Emerging Modulators of TMEM16A and Their Therapeutic Potential

Calcium-activated chloride channels (CaCCs) are widespread chloride channels which rely on calcium activation to perform their functions. In 2008, TMEM16A (also known as anoctamin1, ANO1) was identified as the molecular basis of the CaCCs, which provided the possibility to study the physiological fu...

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Published inThe Journal of membrane biology Vol. 254; no. 4; pp. 353 - 365
Main Authors Hao, Anqi, Guo, Shuai, Shi, Sai, Wang, Xuzhao, Zhan, Yong, Chen, Yafei, An, Hailong
Format Journal Article
LanguageEnglish
Published New York Springer US 01.08.2021
Springer Nature B.V
Subjects
Anoctamin-1 - genetics
Asthma
Biochemistry
Biomedical and Life Sciences
Calcium - metabolism
Calcium channels
Calcium chloride
Cancer
Chloride channels (calcium-gated)
Chloride Channels - genetics
Chloride ions
Excitability
Fertilization
Gastric motility
Gastrointestinal Motility
Human Physiology
Ion channels
Life Sciences
Modulators
Motility
Muscle contraction
Muscles
Muscular function
Neuromodulation
Physiology
Smooth muscle
Therapeutic targets
Topical Review
Efficacy
TMEM16A/ANO1
Modulators
Screening methods
Diseases
Online AccessGet full text

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Abstract Calcium-activated chloride channels (CaCCs) are widespread chloride channels which rely on calcium activation to perform their functions. In 2008, TMEM16A (also known as anoctamin1, ANO1) was identified as the molecular basis of the CaCCs, which provided the possibility to study the physiological function of CaCCs. TMEM16A is widely expressed in various cells and controls basic physiological functions, including neuronal and cardiac excitability, nerve transduction, smooth muscle contraction, epithelial Cl − secretion and fertilization. However, the abnormal function of TMEM16A may cause a variety of diseases, including asthma, gastrointestinal motility disorder and various cancers. Therefore, TMEM16A is a putative drug target for many diseases, and it is important to determine specific and efficient modulators of TMEM16A channel. In recent years, we and others have screened several natural modulators of TMEM16A against cancers and gastrointestinal motility dysfunction. This article reviews the screening methods, efficacy of TMEM16A modulators and pharmacological effects of TMEM16A modulators on different diseases. Graphic Abstact
AbstractList Calcium-activated chloride channels (CaCCs) are widespread chloride channels which rely on calcium activation to perform their functions. In 2008, TMEM16A (also known as anoctamin1, ANO1) was identified as the molecular basis of the CaCCs, which provided the possibility to study the physiological function of CaCCs. TMEM16A is widely expressed in various cells and controls basic physiological functions, including neuronal and cardiac excitability, nerve transduction, smooth muscle contraction, epithelial Cl secretion and fertilization. However, the abnormal function of TMEM16A may cause a variety of diseases, including asthma, gastrointestinal motility disorder and various cancers. Therefore, TMEM16A is a putative drug target for many diseases, and it is important to determine specific and efficient modulators of TMEM16A channel. In recent years, we and others have screened several natural modulators of TMEM16A against cancers and gastrointestinal motility dysfunction. This article reviews the screening methods, efficacy of TMEM16A modulators and pharmacological effects of TMEM16A modulators on different diseases. GRAPHIC ABSTACT.
Calcium-activated chloride channels (CaCCs) are widespread chloride channels which rely on calcium activation to perform their functions. In 2008, TMEM16A (also known as anoctamin1, ANO1) was identified as the molecular basis of the CaCCs, which provided the possibility to study the physiological function of CaCCs. TMEM16A is widely expressed in various cells and controls basic physiological functions, including neuronal and cardiac excitability, nerve transduction, smooth muscle contraction, epithelial Cl − secretion and fertilization. However, the abnormal function of TMEM16A may cause a variety of diseases, including asthma, gastrointestinal motility disorder and various cancers. Therefore, TMEM16A is a putative drug target for many diseases, and it is important to determine specific and efficient modulators of TMEM16A channel. In recent years, we and others have screened several natural modulators of TMEM16A against cancers and gastrointestinal motility dysfunction. This article reviews the screening methods, efficacy of TMEM16A modulators and pharmacological effects of TMEM16A modulators on different diseases. Graphic Abstact
Calcium-activated chloride channels (CaCCs) are widespread chloride channels which rely on calcium activation to perform their functions. In 2008, TMEM16A (also known as anoctamin1, ANO1) was identified as the molecular basis of the CaCCs, which provided the possibility to study the physiological function of CaCCs. TMEM16A is widely expressed in various cells and controls basic physiological functions, including neuronal and cardiac excitability, nerve transduction, smooth muscle contraction, epithelial Cl− secretion and fertilization. However, the abnormal function of TMEM16A may cause a variety of diseases, including asthma, gastrointestinal motility disorder and various cancers. Therefore, TMEM16A is a putative drug target for many diseases, and it is important to determine specific and efficient modulators of TMEM16A channel. In recent years, we and others have screened several natural modulators of TMEM16A against cancers and gastrointestinal motility dysfunction. This article reviews the screening methods, efficacy of TMEM16A modulators and pharmacological effects of TMEM16A modulators on different diseases.Graphic Abstact
Author Shi, Sai
Chen, Yafei
An, Hailong
Hao, Anqi
Guo, Shuai
Wang, Xuzhao
Zhan, Yong
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Keywords Efficacy
TMEM16A/ANO1
Modulators
Screening methods
Diseases
Language English
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Snippet Calcium-activated chloride channels (CaCCs) are widespread chloride channels which rely on calcium activation to perform their functions. In 2008, TMEM16A...
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SubjectTerms Anoctamin-1 - genetics
Asthma
Biochemistry
Biomedical and Life Sciences
Calcium - metabolism
Calcium channels
Calcium chloride
Cancer
Chloride channels (calcium-gated)
Chloride Channels - genetics
Chloride ions
Excitability
Fertilization
Gastric motility
Gastrointestinal Motility
Human Physiology
Ion channels
Life Sciences
Modulators
Motility
Muscle contraction
Muscles
Muscular function
Neuromodulation
Physiology
Smooth muscle
Therapeutic targets
Topical Review
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Title Emerging Modulators of TMEM16A and Their Therapeutic Potential
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Volume 254
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