Ligand-Based Peptide Design and Combinatorial Peptide Libraries to Target G Protein-Coupled Receptors

Ligand-based peptide design and combinatorial peptide libraries to target G protein-coupled receptors.

G protein-coupled receptors (GPCRs) are considered to represent the most promising drug targets; it has been repeatedly said that a large fraction of the currently marketed drugs elicit their actions by binding to GPCRs (with cited numbers varying from 30-50%). Closer scrutiny, however, shows that only a modest fraction of (≈60) GPCRs are, in fact, exploited as drug targets, only ≈20 of which a...

Peptide ligand recognition by G protein-coupled receptors

The past few years have seen spectacular progress in the structure determination of G protein-coupled receptors (GPCRs). We now have structural representatives from classes A, B, C, and F. Within the rhodopsin-like class A, most structures belong to the α group, whereas fewer GPCR structures are available from the β, γ, and δ groups, which include peptide GPCRs such as the receptors for neurote...

Peptide interactions with G-protein coupled receptors.

Peptide recognition by G-protein coupled receptors (GPCRs) is reviewed with an emphasis on the indirect approach used to determine the receptor-bound conformation of peptide ligands. This approach was developed in response to the lack of detailed structural information available for these receptors. Recent advances in the structural determination of rhodopsin (the GPCR of the visual system) by ...

Ligand Design for G Protein-coupled Receptors

G-protein-coupled receptors for peptide hormones in yeast.

Introduction The conjugation of two haploid yeast cells is usually controlled by the reciprocal exchange of diffusible mating factors, cells of each mating type releasing peptides that induce matingspecific changes in cells of the opposite type. Binding of these peptides, or pheromones, to G-protein-coupled receptors at the surface of the target cell triggers an intracellular response that lead...