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.

Human

The orphan receptor ChemR23 (also referred to as CMKLR1 or DEZ) is a G-protein coupled receptor (GPCR) with homology to neuropeptide and chemoattractant receptors. ChemR23 is also a Gαi-linked receptor expressed primarily by monocytes, MΦs, and plasmacytoid dendritic cells. CMKLR1 has been shown to be expressed by DC generated in vitro from monocytes, to mediate their migration to the proteolytically regulated chemoattractant chemerin, and CMKLR1 may be a key mediator of pDC recruitment from the blood into tissue sites enriched in active chemerin.

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.

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

The GPR68 is a proton-sensing receptor involved in pH homeostasis. A study revealed that in osteosarcoma cells and primary human osteoblast precursors which expression of GPR68 exhibit strong PH-dependent inositol phosphate formation.

Human

C-C chemokine receptor type 1 (CCR1) is a G protein-coupled receptor member of the CC chemokine subfamily of receptors. Following interaction with its specific chemokine ligands, like macrophage inflammatory protein 1 alpha (MIP-1 alpha), regulated on activation normal T expressed and secreted protein (RANTES), and monocyte chemoattractant protein 3 (MCP-3), it triggers the onset of a process known as chemotaxis. GenScript’s human CCR1-expressing stable subline is guaranteed to function properly in the calcium flux assay.

Human

Free fatty acid G protein coupled receptor family consists of four members and plays significant roles in nutrition regulation. GPR40 and GPR120 are activated by medium and long-chain FFAs, whereas GPR41 and GPR43 can be activated by short-chain FFAs. GPR40 is preferentially expressed in pancreatic beta-cells and mediates the majority of the effects of FFAs on insulin secretion. Researches show that GPR40 is a potential therapeutic target and plays an important role in the chain of events linking obesity and type2 diabetes.

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

The gene GPBRA1 encodes G protein-coupled bile acid receptor. Bile acid-binding induces its internalization, activation of extracellular signal-regulated kinase and intracellular cAMP production.

Human

GPR103 is known as an orphan G protein-coupled receptor with reported expression in brain, heart, kidney, adrenal gland, retina, and testis. GPR103 mRNA has been reported to be highly expressed in the superficial layers of the entire spinal cord and a high density of 26RFa binding sites was observed in the superficial layers of the dorsal horn. QRFP binds and activates the human GPR103, as well as mouse GPR103A and GPR103B, with nanomolar affinities in transfected cells. Therefore, the current experiments investigated the effects of QRFP administration in rats and the effects of a high fat diet on prepro-QRFP mRNA and GPR103 receptor mRNA levels. 26RFa and QRFP are endogenous ligands of GPR103. An immunohistochemical study revealed that GPR103-like immunoreactivity (LI) was observed in the superficial layers of spinal dorsal horn, that QRFP-LI was observed in the dorsal root ganglion and that intrathecal 26RFa suppressed the expression of Fos-LI induced by paw formalin injection in the superficial layers of the spinal dorsal horn.

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.