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TitlePROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network.
Journal, issue, pagesStructure, Vol. 32, Page 2352-2363.e8, Year 2024
Publish dateApr 16, 2024 (structure data deposition date)
AuthorsHuber, A.D. / Lin, W. / Poudel, S. / Miller, D.J. / Chen, T.
External linksStructure / PubMed:39389062
MethodsX-ray diffraction
Resolution2.6 Å
Structure data

PDB-9beq:
Crystal structure of pregnane X receptor ligand binding domain complexed with AP1867
Method: X-RAY DIFFRACTION / Resolution: 2.6 Å

Chemicals

ChemComp-AP1:
{3-[3-(3,4-DIMETHOXY-PHENYL)-1-(1-{1-[2-(3,4,5-TRIMETHOXY-PHENYL)-BUTYRYL]-PIPERIDIN-2YL}-VINYLOXY)-PROPYL]-PHENOXY}-ACETIC ACID

ChemComp-HOH:
WATER

Source
  • homo sapiens (human)
KeywordsTRANSCRIPTION / PXR / pregnane X receptor / NR1I2 / nuclear receptor / drug metabolism / AP1867 / FKBP

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