title: Pharmacoperones: a new therapeutic approach for diseases caused by misfolded G protein-coupled receptors.
abstract: G Protein-coupled receptors (GPCRs) are cell membrane proteins that recognize specific chemical signals such as drugs and hormones and transduce these signals into cellular responses by activating G-proteins. As is the case for all newly synthesized proteins, GPCRs are subjected to conformational scrutiny at the endoplasmic reticulum prior to processing and trafficking to the cell surface membrane. Because of this stringent quality control screening mechanism, mutations that result in protein misfolding frequently lead to retention in the endoplasmic reticulum, aggregation or other misrouting and, eventually, to disease. This article reviews some patents and new therapeutic opportunities based on the misfolding and retention of otherwise functional GPCRs that represent promising approaches to correct conformational abnormalities leading to distinct disease states.
authors.affiliation: Research Unit in Reproductive Medicine, Hospital de Ginecobstetricia Luis Castelazo Ayala, Instituto Mexicano del Seguro Social, Av. Rio Magdalena 289, 60. piso, Col. Tizapan San Angel, C.P. 01090, Mexico D.F., Mexico. aulloaa@servidor.unam.mx
authors.forename: Alfredo
authors.initials: A
authors.lastname: Ulloa-Aguirre
authors.forename: P
authors.initials: P
authors.lastname: Michael Conn
mesh_terms: D000818:Animals; D004721:Endoplasmic Reticulum / Q000378:metabolism; D006801:Humans; D008954:Models, Biological; D018832:Molecular Chaperones / Q000494:pharmacology* / Q000627:therapeutic use*; D058990:Molecular Targeted Therapy / Q000639:trends*; D009154:Mutation; D017510:Protein Folding / Q000187:drug effects*; D021381:Protein Transport / Q000187:drug effects; D043562:Receptors, G-Protein-Coupled / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism*; D011966:Receptors, LHRH / Q000235:genetics / Q000378:metabolism
chemical_list: D018832:Molecular Chaperones; D043562:Receptors, G-Protein-Coupled; D011966:Receptors, LHRH
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