Molecular architecture of the vanilloid receptor -: Insights for drug design

被引：72

作者：

Ferrer-Montiel, A ^{[1
]}

García-Martínez, C ^{[1
]}

Morenilla-Palao, C ^{[1
]}

García-Sanz, N ^{[1
]}

Fernández-Carvajal, A ^{[1
]}

Fernández-Ballester, G ^{[1
]}

Planells-Cases, R ^{[1
]}

机构：

[1] Univ Miguel Hernandez, Inst Biol Mol & Celular, Ed Torregaitan, Alicante 03202, Spain

来源：

EUROPEAN JOURNAL OF BIOCHEMISTRY | 2004年 / 271卷 / 10期

关键词：

D O I：

10.1111/j.1432-1033.2004.04083.x

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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.

引用

页码：1820 / 1826

页数：7

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