Comparison of activity, structure, and dynamics of SF-1 and LRH-1 complexed with small molecule modulators.

ABSTRACT: Steroidogenic factor-1 (SF-1) is a phospholipid-sensing nuclear receptor expressed in the adrenal glands, gonads, and hypothalamus which controls steroidogenesis and metabolism. There is significant therapeutic interest in SF-1 because of its oncogenic properties in adrenocortical cancer. Synthetic modulators are attractive for targeting SF-1 for clinical and laboratory purposes due to the poor pharmaceutical properties of its native phospholipid ligands. While small molecule agonists targeting SF-1 have been synthesized, no crystal structures have been reported of SF-1 in complexes with synthetic compounds. This has prevented the establishment of structure-activity relationships that would enable better characterization of ligand-mediated activation and improvement in current chemical sca

SUBMITTER: Cato ML 

PROVIDER: S-EPMC10407255 | biostudies-literature | 2023 Aug

REPOSITORIES: biostudies-literature