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

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...

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Published inPloS 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
LanguageEnglish
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
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Abstract 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 have low potency and selectivity for ANO1. Here, we performed a high-throughput screening to identify highly potent and selective small molecule inhibitors of ANO1. Three novel ANO1 inhibitors were discovered from screening of 54,400 synthetic small molecules, and they were found to fully block ANO1 channel activity with an IC50 < 3 μM. Electrophysiological analysis revealed that the most potent inhibitor, 2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9), completely inhibited ANO1 chloride current with submicromolar potency. Notably, unlike previous small-molecule ANO1 inhibitors identified to date, Ani9 displayed high selectivity for ANO1 as compared to ANO2, which shares a high amino acid homology to ANO1. In addition, Ani9 did not affect the intracellular calcium signaling and CFTR chloride channel activity. Our results suggest that Ani9 may be a useful pharmacological tool for studying ANO1 and a potential development candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma.
AbstractList 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 have low potency and selectivity for ANO1. Here, we performed a high-throughput screening to identify highly potent and selective small molecule inhibitors of ANO1. Three novel ANO1 inhibitors were discovered from screening of 54,400 synthetic small molecules, and they were found to fully block ANO1 channel activity with an IC50 < 3 μM. Electrophysiological analysis revealed that the most potent inhibitor, 2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9), completely inhibited ANO1 chloride current with submicromolar potency. Notably, unlike previous small-molecule ANO1 inhibitors identified to date, Ani9 displayed high selectivity for ANO1 as compared to ANO2, which shares a high amino acid homology to ANO1. In addition, Ani9 did not affect the intracellular calcium signaling and CFTR chloride channel activity. Our results suggest that Ani9 may be a useful pharmacological tool for studying ANO1 and a potential development candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma.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 have low potency and selectivity for ANO1. Here, we performed a high-throughput screening to identify highly potent and selective small molecule inhibitors of ANO1. Three novel ANO1 inhibitors were discovered from screening of 54,400 synthetic small molecules, and they were found to fully block ANO1 channel activity with an IC50 < 3 μM. Electrophysiological analysis revealed that the most potent inhibitor, 2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9), completely inhibited ANO1 chloride current with submicromolar potency. Notably, unlike previous small-molecule ANO1 inhibitors identified to date, Ani9 displayed high selectivity for ANO1 as compared to ANO2, which shares a high amino acid homology to ANO1. In addition, Ani9 did not affect the intracellular calcium signaling and CFTR chloride channel activity. Our results suggest that Ani9 may be a useful pharmacological tool for studying ANO1 and a potential development candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma.
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 have low potency and selectivity for ANO1. Here, we performed a high-throughput screening to identify highly potent and selective small molecule inhibitors of ANO1. Three novel ANO1 inhibitors were discovered from screening of 54,400 synthetic small molecules, and they were found to fully block ANO1 channel activity with an IC.sub.50 < 3 [mu]M. Electrophysiological analysis revealed that the most potent inhibitor, 2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9), completely inhibited ANO1 chloride current with submicromolar potency. Notably, unlike previous small-molecule ANO1 inhibitors identified to date, Ani9 displayed high selectivity for ANO1 as compared to ANO2, which shares a high amino acid homology to ANO1. In addition, Ani9 did not affect the intracellular calcium signaling and CFTR chloride channel activity. Our results suggest that Ani9 may be a useful pharmacological tool for studying ANO1 and a potential development candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma.
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 have low potency and selectivity for ANO1. Here, we performed a high-throughput screening to identify highly potent and selective small molecule inhibitors of ANO1. Three novel ANO1 inhibitors were discovered from screening of 54,400 synthetic small molecules, and they were found to fully block ANO1 channel activity with an IC 50 < 3 μM. Electrophysiological analysis revealed that the most potent inhibitor, 2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9), completely inhibited ANO1 chloride current with submicromolar potency. Notably, unlike previous small-molecule ANO1 inhibitors identified to date, Ani9 displayed high selectivity for ANO1 as compared to ANO2, which shares a high amino acid homology to ANO1. In addition, Ani9 did not affect the intracellular calcium signaling and CFTR chloride channel activity. Our results suggest that Ani9 may be a useful pharmacological tool for studying ANO1 and a potential development candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma.
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 have low potency and selectivity for ANO1. Here, we performed a high-throughput screening to identify highly potent and selective small molecule inhibitors of ANO1. Three novel ANO1 inhibitors were discovered from screening of 54,400 synthetic small molecules, and they were found to fully block ANO1 channel activity with an IC50 < 3 μM. Electrophysiological analysis revealed that the most potent inhibitor, 2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9), completely inhibited ANO1 chloride current with submicromolar potency. Notably, unlike previous small-molecule ANO1 inhibitors identified to date, Ani9 displayed high selectivity for ANO1 as compared to ANO2, which shares a high amino acid homology to ANO1. In addition, Ani9 did not affect the intracellular calcium signaling and CFTR chloride channel activity. Our results suggest that Ani9 may be a useful pharmacological tool for studying ANO1 and a potential development candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma.
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 have low potency and selectivity for ANO1. Here, we performed a high-throughput screening to identify highly potent and selective small molecule inhibitors of ANO1. Three novel ANO1 inhibitors were discovered from screening of 54,400 synthetic small molecules, and they were found to fully block ANO1 channel activity with an IC 50 < 3 μM. Electrophysiological analysis revealed that the most potent inhibitor, 2-(4-chloro-2-methylphenoxy)-N-[(2-methoxyphenyl)methylideneamino]-acetamide (Ani9), completely inhibited ANO1 chloride current with submicromolar potency. Notably, unlike previous small-molecule ANO1 inhibitors identified to date, Ani9 displayed high selectivity for ANO1 as compared to ANO2, which shares a high amino acid homology to ANO1. In addition, Ani9 did not affect the intracellular calcium signaling and CFTR chloride channel activity. Our results suggest that Ani9 may be a useful pharmacological tool for studying ANO1 and a potential development candidate for drug therapy of cancer, hypertension, pain, diarrhea and asthma.
Audience Academic
Author Jo, Sungwoo
Lee, Ho K.
Seo, Yohan
Jo, Minjae
Park, Jinhong
Jeon, Dong-kyu
Namkung, Wan
AuthorAffiliation 1 College of Pharmacy, Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon 406–840, Korea
2 Department of Integrated OMICS for Biomedical Science, WCU Program of Graduate School, Yonsei University, Seoul 120–749, Korea
Albany Medical College, UNITED STATES
AuthorAffiliation_xml – name: 1 College of Pharmacy, Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Incheon 406–840, Korea
– name: Albany Medical College, UNITED STATES
– name: 2 Department of Integrated OMICS for Biomedical Science, WCU Program of Graduate School, Yonsei University, Seoul 120–749, Korea
Author_xml – sequence: 1
  givenname: Yohan
  surname: Seo
  fullname: Seo, Yohan
– sequence: 2
  givenname: Ho K.
  surname: Lee
  fullname: Lee, Ho K.
– sequence: 3
  givenname: Jinhong
  surname: Park
  fullname: Park, Jinhong
– sequence: 4
  givenname: Dong-kyu
  surname: Jeon
  fullname: Jeon, Dong-kyu
– sequence: 5
  givenname: Sungwoo
  surname: Jo
  fullname: Jo, Sungwoo
– sequence: 6
  givenname: Minjae
  surname: Jo
  fullname: Jo, Minjae
– sequence: 7
  givenname: Wan
  surname: Namkung
  fullname: Namkung, Wan
BackLink https://www.ncbi.nlm.nih.gov/pubmed/27219012$$D View this record in MEDLINE/PubMed
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2016 Seo et al. This is an open access article distributed under the terms of the Creative Commons Attribution License: http://creativecommons.org/licenses/by/4.0/ (the “License”), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.
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Competing Interests: The authors have declared that no competing interests exist.
Conceived and designed the experiments: WN YS. Performed the experiments: YS HL JP DJ SJ. Analyzed the data: WN HL JP YS MJ. Contributed reagents/materials/analysis tools: WN YS. Wrote the paper: WN YS.
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Snippet Anoctamin1 (ANO1)/transmembrane protein 16A (TMEM16A), a calcium-activated chloride channel (CaCC), is involved in many physiological functions such as fluid...
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StartPage e0155771
SubjectTerms 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
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Title Ani9, A Novel Potent Small-Molecule ANO1 Inhibitor with Negligible Effect on ANO2
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http://dx.doi.org/10.1371/journal.pone.0155771
Volume 11
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