Substituted 2-Acylaminocycloalkylthiophene-3-carboxylic Acid Arylamides as Inhibitors of the Calcium-Activated Chloride Channel Transmembrane Protein 16A (TMEM16A).
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.7b00020
Abstract: Transmembrane protein 16A (TMEM16A), also called anoctamin 1 (ANO1), is a calcium-activated chloride channel expressed widely mammalian cells, including epithelia, vascular smooth muscle tissue, electrically excitable cells, and some tumors. TMEM16A inhibitors have been proposed… read more here.
Keywords: protein 16a; chloride channel; activated chloride; calcium activated ... See more keywords
Molecular determinants of pH sensing in the proton-activated chloride channel
Sign Up to like & getrecommendations! Published in 2022 at "Proceedings of the National Academy of Sciences of the United States of America"
DOI: 10.1073/pnas.2200727119
Abstract: Significance The acidic environment is critical for the proper function of many intracellular organelles. It is also associated with various diseases such as ischemia, cancer, and inflammation. In response to acidic pH, the proton-activated chloride… read more here.
Keywords: proton activated; molecular determinants; activated chloride; determinants sensing ... See more keywords
PAC proton-activated chloride channel contributes to acid-induced cell death in primary rat cortical neurons
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DOI: 10.1080/19336950.2020.1730019
Abstract: ABSTRACT Severe local acidosis causes tissue damage and pain, and is associated with many diseases, including cerebral and cardiac ischemia, cancer, infection, and inflammation. However, the molecular mechanisms of the cellular response to extracellular acidic… read more here.
Keywords: activated chloride; cell death; proton; proton activated ... See more keywords
Gating choreography and mechanism of the human proton-activated chloride channel ASOR
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DOI: 10.1126/sciadv.abm3942
Abstract: The proton-activated chloride channel ASOR (TMEM206/PAC) permeates anions across cellular membranes in response to acidification, thereby enhancing acid-induced cell death and regulating endocytosis. The molecular mechanisms of pH-dependent control are not understood, in part because… read more here.
Keywords: chloride channel; proton activated; asor; activated chloride ... See more keywords
Effect of New Derivatives of 2-Aminothiophene-3-Carboxylic Acid on Calcium-Activated Chloride Currents in Rat Neurons
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DOI: 10.1134/s1607672918060042
Abstract: Using the patch-clamp method in the whole-cell configuration, we showed that the new derivatives of 2-aminothiophene-3-carboxylic acid, which were synthesized by us earlier, can both block (compound 1) and potentiate (compound 2) calcium-activated chloride currents… read more here.
Keywords: new derivatives; carboxylic acid; activated chloride; calcium activated ... See more keywords