Ani9, A Novel Potent Small-Molecule ANO1 Inhibitor with Negligible Effect on ANO2

• Published in: PloS one Vol. 11; no. 5; p. e0155771
• Main Authors: Seo, Yohan, Lee, Ho K., Park, Jinhong, Jeon, Dong-kyu, Jo, Sungwoo, Jo, Minjae, Namkung, Wan
• Format: Journal Article
• Language: English
• Published: United States Public Library of Science 24.05.2016; Public Library of Science (PLoS)
• Subjects: Acetamides - pharmacology; Acids; Amino acids; Anoctamin-1; Anoctamins; Asthma; Biology and Life Sciences; Calcium; Calcium (intracellular); Calcium - metabolism; Calcium chloride; Calcium signalling; Cancer; Cell adhesion & migration; Cell culture; Cell Line; Channel gating; Chloride; Chloride channels (calcium-gated); Chloride Channels - antagonists & inhibitors; Chloride Channels - genetics; Chloride currents; Diarrhea; Gene Expression Regulation - drug effects; Genetic aspects; High-throughput screening; High-Throughput Screening Assays; Homology; Humans; Hydrazones - pharmacology; Hypertension; Inhibitors; Intracellular signalling; Ion channels; Medicine and Health Sciences; Membrane proteins; Membrane Proteins - genetics; Membrane Proteins - metabolism; Muscle contraction; Muscles; Neoplasm Proteins - antagonists & inhibitors; Neoplasm Proteins - genetics; Pain; Pain perception; Penicillin; Pharmaceutical sciences; Pharmacology; Pharmacy; Physical Sciences; Physiological aspects; Prostate cancer; Proteins; Pulmonary arteries; Pulmonary hypertension; Rodents; Screening; Secretion; Selectivity; Sequence Homology, Amino Acid; Small Molecule Libraries - pharmacology; Smooth muscle; Squamous cell carcinoma; Veins & arteries; Viruses; South Korea

Anoctamin1 (ANO1)/transmembrane protein 16A (TMEM16A), a calcium-activated chloride channel (CaCC), is involved in many physiological functions such as fluid secretion, smooth muscle contraction, nociception and cancer progression. To date, only a few ANO1 inhibitors have been described, and these h...