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Editorial
. 2017 Jul 6;10(3):64.
doi: 10.3390/ph10030064.

Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts

Susan Huang  1 , Arpad Szallasi  2
Affiliations
Editorial

Transient Receptor Potential (TRP) Channels in Drug Discovery: Old Concepts & New Thoughts

Susan Huang et al. Pharmaceuticals (Basel). .

Abstract

2017 marks the 20th anniversary of the molecular cloning by David Julius and colleagues (1997) of the long sought-after capsaicin receptor, now known as TRPV1 (Transient Receptor Potential Vanilloid 1) [1]. This seminal discovery has opened up a "hot" new field of basic research and launched drug discovery efforts into the large family (by the latest count 28 mammalian members, 27 in humans) of TRP ion channels [2]. Indeed, it took less than a decade for the first potent, small molecule TRPV1 antagonists to enter phase 1 clinical trials [3]. Yet, despite the large amount of resources that has been invested in TRPV1 research, there are currently no TRPV1-targeted drugs in phase 3 clinical trials. In this special issue of Pharmaceuticals, we aim to capture the progress in the TRP channel field over the past twenty years, with 15 articles covering a variety of TRP channels and potential relevant disease states and applications.

Keywords: Drug Discovery; TRP; Transient Receptor Potential Channels.

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Conflict of interest statement

The authors declare no conflict of interest.

References

    1. Caterina M.J., Schumacher M.A., Tominaga M., Rosen T.A., Levine J.D., Julius D. The capsaicin receptor: A heat-activated ion channel in the pain pathway. Nature. 1997;389:816–824. - PubMed
    1. Nilius B., Szallasi A. Transient Receptor Potential channels as drug targets: From the science of basic science to the art of medicine. Pharmacol. Rev. 2014;66:676–814. doi: 10.1124/pr.113.008268. - DOI - PubMed
    1. Szallasi A., Cortright D.N., Blum C.A., Eid S.R. The vanilloid receptor TRPV1: 10 years from channel cloning to antagonist proof-of-concept. Nat. Rev. Drug Discov. 2007;6:357–372. doi: 10.1038/nrd2280. - DOI - PubMed
    1. Mickle A.D., Shephens A.J., Mohapatra D.P. Nociceptive TRP channels: Sensory detectors and transducers in multiple pain pathologies. Pharmaceuticals. 2016;9:72–76. doi: 10.3390/ph9040072. - DOI - PMC - PubMed
    1. Chung M.-K., Campbell J.N. Use of capsaicin to treat pain: Mechanistic and therapeutic considerations. Pharmaceuticals. 2016;9:66. doi: 10.3390/ph9040066. - DOI - PMC - PubMed

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