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TRP Channels as Potential Drug Targets.
Annu Rev Pharmacol Toxicol. 2018 01 06; 58:309-330.AR

Abstract

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.

Authors+Show Affiliations

Hydra Biosciences, Cambridge, Massachusetts 02138, USA; email: mmoran@hydrabio.com.

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

28945977

Citation

Moran, Magdalene M.. "TRP Channels as Potential Drug Targets." Annual Review of Pharmacology and Toxicology, vol. 58, 2018, pp. 309-330.
Moran MM. TRP Channels as Potential Drug Targets. Annu Rev Pharmacol Toxicol. 2018;58:309-330.
Moran, M. M. (2018). TRP Channels as Potential Drug Targets. Annual Review of Pharmacology and Toxicology, 58, 309-330. https://doi.org/10.1146/annurev-pharmtox-010617-052832
Moran MM. TRP Channels as Potential Drug Targets. Annu Rev Pharmacol Toxicol. 2018 01 6;58:309-330. PubMed PMID: 28945977.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - TRP Channels as Potential Drug Targets. A1 - Moran,Magdalene M, Y1 - 2017/09/25/ PY - 2017/9/26/pubmed PY - 2019/6/22/medline PY - 2017/9/26/entrez KW - TRP channel KW - TRPA1 KW - TRPV4 KW - drug discovery KW - genetic disorders SP - 309 EP - 330 JF - Annual review of pharmacology and toxicology JO - Annu Rev Pharmacol Toxicol VL - 58 N2 - 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. SN - 1545-4304 UR - https://www.unboundmedicine.com/medline/citation/28945977/TRP_Channels_as_Potential_Drug_Targets_ L2 - https://arjournals.annualreviews.org/doi/10.1146/annurev-pharmtox-010617-052832?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -