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   Articles with "tmem16a" as a keyword



TMEM16A/ANO1 suppression improves response to antibody‐mediated targeted therapy of EGFR and HER2/ERBB2

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recommendations! Published in 2017 at "Genes"

DOI: 10.1002/gcc.22450

Abstract: TMEM16A, a Ca2+‐activated Cl− channel, contributes to tumor growth in breast cancer and head and neck squamous cell carcinoma (HNSCC). Here, we investigated whether TMEM16A influences the response to EGFR/HER family‐targeting biological therapies. Inhibition of… read more here.

Keywords: egfr her2; improves response; tmem16a; antibody ... See more keywords

TMEM16A (ANO1) as a therapeutic target in cystic fibrosis.

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recommendations! Published in 2022 at "Current opinion in pharmacology"

DOI: 10.1016/j.coph.2022.102206

Abstract: Cystic fibrosis (CF) is a multi-organ genetic disease caused by loss of function of CFTR, a cAMP-regulated chloride channel expressed in epithelial cells. In airway epithelia, CFTR-dependent chloride secretion is required to humidify mucosal surface… read more here.

Keywords: cystic fibrosis; tmem16a; tmem16a ano1; ano1 therapeutic ... See more keywords

Identification of evodiamine and rutecarpine as novel TMEM16A inhibitors and their inhibitory effects on peristalsis in isolated Guinea-pig ileum.

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recommendations! Published in 2021 at "European journal of pharmacology"

DOI: 10.1016/j.ejphar.2021.174340

Abstract: The transmembrane member 16A (TMEM16A)-encoded Ca2+-activated Cl- channel (CaCC) is expressed in interstitial cells of Cajal (ICCs) and involved in the generation of the slow-wave currents of gastrointestinal (GI) smooth muscles. TMEM16A modulators have been… read more here.

Keywords: inhibitory effects; tmem16a; evodiamine rutecarpine; tmem16a inhibitors ... See more keywords

Voltage-Dependent Protonation of the Calcium Pocket Enable Activation of the Calcium-Activated Chloride Channel Anoctamin-1 (TMEM16A)

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recommendations! Published in 2020 at "Scientific Reports"

DOI: 10.1038/s41598-020-62860-9

Abstract: Anoctamin-1 (ANO1 or TMEM16A) is a homo-dimeric Ca 2+ -activated Cl − channel responsible for essential physiological processes. Each monomer harbours a pore and a Ca 2+ -binding pocket; the voltage-dependent binding of two intracellular… read more here.

Keywords: voltage; dependent protonation; voltage dependent; tmem16a ... See more keywords

Identification of novel TMEM16A blockers through integrated virtual screening, molecular dynamics, and experimental studies

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recommendations! Published in 2025 at "Scientific Reports"

DOI: 10.1038/s41598-025-99751-w

Abstract: The 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 for… read more here.

Keywords: screening molecular; virtual screening; identification novel; tmem16a ... See more keywords

Calcium-activated chloride channel TMEM16A opens via pi-helical transition in transmembrane segment 4

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recommendations! Published in 2025 at "Proceedings of the National Academy of Sciences of the United States of America"

DOI: 10.1073/pnas.2421900122

Abstract: Significance TMEM16A is an anion channel whose main physiological function is to couple chloride conduction to the level of intracellular Ca2+. Despite physiological importance and high pharmacological potential of TMEM16A, its gating mechanism remains incompletely… read more here.

Keywords: channel; helical transition; transition transmembrane; tmem16a ... See more keywords

Trans-ε-viniferin as an inhibitor of TMEM16A preventing intestinal smooth muscle contraction.

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recommendations! Published in 2023 at "Journal of Asian natural products research"

DOI: 10.1080/10286020.2023.2165067

Abstract: TMEM16A regulator is an important tool to study the physiological functions and pathogenesis related to TMEM16A. In the present study, trans-ε-viniferin (TV) was identified as a TMEM16A inhibitor with inhibitory activity against TMEM16A mediated Cl-… read more here.

Keywords: intestinal smooth; trans viniferin; muscle contraction; inhibitor ... See more keywords

The TMEM16A channel as a potential therapeutic target in vascular disease

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recommendations! Published in 2024 at "Current Opinion in Nephrology and Hypertension"

DOI: 10.1097/mnh.0000000000000967

Abstract: Purpose of review The transmembrane protein 16A (TMEM16A) Ca2+-activated Cl− channel constitutes a key depolarising mechanism in vascular smooth muscle and contractile pericytes, while in endothelial cells the channel is implicated in angiogenesis and in… read more here.

Keywords: vascular disease; tmem16a; channel; tmem16a channels ... See more keywords

Endothelial cell TMEM16A channels regulate arterial contractility and blood pressure

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recommendations! Published in 2023 at "Physiology"

DOI: 10.1152/physiol.2023.38.s1.5726735

Abstract: Endothelial cells (ECs) are electrically coupled to arterial smooth muscle cells in the vascular wall and can modulate their contractility through direct control of membrane potential and via the production of several vasoactive substances. ECs… read more here.

Keywords: tmem16a channels; contractility; physiology; tmem16a ... See more keywords

TMEM16A Potentiation: A Novel Therapeutic Approach for the Treatment of Cystic Fibrosis

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recommendations! Published in 2020 at "American Journal of Respiratory and Critical Care Medicine"

DOI: 10.1164/rccm.201908-1641oc

Abstract: Rationale: Enhancing non–CFTR (cystic fibrosis transmembrane conductance regulator)-mediated anion secretion is an attractive therapeutic approach for the treatment of cystic fibrosis (CF) and other mucoobstructive diseases. Objectives: To determine the effects of TMEM16A potentiation on… read more here.

Keywords: tmem16a; cystic fibrosis; approach treatment; secretion ... See more keywords

TMEM16A chloride channel does not drive mucus production

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recommendations! Published in 2019 at "Life Science Alliance"

DOI: 10.26508/lsa.201900462

Abstract: Despite being essential for airway hydration, TMEM16A is not required for mucus (MUC5AC) production. Cell proliferation is the main driver for TMEM16A up-regulation during inflammation. Airway mucus obstruction is the main cause of morbidity in… read more here.

Keywords: production; mucus production; proliferation; muc5ac ... See more keywords