TMEM16A in Cystic Fibrosis: Activating or Inhibiting? [PDF]
Frontiers in Pharmacology, 2019 The inflammatory airway disease cystic fibrosis (CF) is characterized by airway obstruction due to mucus hypersecretion, airway plugging, and bronchoconstriction.
Karl Kunzelmann +8 more
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TMEM16A inhibition suppresses melanoma metastasis. [PDF]
Acta Biochim Biophys Sin (Shanghai)Zhou N +5 more
europepmc +3 more sources
Identification of novel TMEM16A blockers through integrated virtual screening, molecular dynamics, and experimental studies [PDF]
Scientific ReportsThe calcium-activated chloride channel TMEM16A is a promising drug target for treating hypertension, secretory diarrheas, and various cancers, including head and neck cancer. Despite its potential, no FDA-approved drugs have provided the structural basis
Mattanun Sangkhawasi +6 more
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The Tmem16a chloride channel is required for mucin maturation after secretion from goblet-like cells in the Xenopus tropicalis tadpole skin [PDF]
Scientific ReportsThe TMEM16A chloride channel is proposed as a therapeutic target in cystic fibrosis, where activation of this ion channel might restore airway surface hydration and mitigate respiratory symptoms.
Eamon Dubaissi +10 more
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The pharmacology of the TMEM16A channel: therapeutic opportunities
Trends in Pharmacological Sciences, 2022 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 ...
Rumaitha Al-Hosni +3 more
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Niclosamide potentiates TMEM16A and induces vasoconstriction
Biophysical Journal, 2023 ABSTRACT The TMEM16A calcium-activated chloride channel is a promising therapeutic target for various diseases. Niclosamide, an anthelmintic medication, has been considered as a TMEM16A inhibitor for treating asthma and chronic obstructive pulmonary disease, but was recently found to possess broad-spectrum off-target effects.
Pengfei Liang +4 more
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The Molecular Mechanism of Ginsenoside Analogs Activating TMEM16A [PDF]
Biophysical Journal, 2020 The calcium-activated chloride channel TMEM16A is involved in many physiological processes, and insufficient function of TMEM16A may lead to the occurrence of various diseases. Therefore, TMEM16A activators are supposed to be potentially useful for treatment of TMEM16A downregulation-inducing diseases.
Shuai Guo +7 more
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Activation of TMEM16A Ca2+-activated Cl− channels by ROCK1/moesin promotes breast cancer metastasis
Journal of Advanced Research, 2021 Introduction: Transmembrane protein 16A (TMEM16A) is a Ca2+-activated chloride channel that plays a role in cancer cell proliferation, migration, invasion, and metastasis.
Shuya Luo +13 more
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Fractionation of a herbal antidiarrheal medicine reveals eugenol as an inhibitor of Ca2+-Activated Cl- channel TMEM16A. [PDF]
PLoS ONE, 2012 The Ca(2+)-activated Cl(-) channel TMEM16A is involved in epithelial fluid secretion, smooth muscle contraction and neurosensory signaling. We identified a Thai herbal antidiarrheal formulation that inhibited TMEM16A Cl(-) conductance. C18-reversed-phase
Zhen Yao +5 more
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Functional expression of TMEM16A in taste bud cells [PDF]
The Journal of Physiology, 2021 Key points Taste transduction occurs in taste buds in the tongue epithelium. The Ca2+‐activated Cl– channels TMEM16A and TMEM16B play relevant physiological roles in several sensory systems. Here, we report that TMEM16A, but not TMEM16B, is expressed in the apical part of taste buds.
Guarascio D. M. +4 more
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