TRP Channels as Potential Drug Targets

被引：168

作者：

Moran, Magdalene M. ^{[1
]}

机构：

[1] Hydra Biosci, Cambridge, MA 02138 USA

来源：

ANNUAL REVIEW OF PHARMACOLOGY AND TOXICOLOGY, VOL 58 | 2018年 / 58卷

关键词：

TRP channel; drug discovery; TRPA1; TRPV4; genetic disorders; POLYCYSTIC KIDNEY-DISEASE; FOCAL SEGMENTAL GLOMERULOSCLEROSIS; MUCOLIPIDOSIS TYPE-IV; OF-FUNCTION MUTATION; SPINAL MUSCULAR-ATROPHY; INDUCED LUNG INJURY; ION-CHANNEL; SENSORY NEURONS; CAPSAICIN RECEPTOR; ATOPIC-DERMATITIS;

D O I：

10.1146/annurev-pharmtox-010617-052832

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The transient receptor potential (TRP) superfamily of channels comprises a diverse group of cation channels. Four TRP channel subunits coassemble to form functional homo-or heterotetramers that pass sodium, calcium, or both in the inward direction. Modulating TRP channel activity provides an important way to impact cellular function by regulating both membrane excitability and intracellular calcium levels. The import of these channels is underscored by the number of genetic diseases caused when they are mutated: Skeletal, skin, sensory, ocular, cardiac, and neuronal disturbances all arise from aberrant TRP function. Not surprisingly, there has been significant pharmaceutical interest in targeting these fascinating channels. Compounds that modulate TRP vanilloid 1 (TRPV1), TRPV3, TRPV4, TRP ankyrin 1 (TRPA1), and TRP melastatin 8 (TRPM8) have all entered clinical trials. The goal of this review is to familiarize the readers with the rationale behind the pursuit of these channels in drug discovery and the status of those efforts.

引用

页码：309 / 329

页数：21

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