Resetting of G-protein-coupled receptors (GPCRs) from their active state back to their biologically inert ground state is an integral part of GPCR signaling. This "on-off" GPCR cycle is regulated by reversible phosphorylation. Retinal rod and cone photoreceptors arguably represent the best-understood example of such GPCR signaling. Their visual pigments (opsins) are activated by light, transduc...

G Proteins couple receptors for diverse extracellular signals to effecters such as enzymes and ion channels. The majority of polypeptide hormones, all monoamine neurotransmitters, PGs, and even extracellular Ca’+ signal their target cells through G protein-coupled receptors (GPCR). In the past few years, mutations in G proteins and GPCR have been identified as the causes of several endocrine di...

The interaction of an agonist-bound G-protein-coupled receptor (GPCR) with its cognate G-protein initiates a sequence of experimentally quantifiable changes in both the GPCR and G-protein. These include the release of GDP from G(alpha), the formation of a ternary complex between the nucleotide-free G-protein and the GPCR, which has a high affinity for agonist, followed by the binding of GTP to ...

Agonist-induced endocytosis is a key regulatory mechanism for controlling the responsiveness of cell by changing density surface receptors. In addition to role in signal termination, endocytosed G protein–coupled receptors (GPCRs) have been found from intracellular compartments cell. Arrestins are generally believed be master regulators GPCR binding both phosphorylated and adaptor protein 2 (AP...

In human physiology, cholesterol plays an imperative part in membrane cells which regulates the function of G-protein-coupled receptors (GPCR) family. Cholesterol is individual type lipid structure and about 90 percent cellular present at plasma region. Recognition/interaction Amino acid Consensus (CRAC) sequence, generally referred as CRAC (L/V)-X1−5-(Y)-X1−5-(K/R) new cholesterol-binding doma...

Most evidence indicates that, as for family C G protein-coupled receptors (GPCRs), family A GPCRs form homo- and heteromers. Homodimers seem to be a predominant species, with potential dynamic formation of higher-order oligomers, particularly tetramers. Although monomeric GPCRs can activate G proteins, the pentameric structure constituted by one GPCR homodimer and one heterotrimeric G protein m...

Recent realization that plasma membrane G protein-coupled receptors (GPCRs) may translocate and establish ligand-responsive signaling complexes in other cellular structures has motivated studies of site-specific differences in transductional pathways. GPCRs and their ligands may signal transcription and other nuclear events by two basic mechanisms. The first consists of GPCR-complex activation ...

Abstract Background Roughly one third of cases chronic heart failure (HF) are caused by genetic predisposition, metabolic stress and cardiac inflammation. Animal studies suggest that heart-reactive autoantibodies, most notably those directed against G-protein-coupled receptors (GPCR), could also play a pathogenetic role in the disease. However, so far, causal link between humoral GPCR-autoimmun...

G protein-coupled receptors (GPCRs) are cell-surface receptors that regulate neurotransmission, cardiovascular function, metabolic homeostasis, and many other physiological processes. Due to their central role in human physiology, these receptors are among the most important targets of therapeutic drugs, and are they among the most extensively studied integral membrane proteins. To better under...