Structure Biology and Drug Discovery of Nuclear Hormone Receptors(时间:2009年12月28日上午9:00)
报告题目:Structure Biology and Drug Discovery of Nuclear Hormone Receptors
报告人: H. Eric Xu, PhD
Laboratory of Structural Sciences, Van Andel Research Institute, USA
时间: 2009年12月28日上午9:00
.地点: 中科院遗传发育所1号楼B-210会议室
Abstract of Presentation:
The 48 human nuclear receptors can be categorized into classic endocrine receptors, adopted orphan receptors and true orphan receptors. The classic endocrine receptors include receptors for steroid hormones, retinoid acids, thyroid hormone, and vitamin D. The adopted orphan receptors are those for which no ligand was known when the receptor was cloned but since then either natural or/and synthetic ligands have been identified. Both the classic endocrine receptors and adopted receptors are important targets for drug discovery not only because of their profound roles in human physiology and diseases but also because of their inherited structure to interact with small molecules that are selected through evolution. In this presentation, he will describe crystal structures of the human glucocorticoid receptor and PPARs, two receptors that are critical in glucose regulation and inflammation, with focus on stereo insights of these structures into ligand recognition and drug discovery. He will also present the crystal structures of a number of orphan receptors for which no ligand has been identified to date, and describe how structural studies have helped to elucidate ligand-dependent and -independent regulation of these receptors. In the end, he will switch to an exciting progress in the field of plant hormone receptors for abscisic acids, which are crucial for stress response of plants to salt and drought environments.