyridin-3-ylphenyl)-2,6,7,8,11,12,14,15,16,17-decahydro-1H-cyclopenta[a]phenanthren-3-one

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / PARTIAL AGONIST / ASOPRISNIL

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