Molecular architecture of the vanilloid receptor. Insights for drug design
| Autor: | Antonio Ferrer-Montiel, Asia Fernández-Carvajal, Rosa Planells-Cases, Cruz Morenilla-Palao, Gregorio Fernández-Ballester, Carolina García-Martínez, Nuria García-Sanz |
|---|---|
| Rok vydání: | 2004 |
| Předmět: |
Models
Molecular Analgesics Molecular model Chemistry Receptors Drug musculoskeletal neural and ocular physiology TRPV1 Druggability Biochemistry Structure-Activity Relationship Transient receptor potential channel nervous system Drug Design Hyperalgesia Nociceptor Biophysics medicine Animals Humans lipids (amino acids peptides and proteins) medicine.symptom Receptor Ionotropic effect |
| Zdroj: | European Journal of Biochemistry. 271:1820-1826 |
| ISSN: | 1432-1033 0014-2956 |
| DOI: | 10.1111/j.1432-1033.2004.04083.x |
| Popis: | 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. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|