title: G protein-coupled receptor transactivation: from molecules to mice.
abstract: G protein-coupled receptors (GPCRs) mediate a diverse range of physiological functions via activation of complex signaling systems. Organization of GPCRs in to dimers and oligomers provides a mechanism for both signal diversity and specificity in cellular responses, yet our understanding of the physiological significance of dimerization, particularly homodimerization, has not been forthcoming. This chapter will describe how we have investigated the physiological importance of GPCR homodimerization, using the luteinizing hormone/chorionic gonadotropin receptor as a model GPCR. Using transactivation as a mode of assessing receptor dimerization, we describe our cellular system and functional assays for assessment of transactivation in vitro and detail our strategy for generating a mouse model to assess GPCR transactivation in vivo.
authors.affiliation: Department of Surgery and Cancer, Institute of Reproductive and Developmental Biology, Imperial College London, London, United Kingdom.
authors.forename: Kim C
authors.initials: KC
authors.lastname: Jonas
authors.forename: Adolfo
authors.initials: A
authors.lastname: Rivero-Müller
authors.forename: Ilpo T
authors.initials: IT
authors.lastname: Huhtaniemi
authors.forename: Aylin C
authors.initials: AC
authors.lastname: Hanyaloglu
mesh_terms: D000818:Animals; D022202:Chromosomes, Artificial, Bacterial; D004622:Embryo, Mammalian; D005260:Female; D005298:Fertility / Q000235:genetics*; D005455:Fluorescent Antibody Technique; D017930:Genes, Reporter; D057809:HEK293 Cells; D006801:Humans; D008156:Luciferases / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D008297:Male; D051379:Mice; D008822:Mice, Transgenic; D009154:Mutation; D011485:Protein Binding; D020033:Protein Isoforms / Q000737:chemistry / Q000235:genetics / Q000378:metabolism; D055503:Protein Multimerization; D011974:Receptors, LH / Q000737:chemistry / Q000235:genetics / Q000378:metabolism*; D015398:Signal Transduction; D013737:Testis / Q000166:cytology / Q000196:embryology / Q000378:metabolism*; D015533:Transcriptional Activation; D014162:Transfection
chemical_list: D020033:Protein Isoforms; D011974:Receptors, LH; D008156:Luciferases
keywords: BAC; Dimer; GPCR; Gonadotropin; Luteinizing hormone; Mouse model; Reproduction; Signaling; Transactivation