Identification of nuclear receptor ligands by Differential Scanning Fluorimetry(DSF) (CAT#: STEM-MB-0768-WXH)

Introduction

Identification of ligands that interact with nuclear receptors is both a major biological problem and an important initial step in drug discovery.
Nuclear receptors (NRs) are transcription factors found in all metazoa that regulate a wide variety of cellular, physiological and developmental processes. Canonically, the activities of NRs are modulated by interactions between small-molecule ligands and a structurally-conserved ligand-binding domain (LBD) of the NR, inducing conformational changes that result in new interaction surfaces for the recruitment of transcriptional coactivators and/or corepressors. The intrinsic chemical properties of known NR ligands, in particular, with most possessing the ability to diffuse readily through both aqueous and membranous environments, make them highly effective intercellular signaling molecules.