Polymodal Transient Receptor Potential Vanilloid Type 1 Nocisensor: Structure, Modulators, and Therapeutic Applications

Minghua Cui, Vijayakumar Gosu, Shaherin Basith, Sunhye Hong, Sun Choi

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

38 Scopus citations


Transient receptor potential (TRP) channels belong to a superfamily of sensory-related ion channels responding to a wide variety of thermal, mechanical, or chemical stimuli. In an attempt to comprehend the piquancy and pain mechanism of the archetypal vanilloids, transient receptor potential vanilloid (TRPV) 1 was discovered. TRPV1, a well-established member of the TRP family, is implicated in a range of functions including inflammation, painful stimuli sensation, and mechanotransduction. TRPV1 channels are nonselective cation receptors that are gated by a broad array of noxious ligands. Such polymodal-sensor aspect makes the TRPV1 channel extremely versatile and important for its role in sensing burning pain. Besides ligands, TRPV1 signaling can also be modulated by lipids, secondary messengers, protein kinases, cytoskeleton, and several other proteins. Due to its central role in hyperalgesia transduction and inflammatory processes, it is considered as the primary pharmacological pain target. Moreover, understanding the structural and functional intricacies of the channel is indispensable for the therapeutic intervention of TRPV1 in pain and other pathological disorders. In this chapter, we seek to give a mechanistic outlook on the TRPV1 channel. Specifically, we will explore the TRPV1 structure, activation, modulation, ligands, and its therapeutic targeting. However, the major objective of this review is to highlight the fact that TRPV1 channel can be treated as an effective therapeutic target for treating several pain- and nonpain-related physiological and pathological states.

Original languageEnglish
Title of host publicationAdvances in Protein Chemistry and Structural Biology
EditorsRossen Donev
PublisherAcademic Press Inc.
Number of pages45
ISBN (Print)9780128048269
StatePublished - 2016

Publication series

NameAdvances in Protein Chemistry and Structural Biology
ISSN (Print)1876-1623
ISSN (Electronic)1876-1631

Bibliographical note

Funding Information:
This work was supported by the National Leading Research Laboratory (NLRL) program (2011-0028885) funded by the Ministry of Science, ICT & Future Planning (MSIP), and the National Research Foundation (NRF) of Korea.

Publisher Copyright:
© 2016 Elsevier Inc.


  • Agonist
  • Antagonist
  • Capsaicin
  • Hyperalgesia
  • Ion channel
  • Nociceptor
  • Pain
  • TRPV1
  • Vanilloid


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