Harel Weinstein

TL;DR: This chapter discusses the integrated methods for the construction of three-dimensional models and computational probing of structure–function relations in G protein-coupled receptors (GPCR) and expects increased rate of success achieved by molecular modeling and computational simulation methods in providing structural insights relevant to the functions of biological molecules.

TL;DR: Besides the heuristically interesting nature of functional selectivity, there is a clear impact on drug discovery, because this mechanism raises the possibility of selecting or designing novel ligands that differentially activate only a subset of functions of a single receptor, thereby optimizing therapeutic action.

TL;DR: A likely candidate is identified: T1R3, a previously unknown G protein-coupled receptor (GPCR) and the only GPCR in this region of the sequenced human genome syntenous to the region of Sac in mouse, which is the major determinant of differences between sweet-sensitive and -insensitive strains of mice in their responsiveness to saccharin, sucrose and other sweeteners.

TL;DR: The structure and Conformation of GnRH and Its Analogs and the roles of individual amino acids in GnRH activity at the mammalian receptor are studied to derive conclusions about peptide structure-activity data.

TL;DR: Findings suggest that IANBD bound to 125Cys and 285Cys are exposed to a more polar environment upon agonist binding, and indicate that movements of transmembrane segments III and VI are involved in activation of G protein‐coupled receptors.