title: Molecular architecture of the vanilloid receptor. Insights for drug design.
abstract: The transient receptor potential channel vanilloid receptor subunit 1 (TRPV1) is a molecular integrator of physical and chemical stimuli in the peripheral nociceptor terminals. TRPV1 is an ionotropic channel that plays a critical role in both thermal nociception and inflammatory hyperalgesia. Structure-function relationships are providing fundamental insights of the modular architecture of this neuronal receptor. As a result, the molecular determinants that endow TRPV1 with its physiological properties, namely activation by heat, potentiation by extracellular acidic pH, and interaction with vanilloid-like compounds, as well as its permeation properties are being unveiled. This information can now be used to build up molecular models for the protein which, upon experimental validation, could be used as tools to thrust the target-oriented design of druggable TRPV1 ligands.
authors.affiliation: Instituto de Biología Molecular y Celular, Universidad Miguel Hernández, Alicante, Spain. aferrer@umh.es
authors.forename: Antonio
authors.initials: A
authors.lastname: Ferrer-Montiel
authors.forename: Carolina
authors.initials: C
authors.lastname: García-Martínez
authors.forename: Cruz
authors.initials: C
authors.lastname: Morenilla-Palao
authors.forename: Nuria
authors.initials: N
authors.lastname: García-Sanz
authors.forename: Asia
authors.initials: A
authors.lastname: Fernández-Carvajal
authors.forename: Gregorio
authors.initials: G
authors.lastname: Fernández-Ballester
authors.forename: Rosa
authors.initials: R
authors.lastname: Planells-Cases
mesh_terms: D000700:Analgesics / Q000737:chemistry / Q000494:pharmacology; D000818:Animals; D015195:Drug Design; D006801:Humans; D008958:Models, Molecular; D011955:Receptors, Drug / Q000737:chemistry* / Q000502:physiology*; D013329:Structure-Activity Relationship
chemical_list: D000700:Analgesics; D011955:Receptors, Drug