G protein-coupled receptors (GPCRs) are integral membrane proteins that act as cell surface receptors
GPCRs are the largest and most diverse group of membrane receptors in eukaryotes, and the largest protein family in the human genome, with around 800 members. GPCRs are also implicated in many diseases, such as cancer, metabolic diseases, and cardiac and inflammatory disorders. Because of this, they are popular targets for drug screening and development, with estimates suggesting that GPCRs are targets for about half of all drugs currently on the market. GPCRs are attractive targets because of their seven-transmembrane protein structure and the diverse downstream signaling pathways they can trigger. These pathways can include calcium mobilization, phosphorylation, or cyclic adenosines-3,5-monophosphate (cAMP).
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Novel interaction between neurotrophic factor-α1/carboxypeptidase E and serotonin receptor, 5-HTR1E, protects human neurons against oxidative/neuroexcitotoxic stress via β-arrestin/ERK signaling. Sharma, Vinay Kumar / Yang, Xuyu / Kim, Soo-Kyung / Mafi, Amirhossein / Saiz-Sanchez, Daniel / Villanueva-Anguita, Patricia / Xiao, Lan / Inoue, Asuka / Goddard, William A / Loh, Y Peng Published in Cellular and Molecular Life Sciences, 2021 Dec, using RC210240 |
PubMed: 34966948 |
Luciferase Reporter Assay System for Deciphering GPCR Pathways. Cheng, Zhijie / Garvin, Denise / Paguio, Aileen / Stecha, Pete / Wood, Keith / Fan, Frank Published in Cellular and Molecular Life Sciences, 2010 Dec |
PubMed: 21331312 |
GPR171 expression enhances proliferation and metastasis of lung cancer cells Dho, So Hee / Lee, Kwang-Pyo / Jeong, Dongjun / Kim, Chang-Jin / Chung, Kyung-Sook / Kim, Ji Young / Park, Bum-Chan / Park, Sung Sup / Kim, Seon-Young / Kwon, Ki-Sun Published in Cellular and Molecular Life Sciences, 2016 Feb |
PubMed: 26760963 |
GPCR Effector Pathways
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