The pharmacology of the TMEM16A channel: therapeutic opportunities

Rumaitha Al-Hosni; Zeki Ilkan; Emilio Agostinelli; Paolo Tammaro

doi:10.1016/j.tips.2022.06.006

The pharmacology of the TMEM16A channel: therapeutic opportunities

Rumaitha Al-Hosni, Zeki Ilkan, Emilio Agostinelli, Paolo Tammaro

Research output: Contribution to journal › Review article › peer-review

32 Scopus citations

Abstract

The TMEM16A Ca²⁺-gated Cl⁻ channel is involved in a variety of vital physiological functions and may be targeted pharmacologically for therapeutic benefit in diseases such as hypertension, stroke, and cystic fibrosis (CF). The determination of the TMEM16A structure and high-throughput screening efforts, alongside ex vivo and in vivo animal studies and clinical investigations, are hastening our understanding of the physiology and pharmacology of this channel. Here, we offer a critical analysis of recent developments in TMEM16A pharmacology and reflect on the therapeutic opportunities provided by this target.

Original language	English
Pages (from-to)	712-725
Number of pages	14
Journal	Trends in Pharmacological Sciences
Volume	43
Issue number	9
DOIs	https://doi.org/10.1016/j.tips.2022.06.006
State	Published - Sep 2022
Externally published	Yes

Keywords

TMEM16A
anoctamin 1
calcium signalling
cancer
chronic obstructive pulmonary disease
cystic fibrosis
hypertension
ion channels
pain
pericyte
stroke
vascular smooth muscle

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title = "The pharmacology of the TMEM16A channel: therapeutic opportunities",

abstract = "The TMEM16A Ca2+-gated Cl− channel is involved in a variety of vital physiological functions and may be targeted pharmacologically for therapeutic benefit in diseases such as hypertension, stroke, and cystic fibrosis (CF). The determination of the TMEM16A structure and high-throughput screening efforts, alongside ex vivo and in vivo animal studies and clinical investigations, are hastening our understanding of the physiology and pharmacology of this channel. Here, we offer a critical analysis of recent developments in TMEM16A pharmacology and reflect on the therapeutic opportunities provided by this target.",

keywords = "TMEM16A, anoctamin 1, calcium signalling, cancer, chronic obstructive pulmonary disease, cystic fibrosis, hypertension, ion channels, pain, pericyte, stroke, vascular smooth muscle",

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T1 - The pharmacology of the TMEM16A channel

T2 - therapeutic opportunities

AU - Al-Hosni, Rumaitha

AU - Ilkan, Zeki

AU - Agostinelli, Emilio

AU - Tammaro, Paolo

PY - 2022/9

Y1 - 2022/9

N2 - The TMEM16A Ca2+-gated Cl− channel is involved in a variety of vital physiological functions and may be targeted pharmacologically for therapeutic benefit in diseases such as hypertension, stroke, and cystic fibrosis (CF). The determination of the TMEM16A structure and high-throughput screening efforts, alongside ex vivo and in vivo animal studies and clinical investigations, are hastening our understanding of the physiology and pharmacology of this channel. Here, we offer a critical analysis of recent developments in TMEM16A pharmacology and reflect on the therapeutic opportunities provided by this target.

AB - The TMEM16A Ca2+-gated Cl− channel is involved in a variety of vital physiological functions and may be targeted pharmacologically for therapeutic benefit in diseases such as hypertension, stroke, and cystic fibrosis (CF). The determination of the TMEM16A structure and high-throughput screening efforts, alongside ex vivo and in vivo animal studies and clinical investigations, are hastening our understanding of the physiology and pharmacology of this channel. Here, we offer a critical analysis of recent developments in TMEM16A pharmacology and reflect on the therapeutic opportunities provided by this target.

KW - TMEM16A

KW - anoctamin 1

KW - calcium signalling

KW - cancer

KW - chronic obstructive pulmonary disease

KW - cystic fibrosis

KW - hypertension

KW - ion channels

KW - pain

KW - pericyte

KW - stroke

KW - vascular smooth muscle

UR - https://www.scopus.com/pages/publications/85133757216

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DO - 10.1016/j.tips.2022.06.006

M3 - Review article

C2 - 35811176

AN - SCOPUS:85133757216

SN - 0165-6147

VL - 43

SP - 712

EP - 725

JO - Trends in Pharmacological Sciences

JF - Trends in Pharmacological Sciences

IS - 9

ER -

The pharmacology of the TMEM16A channel: therapeutic opportunities

Abstract

Keywords

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