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Published on: February 17, 2017
Transient receptor potential (TRP) channels: a clinical perspective
Yosuke Kaneko1, Arpad Szallasi
1Discovery Research Alliance, Ono Pharmaceutical Co. Ltd, Osaka, Japan.
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.
Insights
Transient receptor potential (TRP) channels mediate sensory signals and are implicated in diseases. TRP channel drug discovery is expanding into new therapeutic areas beyond pain relief.
Area of Science:
- Molecular biology
- Pharmacology
- Genetics
Background:
- Transient receptor potential (TRP) channels are crucial for sensory signaling and cellular functions.
- Mutations in TRP channel genes cause inherited diseases known as TRP channelopathies, affecting multiple organ systems.
- TRP channels represent significant targets for novel drug development.
Purpose of the Study:
- To review the current state of TRP channel research in drug discovery.
- To highlight the expansion of TRP channel drug discovery into new disease areas.
- To underscore the potential of TRP channels for developing first-in-class therapeutics.
Main Methods:
- Literature review of TRP channel research.
- Analysis of current drug discovery efforts and clinical trials.
- Exploration of TRP channel involvement in various diseases.
Main Results:
- TRP channels are implicated in cardiovascular, renal, skeletal, and nervous system disorders.
- TRP channel antagonists (e.g., TRPV1, TRPV3, TRPA1) are in clinical trials for pain management.
- Drug discovery efforts are expanding to include asthma, cancer, anxiety, cardiac hypertrophy, obesity, and metabolic disorders.
Conclusions:
- TRP channels are versatile targets with potential for treating a wide range of diseases.
- Understanding TRP channel function is key to developing innovative treatments.
- The field of TRP channel drug discovery is rapidly evolving, offering promising therapeutic avenues.
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