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Peripheral Serotonin Synthesis as a New Drug Target
Susann Matthes1, Michael Bader2
1Max-Delbrück Center for Molecular Medicine (MDC), Robert-Rössle-Straße 10, 13125 Berlin-Buch, Germany; University of Lübeck, Institute for Biology, Ratzeburger Allee 160, 23562 Lübeck, Germany.
Trends in Pharmacological Sciences
|April 10, 2018
Summary
Peripheral serotonin (5-HT) synthesis, regulated by tryptophan hydroxylase (TPH), impacts gut health and disease. TPH inhibitors offer targeted therapeutic potential for conditions like carcinoid syndrome.
Area of Science:
- Biochemistry
- Pharmacology
- Gastroenterology
Background:
- Serotonin (5-HT) is synthesized via tryptophan hydroxylase (TPH).
- TPH1 in gut enterochromaffin cells and TPH2 in neurons produce distinct 5-HT pools.
- Peripheral 5-HT influences platelet function and inflammatory/fibrotic diseases.
Purpose of the Study:
- To review the development of TPH inhibitors.
- To discuss their therapeutic applications in peripheral 5-HT-related diseases.
- To explore future treatment options using these compounds.
Main Methods:
- Review of existing literature on TPH inhibitors.
- Analysis of studies involving TPH1-deficient mice models.
- Examination of clinical data for approved TPH inhibitors like telotristat ethyl.
Main Results:
- TPH1 inhibition effectively targets peripheral 5-HT production.
- TPH inhibitors demonstrate efficacy in various rodent disease models.
- Telotristat ethyl is the first approved TPH inhibitor for carcinoid syndrome.
Conclusions:
- Targeting peripheral serotonin synthesis with TPH inhibitors is a viable therapeutic strategy.
- These inhibitors show promise for treating inflammatory, fibrotic, and other conditions.
- Further research into TPH inhibitor applications is warranted.
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