Endogenous Modulators of TRP Channels

Author(s): Enza Palazzo, Francesco Rossi, Vito de Novellis, Sabatino Maione

Journal Name: Current Topics in Medicinal Chemistry

Volume 13 , Issue 3 , 2013

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The transient receptor potential (TRP) superfamily consists of a large number of cation channels permeable to both monovalent and divalent cations. The 28 mammalian TRP channels can be divided into seven subfamilies: the TRPC (canonical), TRPV (vanilloid), TRPM (melastatin), TRPP (polycystin), TRPML (mucolipin), TRPN (no mechanopotential, NOMP) and the TRPA (ankyrin) groups. TRP channels are widely expressed in several cell types in every tissue and play a critical role in the regulation of various cell functions. Altogether these channels function as sensory transducers and detect chemical, thermal and mechanical stimuli. Endogenous substances acting on TRP channels can be released during the early stage of some pathological conditions. These substances can affect TRP channel functions and lead to the progression of diseases such as inflammation and chronic pain. For example, endogenous lipids, such as unsaturated fatty acids and their cyclooxygenase, lipoxygenase or epoxygenase related metabolites, were shown to modulate TRP channel activity by direct binding. Other lipidergic ligands include isoprene derivatives (e.g. diacylglycerol, lysophospholipids and resolvine) which play diverse activity on different TRP channels. This review focuses on lipidergic mediators which affect TRP channel activity. Opportunities to exploit TRP channels for novel therapeutic strategies will be discussed.

Keywords: Endogenous TRP ligands, neurogenic inflammation cascade, pain sensitization, TRPV1 desentization, peripheral sensory neurons

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Article Details

Year: 2013
Published on: 28 March, 2013
Page: [398 - 407]
Pages: 10
DOI: 10.2174/1568026611313030014

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