Introduction of GPR78
G-protein coupled receptor 78 (GPR78) is a protein that in humans is encoded by the GPR78 gene. Gene Ontology (GO) annotations associated with this gene include G-protein coupled receptor activity. An important paralog of this gene is GPR26. GPR78 is a member of the G protein-coupled receptor family. G protein-coupled receptors contain 7 transmembrane domains and transduce extracellular signals through heterotrimeric G proteins. GPR78 is currently considered to be an orphan receptor that displays a significant level of constitutive activity. The effects of GPR78 are mediated by G(s)-alpha protein that stimulates adenylate cyclase, leading to an elevation of intracellular cAMP.
|Basic Information of GPR78|
|Protein Name||G-protein coupled receptor 78|
|Organism||Homo sapiens (Human)|
Function of GPR78 Membrane Protein
GRP78 is a major endoplasmic reticulum chaperone with Ca2+ binding ability. It can also act as an ER stress signal conditioner. GPR78 is associated with diseases such as schizophrenia. Upregulation of GRP78 expression is related to several cancer types, such as urinary, digestive, breast, brain, respiratory systems, and osteosarcoma. The presence of GRP78 autoantibodies in the serum of cancer patients is often associated with a poor prognosis because GRP78 promotes tumor cell proliferation, survival, and metastasis by inhibiting ER stress-induced apoptosis. It has been reported that overexpression of GRP78 is associated with chemoresistance. In addition, it has been reported that GRP78 inhibitor therapy or GRP78 knockdown may enhance chemotherapy-induced apoptosis in most of the cancer types mentioned above.
Fig.1 The GPR78 gene. (Underwood, 2006)
Application of GPR78 Membrane Protein in Literature
The article reveals that CD24 antagonizes L-OHP-induced cytotoxicity and that GRP78 is involved in this process. The combination of compounds that suppress GRP78 may help to improve the effectiveness of L-OHP in the treatment of colorectal cancer.
The article reports that down-regulation of GRP78 via 17β-HSD7 inhibition enhances cell apoptosis in response to Letrozole. The results suggest that inhibition of 17β-HSD7 would be a complementary strategy to Letrozole by suppression of GRP78 in ER+ breast cancer.
The results suggest that the knockdown of GPR78 inhibited lung cancer cell metastasis in vivo. GPR78 may be used as a novel regulator for lung cancer metastasis and may serve as a potential drug target against metastatic human lung cancer.
Authors in this group measured the binding affinities between human GRP78 and two transmembrane UPR sensors, with or without the addition of an unfolded protein client. It shows that human GRP78 affinity towards its signaling partners Ire1α and PERK is differently modulated by an unfolded protein client.
This article reveals that Lacidipine could lower blood pressure and prevent left ventricular hypertrophy accompanied by inhibiting expression of GRP78 and CHOP in ERS.
GPR78 Preparation Options
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