TY - JOUR
T1 - Orphan G protein-coupled receptors (GPCRs)
T2 - Biological functions and potential drug targets
AU - Tang, Xiao Long
AU - Wang, Ying
AU - Li, Da Li
AU - Luo, Jian
AU - Liu, Ming Yao
PY - 2012/3
Y1 - 2012/3
N2 - The superfamily of G protein-coupled receptors (GPCRs) includes at least 800 seven-transmembrane receptors that participate in diverse physiological and pathological functions. GPCRs are the most successful targets of modern medicine, and approximately 36% of marketed pharmaceuticals target human GPCRs. However, the endogenous ligands of more than 140 GPCRs remain unidentified, leaving the natural functions of those GPCRs in doubt. These are the so-called orphan GPCRs, a great source of drug targets. This review focuses on the signaling transduction pathways of the adhesion GPCR family, the LGR subfamily, and the PSGR subfamily, and their potential functions in immunology, development, and cancers. In this review, we present the current approaches and difficulties of orphan GPCR deorphanization and characterization.
AB - The superfamily of G protein-coupled receptors (GPCRs) includes at least 800 seven-transmembrane receptors that participate in diverse physiological and pathological functions. GPCRs are the most successful targets of modern medicine, and approximately 36% of marketed pharmaceuticals target human GPCRs. However, the endogenous ligands of more than 140 GPCRs remain unidentified, leaving the natural functions of those GPCRs in doubt. These are the so-called orphan GPCRs, a great source of drug targets. This review focuses on the signaling transduction pathways of the adhesion GPCR family, the LGR subfamily, and the PSGR subfamily, and their potential functions in immunology, development, and cancers. In this review, we present the current approaches and difficulties of orphan GPCR deorphanization and characterization.
KW - G protein-coupled receptors
KW - Gpr48/Lgr4
KW - LGR subfamily
KW - PSGR
KW - adhesion GPCR family
KW - deorphanization
KW - orphan GPCR
UR - https://www.scopus.com/pages/publications/84863236424
U2 - 10.1038/aps.2011.210
DO - 10.1038/aps.2011.210
M3 - 文献综述
C2 - 22367282
AN - SCOPUS:84863236424
SN - 1671-4083
VL - 33
SP - 363
EP - 371
JO - Acta Pharmacologica Sinica
JF - Acta Pharmacologica Sinica
IS - 3
ER -
