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A Review on the Role of TRP Channels and Their Potential as Drug Targets_An Insight Into the TRP Channel Drug Discovery Methodologies

Transient receptor potential (TRP) proteins are a large group of ion channels that control many physiological functions in our body. These channels are considered potential therapeutic drug targets for various diseases such as neurological disorders, cancers, cardiovascular disease, and many more. T...

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Autores principales: Fallah, Hamideh P, Ahuja, Ekta, Lin, Haoquan, Qi, Jinlong, He, Qian, Gao, Shan, An, Hailong, Zhang, Jian, Xie, Yongzhen, Liang, Dong
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Frontiers Media S.A. 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9170958/
https://www.ncbi.nlm.nih.gov/pubmed/35685622
http://dx.doi.org/10.3389/fphar.2022.914499
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author Fallah, Hamideh P
Ahuja, Ekta
Lin, Haoquan
Qi, Jinlong
He, Qian
Gao, Shan
An, Hailong
Zhang, Jian
Xie, Yongzhen
Liang, Dong
author_facet Fallah, Hamideh P
Ahuja, Ekta
Lin, Haoquan
Qi, Jinlong
He, Qian
Gao, Shan
An, Hailong
Zhang, Jian
Xie, Yongzhen
Liang, Dong
author_sort Fallah, Hamideh P
collection PubMed
description Transient receptor potential (TRP) proteins are a large group of ion channels that control many physiological functions in our body. These channels are considered potential therapeutic drug targets for various diseases such as neurological disorders, cancers, cardiovascular disease, and many more. The Nobel Prize in Physiology/Medicine in the year 2021 was awarded to two scientists for the discovery of TRP and PIEZO ion channels. Improving our knowledge of technologies for their study is essential. In the present study, we reviewed the role of TRP channel types in the control of normal physiological functions as well as disease conditions. Also, we discussed the current and novel technologies that can be used to study these channels successfully. As such, Flux assays for detecting ionic flux through ion channels are among the core and widely used tools for screening drug compounds. Technologies based on these assays are available in fully automated high throughput set-ups and help detect changes in radiolabeled or non-radiolabeled ionic flux. Aurora’s Ion Channel Reader (ICR), which works based on label-free technology of flux assay, offers sensitive, accurate, and reproducible measurements to perform drug ranking matching with patch-clamp (gold standard) data. The non-radiolabeled trace-based flux assay coupled with the ICR detects changes in various ion types, including potassium, calcium, sodium, and chloride channels, by using appropriate tracer ions. This technology is now considered one of the very successful approaches for analyzing ion channel activity in modern drug discovery. It could be a successful approach for studying various ion channels and transporters, including the different members of the TRP family of ion channels.
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spelling pubmed-91709582022-06-08 A Review on the Role of TRP Channels and Their Potential as Drug Targets_An Insight Into the TRP Channel Drug Discovery Methodologies Fallah, Hamideh P Ahuja, Ekta Lin, Haoquan Qi, Jinlong He, Qian Gao, Shan An, Hailong Zhang, Jian Xie, Yongzhen Liang, Dong Front Pharmacol Pharmacology Transient receptor potential (TRP) proteins are a large group of ion channels that control many physiological functions in our body. These channels are considered potential therapeutic drug targets for various diseases such as neurological disorders, cancers, cardiovascular disease, and many more. The Nobel Prize in Physiology/Medicine in the year 2021 was awarded to two scientists for the discovery of TRP and PIEZO ion channels. Improving our knowledge of technologies for their study is essential. In the present study, we reviewed the role of TRP channel types in the control of normal physiological functions as well as disease conditions. Also, we discussed the current and novel technologies that can be used to study these channels successfully. As such, Flux assays for detecting ionic flux through ion channels are among the core and widely used tools for screening drug compounds. Technologies based on these assays are available in fully automated high throughput set-ups and help detect changes in radiolabeled or non-radiolabeled ionic flux. Aurora’s Ion Channel Reader (ICR), which works based on label-free technology of flux assay, offers sensitive, accurate, and reproducible measurements to perform drug ranking matching with patch-clamp (gold standard) data. The non-radiolabeled trace-based flux assay coupled with the ICR detects changes in various ion types, including potassium, calcium, sodium, and chloride channels, by using appropriate tracer ions. This technology is now considered one of the very successful approaches for analyzing ion channel activity in modern drug discovery. It could be a successful approach for studying various ion channels and transporters, including the different members of the TRP family of ion channels. Frontiers Media S.A. 2022-05-24 /pmc/articles/PMC9170958/ /pubmed/35685622 http://dx.doi.org/10.3389/fphar.2022.914499 Text en Copyright © 2022 Fallah, Ahuja, Lin, Qi, He, Gao, An, Zhang, Xie and Liang. https://creativecommons.org/licenses/by/4.0/This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) and the copyright owner(s) are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
spellingShingle Pharmacology
Fallah, Hamideh P
Ahuja, Ekta
Lin, Haoquan
Qi, Jinlong
He, Qian
Gao, Shan
An, Hailong
Zhang, Jian
Xie, Yongzhen
Liang, Dong
A Review on the Role of TRP Channels and Their Potential as Drug Targets_An Insight Into the TRP Channel Drug Discovery Methodologies
title A Review on the Role of TRP Channels and Their Potential as Drug Targets_An Insight Into the TRP Channel Drug Discovery Methodologies
title_full A Review on the Role of TRP Channels and Their Potential as Drug Targets_An Insight Into the TRP Channel Drug Discovery Methodologies
title_fullStr A Review on the Role of TRP Channels and Their Potential as Drug Targets_An Insight Into the TRP Channel Drug Discovery Methodologies
title_full_unstemmed A Review on the Role of TRP Channels and Their Potential as Drug Targets_An Insight Into the TRP Channel Drug Discovery Methodologies
title_short A Review on the Role of TRP Channels and Their Potential as Drug Targets_An Insight Into the TRP Channel Drug Discovery Methodologies
title_sort review on the role of trp channels and their potential as drug targets_an insight into the trp channel drug discovery methodologies
topic Pharmacology
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9170958/
https://www.ncbi.nlm.nih.gov/pubmed/35685622
http://dx.doi.org/10.3389/fphar.2022.914499
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