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Antibodies to detect G protein-coupled receptors (GPCRs) from Abgent now available

GPCR
G protein-coupled receptors (GPCRs) are the largest family of transmembrane receptors and are responsible for the transduction of a diverse range of extracellular signals. The range of physiological processes mediated by GPCRs makes them one of the most important classes of proteins for drug discovery.

G protein-coupled receptors (GPCRs), also known as seven-transmembrane domain receptors, 7TM receptors, heptahelical receptors, serpentine receptor, and G protein-linked receptors (GPLR), constitute a large protein superfamily of receptors. They sense molecules outside of the cell and activate intracellular signal transduction pathways and, ultimately, cellular responses. They are called seven-transmembrane receptors because they pass through the cell membrane seven times (only known exceptions are the plant GPCRs).

GPCRs are found only in eukaryotes, including yeast and animals. The ligands that bind and activate these receptors include light-sensitive compounds, odors, pheromones, hormones, and neurotransmitters, and vary in size from small molecules to peptides to large proteins. Consquently, GPCRs are involved in a wide variety of physiologial processes and diseases, and are also the target of approximately 40 % of all modern medicinal drugs.[1,2]

There are two principal signal transduction pathways involving the G protein-coupled receptors: the cAMP signal pathway and the phosphatidylinositol signal pathway.[3] When a ligand binds to the GPCR it causes a conformational change in the GPCR, which allows it to act as a guanine nucleotide exchange factor (GEF). The GPCR can then activate an associated G-protein by exchanging its bound GDP for a GTP. The G-protein's α subunit, together with the bound GTP, can then dissociate from the β and γ subunits to further affect intracellular signaling proteins or target functional proteins directly depending on the α subunit type (Gαs, Gαi/o, Gαq/11, Gα12/13).[4]

In a current model, β-arrestins function as ligand-regulated scaffolds, linking GPCRs to nontraditional effector pathways [e.g., nonreceptor tyrosine kinases (TK), MAP kinases (MAPK), and E3 ubiquitin ligases]. Because β-arrestin binding precludes further heterotrimeric G protein coupling, these two signaling “states” of the receptor are mutually exclusive (see figure 1) .

Principle of GPCR signalling

Figure 1: Principle of GPCR signalling Provided by Abgent

The strength of the GPCR signal imparted to the cell by agonists is determined by the molecular parameters governing the direct activation of the receptor and the allosteric effect of the ligand on endogenous receptor af nity. This signal can then interact with other pathways in the cell and the total cellular response thus becomes the result of an amalgam of stimuli.

To investigate the stoichiometry of the GPCR signalling components in the cell and thereby the change of the nature of the cellular response, Abgent developed a series of spezialised antibodies. Same examples are shown in the list above. For further interesting products browse through all products.

ABIN Antigene Reactivity Hosts Application
ABIN1742041 Melanocortin 4 Receptor (MC4R) (N-Term), (AA 6-20), (Extracellular Loop) Human,Mouse (Murine),Rat (Rattus) Rabbit WB,IHC,ICC
ABIN1742043 Melanocortin 2 Receptor (Adrenocorticotropic Hormone) (MC2R) (1st Extracellular Loop), (AA 87-99) Rat (Rattus) Rabbit WB,IHC
ABIN1742101 Chemokine (C-X-C Motif) Receptor 4 (CXCR4) (N-Term), (AA 2-15), (Extracellular Loop) Human,Mouse (Murine),Rat (Rattus) Rabbit WB,IHC,FACS
ABIN1742103 Chemokine (C-X-C Motif) Receptor 2 (CXCR2) (N-Term), (AA 2-19), (Extracellular Loop) Human Rabbit WB,FACS
ABIN1742105 Chemokine (C-X-C Motif) Receptor 1 (CXCR1) (N-Term), (AA 2-16), (Extracellular Loop) Human Rabbit WB,FACS
ABIN1742113 Bradykinin Receptor B2 (BDKRB2) (C-Term), (AA 336-349), (Intracellular) Human,Mouse (Murine),Rat (Rattus) Rabbit WB,IHC
ABIN1742115 Bradykinin Receptor B1 (BDKRB1) (AA 243-257), (Intracellular), (Cys250Ser-Mutant) Mouse (Murine),Rat (Rattus) Rabbit WB,IHC
ABIN1742125 Alpha2C-Adrenoceptor (2nd Extracellular Loop), (AA 192-207), (Cys202Ser-Mutant) Rat (Rattus) Rabbit WB,IHC
ABIN1742127 Alpha2B-Adrenoceptor (2nd Extracellular Loop), (AA 160-174), (Cys169Ser-Mutant) Rat (Rattus) Rabbit WB,IHC
ABIN1742129 Alpha2A-Adrenoceptor (N-Term), (AA 7-20), (Extracellular Loop) Mouse (Murine),Rat (Rattus) Rabbit WB
ABIN1742131 Alpha1D-Adrenoceptor (3rd Extracellular Loop), (AA 231-245), (Cys240Ser-Mutant) Human,Mouse (Murine),Rat (Rattus) Rabbit WB,IHC,FACS
ABIN1742133 Alpha1B-Adrenoceptor (N-Term), (AA 21-35), (Extracellular Loop) Human,Rat (Rattus) Rabbit WB,ICC,FACS
ABIN1742139 Alpha1A-Adrenoceptor (2nd Extracellular Loop), (AA 171-183), (Cys176Ser-Mutant) Human,Rat (Rattus) Rabbit WB,IHC
ABIN1742141 A1 Adenosine Receptor (AA 213-229), (Intracellular) Human,Mouse (Murine),Rat (Rattus) Rabbit WB,IHC,ICC
ABIN1742143 Adenosine Receptor A3 (ADORA3) (AA 216-230), (Intracellular) Human,Rat (Rattus) Rabbit WB,IHC,ICC
ABIN1742145 Adenosine Receptor A2b (ADORA2B) (2nd Extracellular Loop), (AA 147-166), (Cys154Ser-Mutant) Human,Mouse (Murine),Rat (Rattus) Rabbit WB,IHC
ABIN1742147 A2A Adenosine Receptor (AA 201-215), (Intracellular) Human,Mouse (Murine),Rat (Rattus) Rabbit WB,IHC
ABIN1742173 Angiotensin II Receptor, Type 1 (AGTR1) (N-Term), (AA 4-18), (Extracellular Loop) Human,Mouse (Murine),Rat (Rattus) Rabbit WB,IHC,ICC,FACS

References:

1 Filmore D (2004). "It’s a GPCR world". Modern Drug Discovery (American Chemical Society) 2004 (November): 24–28.

2 Overington JP, Al-Lazikani B, Hopkins AL (December 2006). "How many drug targets are there?". Nat Rev Drug Discov 5 (12): 993–6. PMID 17139284.

3 Gilman AG (1987). "G proteins: transducers of receptor-generated signals". Annu. Rev. Biochem. 56: 615–49. PMID 3113327.

4 Wettschureck N, Offermanns S (October 2005). "Mammalian G proteins and their cell type specific functions". Physiol. Rev. 85 (4): 1159–204. PMID 16183910.