Douglas J. Kojetin, Associate Professor, Department of Integrative Structural and Computational Biology, Department of Molecular Therapeutics, Scripps Research Institutte, FL, will give a talk titled: "Ligand-induced structural dynamics and function of PPARγ learned through NMR"

ABSTRACT

Structural studies of nuclear receptor transcription factors have revealed a conserved mechanism for agonist-induced coactivator interaction and transcriptional activation. In contrast, limited structural data indicate that ligand-induced corepressor-dependent nuclear receptor repression occurs through structurally diverse mechanisms. Furthermore, the conformational ensemble of the apo/ligand-free nuclear receptor ligand-binding domain, which is hypothesized to exchange between transcriptionally active and repressive conformations, remains poorly characterized. I will discuss our efforts to characterize how small molecule pharmacological ligands—agonists, antagonists, and inverse agonists—influence the conformational ensemble and function of the nuclear receptor PPARγ.