PRED-GPCR: GPCR recognition and family classification server [PDF]
The vast cell-surface receptor family of G-protein coupled receptors (GPCRs) is the focus of both academic and pharmaceutical research due to their key role in cell physiology along with their amenability to drug intervention. As the data flow rate from the various genome and proteome projects continues to grow, so does the need for fast, automated and
Panagiotis K. Papasaikas +4 more
openaire +3 more sources
Accelerating GPCR Drug Discovery With Conformation-Stabilizing VHHs
The human genome encodes 850 G protein-coupled receptors (GPCRs), half of which are considered potential drug targets. GPCRs transduce extracellular stimuli into a plethora of vital physiological processes.
Toon Laeremans +10 more
doaj +1 more source
Molecular mechanism of Gαi activation by non-GPCR proteins with a Gα-Binding and Activating motif [PDF]
Heterotrimeric G proteins are quintessential signalling switches activated by nucleotide exchange on Gα. Although activation is predominantly carried out by G-protein-coupled receptors (GPCRs), non-receptor guanine-nucleotide exchange factors (GEFs) have
Baillie, George S. +14 more
core +1 more source
GPCRs in Autocrine and Paracrine Regulations
G protein-coupled receptors (GPCRs) constitute the largest superfamily of integral membrane protein receptors. As signal detectors, the several 100 known GPCRs are responsible for sensing the plethora of endogenous ligands that are critical for the ...
Lap Hang Tse +2 more
doaj +1 more source
The role of ECL2 in CGRP receptor activation: a combined modelling and experimental approach [PDF]
The calcitonin gene-related peptide (CGRP) receptor is a complex of a calcitonin receptor-like receptor (CLR), which is a family B G-protein-coupled receptor (GPCR) and receptor activity modifying protein 1.
Alex C. Conner +13 more
core +2 more sources
The Secretin GPCRs Descended from the Family of Adhesion GPCRs [PDF]
The Adhesion G-protein-coupled receptors (GPCRs) are the most complex gene family among GPCRs with large genomic size, multiple introns, and a fascinating flora of functional domains, though the evolutionary origin of this family has been obscure. Here we studied the evolution of all class B (7tm2)-related genes, including the Adhesion, Secretin, and ...
Karl J V, Nordström +4 more
openaire +2 more sources
G protein-coupled receptors (GPCRs) are the most structurally diverse family of signaling proteins and regulate a variety of cell function. For most GPCRs, the cell surface is their functional destination where they are able to respond a wide range of ...
Xin Xu, Guangyu Wu
doaj +1 more source
Multiple Residues in the Second Extracellular Loop Are Critical for M3 Muscarinic Acetylcholine Receptor Activation [PDF]
Recent studies suggest that the second extracellular loop (o2 loop) of bovine rhodopsin and other class I G protein-coupled receptors (GPCRs) targeted by biogenic amine ligands folds deeply into the transmembrane receptor core where the binding of cis ...
Kim, Soo-Kyung +3 more
core +1 more source
Pathophysiology of GPCR Homo- and Heterodimerization: Special Emphasis on Somatostatin Receptors
G-protein coupled receptors (GPCRs) are cell surface proteins responsible for translating >80% of extracellular reception to intracellular signals.
Rishi K. Somvanshi, Ujendra Kumar
doaj +1 more source
Systematic analysis of primary sequence domain segments for the discrimination between class C GPCR subtypes [PDF]
G-protein-coupled receptors (GPCRs) are a large and diverse super-family of eukaryotic cell membrane proteins that play an important physiological role as transmitters of extracellular signal. In this paper, we investigate Class C, a member of this super-
Alquézar Mancho, René +3 more
core +2 more sources

