LEADER 03028nam 2200409z- 450 001 9910220049403321 005 20231214132846.0 035 $a(CKB)3800000000216283 035 $a(oapen)https://directory.doabooks.org/handle/20.500.12854/56244 035 $a(EXLCZ)993800000000216283 100 $a20202102d2016 |y 0 101 0 $aeng 135 $aurmn|---annan 181 $ctxt$2rdacontent 182 $cc$2rdamedia 183 $acr$2rdacarrier 200 10$aThe Physiology and Pharmacology of Leucine-rich Repeat GPCRs 210 $cFrontiers Media SA$d2016 215 $a1 electronic resource (115 p.) 225 1 $aFrontiers Research Topics 311 $a2-88919-958-4 330 $aG protein-coupled receptors (GPCRs) represent a large and physiologically important class of cell surface receptors. There are approximately 750 known GPCRs present in the human genome that can be subdivided into general classes based upon sequence homology within their transmembrane domains. Therapeutically, GPCRs represent a fertile source for the development of therapies as they are a significant percentage of our current pharmacopeia. Among the three subclasses of GPCRs, the Class A (rhodopsin-like) receptors are by far the most prevalent and extensively studied. However, within the Class A receptors, sub-families of receptors can be distinguished based upon common sequence motifs within the transmembrane domains as well as extracellular and intracellular domains. One such family of Class A receptors is characterized by multiple leucine- rich repeats within their amino- terminal domains (the Leucine-rich Repeat family (LRR)). This family of GPCRs are best represented by the glycoprotein hormone receptors (LHR, FSHR and TSHR) which have been studied extensively but also includes receptors for the peptide hormone relaxin (RXFP1 and RXFP2 (RXFP2 also binds insulin-like peptide 3)) and three other receptors (LGR4, LGR5 and LGR6). LGR4-6 were, until recently, considered orphan receptors. However, emerging data have revealed that these proteins are the receptors for a family of growth factors called R-spondins. Over the last 20 years much has been learned about LRR receptors, including the development of synthetic agonists and antagonists, new insights into signaling (including signaling bias) and the physiological role these receptors play in regulating the function of many tissues. This topic will focus on what is known concerning the regulation of these receptors, their signaling pathways, functional consequences of activation and pharmacology. 610 $aLeucine- rich repeat 610 $aTSH 610 $aGPCR 610 $aR-spondin 610 $aFSH 610 $aPharmacology 610 $aLH 610 $aRelaxin 610 $aLRR 700 $aBrian J. Arey$4auth$01329502 702 $aJames A. Dias$4auth 906 $aBOOK 912 $a9910220049403321 996 $aThe Physiology and Pharmacology of Leucine-rich Repeat GPCRs$93039523 997 $aUNINA