What is it about?
In this paper we show a method of analyzing the activity of Ca2+-activated, monovalent cation channels and show examples for the channels TRPM5 and TRPM4 specifically. This can be used in a high-throughput assay to investigate the ability of small (drug-like) molecules to modulate the activity of these channels. We are capable of identifying both inhibitors or activators/potentiators of the channel activity.
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Why is it important?
Ca2+-activated non-selective cation channels as TRPM4 and TRPM5 have been identified as an important factor in metabolic diseases such as diabetes and cardiac conductive disorders (Brugada-syndrome). Currently there is no known pharmacology to modulate the activity of these channels. With our described technique, we are a step closer to identify such molecules. These molecules can then be used as lead compounds to develop new drugs to treat the aforementioned diseases and can be used in studies to elucidate the details of the pathophysiology.
Perspectives
This screening method is a first step towards the development of new drugs to target Ca2+-activated monovalent cation channels. These channels are important in diseases as diabetes and heart failure. With the identification of these channels as potential new drug targets, there is the opportunity to develop a new class of drugs to treat these diseases.
Koenraad Philippaert
Associatie KU Leuven
Read the Original
This page is a summary of: A Thallium-Based Screening Procedure to Identify Molecules That Modulate the Activity of Ca2+-Activated Monovalent Cation-Selective Channels, SLAS DISCOVERY, January 2018, SAGE Publications,
DOI: 10.1177/2472555217748932.
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