G蛋白偶联受体-2抗体说明书

This gene encodes a G protein-coupled receptor with selectivity for three chemokines, termed IP10(interferon-g-inducible 10 kDa protein), Mig (monokine induced by interferon-g) and I-TAC (interferon-inducible T cell a-chemoattractant). IP10, Mig and I-TAC belong to the structural subfamily of CXC chemokines, in which a single amino acid residue separates the first two of four highly conserved Cys residues. Binding of chemokines to this protein induces cellular responses that are involved in leukocyte traffic, most notably integrin activation, cytoskeletal changes and chemotactic migration. Inhibition by Bordetella pertussis toxin suggests that heterotrimeric G protein of the Gi-subclass couple to this protein. Signal transduction has not been further analyzed but may include the same enzymes that were identified in the signaling cascade induced by other chemokine receptors. As a consequence of chemokine-induced cellular desensitization(phosphorylation-dependent receptor internalization), cellular responses are typically rapid and short in duration. Cellular responsiveness is restored after dephosphorylation of intracellular receptors and subsequent recycling to the cell surface. This gene is prominently expressed in in vitro cultured effector/memory T cells, and in T cells present in many types of inflamed tissues. In addition, IP10, Mig and I-TAC are commonly produced by local cells in inflammatory lesion, suggesting that this gene and its chemokines participate in the recruitment of inflammatory cells. Therefore, this protein is a target for the development of small molecular weight antagonists, which may be used in the treatment of diverse inflammatory diseases. Multiple transcript variants encoding different isoforms have been found for this gene.
Function : Receptor for CXCL9, CXCL10 and CXCL11 and mediates the proliferation of human mesangial cells (HMC).
Isoform 2 is a receptor for CXCL4 and also mediates the inhibitory activities of CXCL9, CXCL10 and CXCL11 on the growth of human microvascular endothelial cells (HMVEC). Interaction with CXCL4 or CXCL10 leads to activation of the p38MAPK pathway and contributes to inhibition of angiogenesis. Overexpression in renal cancer cells down-regulates expression of the anti-apoptotic protein HMOX1 and promotes apoptosis.
Isoform 3 mediates the activity of CXCL11.
Subcellular Location : Cell membrane; Multi-pass membrane protein.
Tissue Specificity : Isoform 1 and isoform 2 are mainly expressed in heart, kidney, liver and skeletal muscle. Isoform 1 is also expressed in placenta.
Post-translational modifications : Sulfation on Tyr-27 and Tyr-29 is essential for CXCL10 binding and subsequent signal transduction induction.
N-glycosylated.
Similarity : Belongs to the G-protein coupled receptor 1 family.
Database links : UniProtKB/Swiss-Prot: P49682.2
G蛋白偶联受体CKR-L2（ G protein-coupled receptor-2 ）又称：又称G蛋白偶联受体9(GPR9)-是受体中最大的家族，大多数的细胞膜表面受体都是G蛋白偶联受体家族的成员。
G蛋白偶联受体是药物研发中最广泛应用的成功药靶，作用于G蛋白偶联受体的药物对疼痛、认知障碍、高血压、胃溃疡、鼻炎和哮喘等各类疾病具有良好的治疗作用。G-蛋白受体在目前临床上使用的约500种药物中，有30%以上以调节G蛋白偶联受体功能为靶标。