Class B GPCRs of the secretin family are important drug targets in many human diseases including diabetes, neurodegeneration, cardiovascular disease and psychiatric disorders. X-ray crystal structures for the glucagon receptor and corticotropin-releasing factor receptor 1 have now been published.

2023年7月31日 · The residues that make up the PCO371-binding pocket are conserved in class B GPCRs, and a single alteration in PTH2R and two residue alterations in GLP1R convert these receptors to respond to...

2021年11月10日 · Two-thirds of human hormones and one-third of clinical drugs activate ~350 G-protein-coupled receptors (GPCR) belonging to four classes: A, B1, C and F.

2020年3月3日 · These manuscripts provide key insights into how peptide ligands are discriminated among class B GPCRs and expand our understanding of class B GPCR-G protein engagement and receptor activation.

2021年1月8日 · Class B. This class of GPCRs is divided into two subfamilies: secretin (B1) and adhesion (B2), containing 15 and 33 members, respectively. 4,21 Secretin subfamily members are characteristic...

2020年2月6日 · Class B G protein-coupled receptors (GPCRs) are important therapeutic targets for major diseases. Here, we present structures of peptide and Gs-bound pituitary adenylate cyclase-activating peptide, PAC1 receptor, and corticotropin-releasing …

The secretin-like (class B) family of G protein-coupled receptors (GPCRs) are key players in hormonal homeostasis and are interesting drug targets for the treatment of several metabolic disorders (type 2 diabetes, osteoporosis, obesity) and nervous system diseases (migraine, anxiety, depression).

The class B GPCRs bind the moderate length natural peptide ligands within a characteristic extracellular domain (ECD) that includes two central anti-parallel β-sheets and an amino-terminal α-helix connected by a series of loops and stabilized by three disulfide bonds.

Class B G protein-coupled receptors (GPCRs) are important therapeutic targets for major diseases. Here, we present structures of peptide and Gs-bound pituitary adenylate cyclase-activating peptide, PAC1 receptor, and corticotropin-releasing factor (CRF), (CRF1) receptor.

2024年2月8日 · Class B1 G protein-coupled receptors (GPCRs) respond to physiologically important peptide hormones and contribute to bone and energy homeostasis, vascular and lymphatic growth and tone, and immune function among other key roles.