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Updated: May 13, 2026

Purification of Endogenous Drosophila Transient Receptor Potential Channels
Published on: December 28, 2021
Endogenous modulators of TRP channels
Enza Palazzo1, Francesco Rossi, Vito de Novellis
1Department of Experimental Medicine, Section of Pharmacology L. Donatelli, Faculty of Medicine and Surgery, Second University of Naples, Via Costantinopoli, 16 80138 Naples, Italy. enza.palazzo@unina2.it
Abstract:
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.
Insights
Transient Receptor Potential (TRP) channels, crucial for sensing stimuli, are modulated by lipid mediators. This review explores how these lipidergic compounds affect TRP channel activity and disease progression.
Area of Science:
- Physiology
- Molecular Biology
- Pharmacology
Background:
- Transient Receptor Potential (TRP) channels are a superfamily of cation channels involved in sensing diverse stimuli.
- These channels are widely expressed and play critical roles in cellular functions and sensory transduction.
- Dysregulation of TRP channel activity is implicated in pathological conditions like inflammation and chronic pain.
Purpose of the Study:
- To review the role of lipidergic mediators in modulating TRP channel activity.
- To explore the impact of these lipid-based compounds on TRP channel function in health and disease.
- To discuss the therapeutic potential of targeting TRP channels with lipidergic modulators.
Main Methods:
- Literature review focusing on studies investigating TRP channels and lipidergic mediators.
- Analysis of research on endogenous lipids and their metabolites acting on TRP channels.
- Synthesis of information regarding the diverse effects of lipidergic ligands on various TRP channel subfamilies.
Main Results:
- Endogenous lipids, including fatty acids and their metabolites, directly bind to and modulate TRP channel activity.
- Various lipidergic ligands, such as diacylglycerol and lysophospholipids, exhibit diverse effects on different TRP channel subfamilies.
- TRP channel modulation by lipidergic substances is linked to the progression of inflammatory and pain-related diseases.
Conclusions:
- Lipidergic mediators are significant regulators of TRP channel function.
- Understanding these interactions provides insights into disease mechanisms.
- Targeting TRP channels with lipidergic compounds presents promising therapeutic opportunities for inflammatory and pain conditions.
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