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Transient receptor potential (TRP) channels: a clinical perspective.
Br J Pharmacol. 2014 May; 171(10):2474-507.BJ

Abstract

Transient receptor potential (TRP) channels are important mediators of sensory signals with marked effects on cellular functions and signalling pathways. Indeed, mutations in genes encoding TRP channels are the cause of several inherited diseases in humans (the so-called 'TRP channelopathies') that affect the cardiovascular, renal, skeletal and nervous systems. TRP channels are also promising targets for drug discovery. The initial focus of research was on TRP channels that are expressed on nociceptive neurons. Indeed, a number of potent, small-molecule TRPV1, TRPV3 and TRPA1 antagonists have already entered clinical trials as novel analgesic agents. There has been a recent upsurge in the amount of work that expands TRP channel drug discovery efforts into new disease areas such as asthma, cancer, anxiety, cardiac hypertrophy, as well as obesity and metabolic disorders. A better understanding of TRP channel functions in health and disease should lead to the discovery of first-in-class drugs for these intractable diseases. With this review, we hope to capture the current state of this rapidly expanding and changing field.

Authors+Show Affiliations

Discovery Research Alliance, Ono Pharmaceutical Co. Ltd, Osaka, Japan.No affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

24102319

Citation

Kaneko, Yosuke, and Arpad Szallasi. "Transient Receptor Potential (TRP) Channels: a Clinical Perspective." British Journal of Pharmacology, vol. 171, no. 10, 2014, pp. 2474-507.
Kaneko Y, Szallasi A. Transient receptor potential (TRP) channels: a clinical perspective. Br J Pharmacol. 2014;171(10):2474-507.
Kaneko, Y., & Szallasi, A. (2014). Transient receptor potential (TRP) channels: a clinical perspective. British Journal of Pharmacology, 171(10), 2474-507. https://doi.org/10.1111/bph.12414
Kaneko Y, Szallasi A. Transient Receptor Potential (TRP) Channels: a Clinical Perspective. Br J Pharmacol. 2014;171(10):2474-507. PubMed PMID: 24102319.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Transient receptor potential (TRP) channels: a clinical perspective. AU - Kaneko,Yosuke, AU - Szallasi,Arpad, PY - 2013/07/09/received PY - 2013/08/28/revised PY - 2013/08/31/accepted PY - 2013/10/10/entrez PY - 2013/10/10/pubmed PY - 2014/12/17/medline KW - TRP channels KW - TRPA1 KW - TRPCs KW - TRPM8 KW - TRPV1 KW - TRPV3 KW - TRPV4 KW - bladder disorders KW - cancer KW - pain KW - respiratory disorders SP - 2474 EP - 507 JF - British journal of pharmacology JO - Br J Pharmacol VL - 171 IS - 10 N2 - Transient receptor potential (TRP) channels are important mediators of sensory signals with marked effects on cellular functions and signalling pathways. Indeed, mutations in genes encoding TRP channels are the cause of several inherited diseases in humans (the so-called 'TRP channelopathies') that affect the cardiovascular, renal, skeletal and nervous systems. TRP channels are also promising targets for drug discovery. The initial focus of research was on TRP channels that are expressed on nociceptive neurons. Indeed, a number of potent, small-molecule TRPV1, TRPV3 and TRPA1 antagonists have already entered clinical trials as novel analgesic agents. There has been a recent upsurge in the amount of work that expands TRP channel drug discovery efforts into new disease areas such as asthma, cancer, anxiety, cardiac hypertrophy, as well as obesity and metabolic disorders. A better understanding of TRP channel functions in health and disease should lead to the discovery of first-in-class drugs for these intractable diseases. With this review, we hope to capture the current state of this rapidly expanding and changing field. SN - 1476-5381 UR - https://www.unboundmedicine.com/medline/citation/24102319/Transient_receptor_potential__TRP__channels:_a_clinical_perspective_ L2 - https://doi.org/10.1111/bph.12414 DB - PRIME DP - Unbound Medicine ER -