Human

The protein encoded by this gene is a member of the G protein-coupled receptor family 1. It is also an integral plasma membrane protein that binds melanin-concentrating hormone. The encoded protein can inhibit cAMP accumulation and stimulate intracellular calcium flux, and is probably involved in the neuronal regulation of food consumption. Melanin-concentrating hormone (MCH) is an important neuropeptide hormone involved in multiple physiological processes. Peptide derivatives of MCH have been developed as tools to aid researches that involve potent radioligands, receptor selective agonists, and potent antagonists. These tools have been used to further understand the role of MCH's physiology primarily in rodents.

Recombinant CHO-K1 cells stably overexpress human G protein-coupled receptor 68 (GPR68) on the surface and contain high levels of G protein Gαi and Gαq to couple with the receptor in downstream signaling pathways.

The G-protein-coupled receptor (GPCR) superfamily represents one of the most important classes of drug targets. GPCRs are divided into subfamilies according to the kind of Gα protein to which they couple. There are Gαs-, Gαi-, and Gαq-coupled receptors. Gαs proteins can activate adenyl cyclase and increase the intracellular concentration of cAMP. Here we employ both 3xCRE element and firefly luciferase as reporters to establish host cell lines that can be used for research involving GPCRs, particularly Gs-coupled GPCRs. The cell line demonstrates an approximately 30-fold dynamic range in the luciferase assay, providing a good screening window that is suitable for screening of GPCR agonist and antagonist.

Human

Lysophosphatidic acid (LPA), a bioactive lipid produced by several cell types including postmitotic neurons and activated platelets, is thought to be involved in various biological processes, including brain development. Three cognate G-protein coupled receptors encoded by lpa(1)/lp(A1)/Edg-2/Gpcr26, lpa(2)/lp(A2)/Edg-4, and lpa(3)/lp(A3)/Edg-7 mediate the cellular effects of LPA. However, many LPA-induced responses, including phospholipase C activation, Ca2+ mobilization, adenylyl cyclase activation, proliferation, JNK activation, AKT activation, and stress fiber formation, were absent or severely reduced in embryonic fibroblasts derived from lpa(1)(-/-) lpa(2)(-/-) mice. The lysophosphatidic acid receptor LPA2 or endothelial differentiation, G-protein coupled receptor 4(EDG-4) is expressed most abundantly in testes and peripheral blood leukocytes. It is reported to be a distinctive functional marker for ovarian carcinoma.

Human

CHO-K1/Gqi5 is a CHO-K1 cell line stably expressing the chimeric Gqi5 alpha subunit protein which a chimeric Gq protein instead of the last five carboxyl-terminal amino acids from Gi. It is used as a host cell for transfection expression of Gi/o-coupled receptors, the constitutively expressed Gqi5 protein in the cells allows many transfected receptors which normally inhibit the cAMP pathway, to couple to Gq signal transduction and mobilize intracellular calcium. The cell line carries the hygromycin B resistance gene and is resistant to hygromycin B.

Human

The neuropeptide galanin elicits a range of biological effects by interacting with specific G-protein-coupled receptors. Galanin receptors are seven-transmembrane proteins that have been shown to activate a variety of intracellular second-messenger pathways. GALR1 inhibits adenylyl cyclase via a G protein of the Gi/Go family. GALR1 is widely expressed in the brain, spinal cord, and peripheral sites including small intestine and heart.

Human

FFA2 (GPR43) is a 330-amino acid G-protein coupled receptor that binds to fatty acid. FFA2 is highly selective expressed in leukocytes, which suggests a role in the recruitment of these cell populations toward sites of bacterial infection.

Histamine is a ubiquitous messenger molecule released from mast cells, enterochromaffin-like cells, and neurons. Its various actions are mediated by histamine receptors H1, H2, H3, and H4. Specifically, the histamine receptor H2 belongs to the rhodopsin-like family of G protein-coupled receptors. As an integral membrane protein, it stimulates gastric acid secretion and regulates gastrointestinal motility and intestinal secretion and is thought to be involved in regulating cell growth and differentiation.

Human

The motilin receptor (MTLR) represents a clinically useful pharmacological target, as agonists binding to the MTLR have gastroprokinetic properties. Motilin is a 22 amino acid peptide that potently stimulates gastrointestinal contractility. The biological effects of motilin are mediated by a Gq-coupled seven transmembrane protein, currently termed motilin receptor (MR) that shares significant sequence similarity with the ghrelin receptor. The motilin receptor is also activated by the antibiotic erythromycin; this interaction appears to mediate some of the gastrointestinal side effects of erythromycin. Although motilides (non-antibiotic derivatives of erythromycin) such as ABT-229 have been investigated for treatment of diabetic gastroporesis, the effectiveness has been limited by tachyphylaxis (decreased response to ligand) resulting from receptor downregulation. Agonists of the motilin receptor with reduced densensitization activity remain a potential treatment for disorders of gastric motility.

Human

Neuromedin U receptor 1 (NMUR1) is a member of G-protein coupled receptor family A and is the most abundant in peripheral tissue, particularly in small intestines and stomach. This protein is a receptor for Neuromedin U (NMU-25). The first biological activity ascribed to NmU was smooth muscle contraction. Neuromedin U has also been reported to increase arterial blood pressure and modify ion transport in the intestinal tract. Finally, NmU injected subcutaneously into rats has been reported to result in a short term increase in circulating ACTH levels and a long term increase in serum corticosterone levels, suggesting a role in regulation of the hypothalamo-pituitary-adrenal axis.

Human

Neurotensin receptor 1 (NTS1) is a member of G-protein coupled receptor family A and is a receptor for Neurotensin (NT). Neurotensin (NT) exerts its intracellular effect by interacting with 3 different receptors. Two of these receptors (NTR1 and NTR2) belong to the G protein-coupled receptor family, whereas the third one (NTR3) is a type I receptor with a single transmembrane domain. The NTS1 is expressed in CNS such as cerebral cortex, basal ganglia, limbic areas, vestibular system, and esophageal smooth muscle.

Mouse

Programmed cell death protein 1, also known as PD-1 and CD279 (cluster of differentiation 279), is a protein that in humans is encoded by the PDCD1 gene.PD-1, functioning as an immune checkpoint, plays an important role in down regulating the immune system by preventing the activation of T-cells, which in turn reduces autoimmunity and promotes self-tolerance. The inhibitory effect of PD-1 is accomplished through a dual mechanism of promoting apoptosis (programmed cell death) in antigen specific T-cells in lymph nodes while simultaneously reducing apoptosis in regulatory T cells (suppressor T cells).