Advances in Orphan Nuclear Receptor Pharmacology: A New Era in Drug Discovery

Over the past decade, advances in biophysical chemistry, genomic analysis, and structural biology have resulted in the exponential growth of knowledge and critical insight into the function and regulation of orphan nuclear receptors. This article summarizes the current progress in illuminating the structure, function, and regulation of orphan nuclear receptors and their involvement in the physiology, development and molecular mechanism of different pathological conditions. Moreover, current strategies for discovering endogenous ligands, downstream NR-regulated target genes, and new drugs for future therapeutics will be discussed.