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Structural Basis for Hydroxycholesterols as Natural Ligands of Orphan Nuclear Receptor RORγ
How hydroxycholesterols naturally bind to the orphan nuclear receptor RORgamma
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Abstract
Hydroxycholesterols promote the recruitment of coactivators by RORgamma.
- The crystal structures of RORgamma's ligand-binding domain were determined when bound to hydroxycholesterols.
- The binding modes of hydroxycholesterols within the RORgamma pocket were characterized.
- All observed RORgamma structures maintained the canonical active conformation.
- Mutations that disrupt hydroxycholesterol binding eliminate the constitutive activity of RORgamma.
- Endogenous hydroxycholesterols may play a significant role in regulating RORgamma-dependent biological processes.
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