2. Academic Validation
  3. Activation of TMEM16A by natural product canthaxanthin promotes gastrointestinal contraction

Activation of TMEM16A by natural product canthaxanthin promotes gastrointestinal contraction

  • FASEB J. 2020 Oct;34(10):13430-13444. doi: 10.1096/fj.202000443RR.
Qiushuang Ji 1 2,  Sai Shi 1 3,  Shuai Guo 1 3,  Yong Zhan 1 3,  Hailin Zhang 4,  Yafei Chen 1,  Hailong An 1 3
Affiliations

Affiliations

  • 1 Key Laboratory of Molecular Biophysics, Hebei Province, Institute of Biophysics, School of Sciences, Hebei University of Technology, Tianjin, China.
  • 2 School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China.
  • 3 School of Electrical Engineering, Hebei University of Technology, Tianjin, China.
  • 4 Key Laboratory of Neural and Vascular Biology, Ministry of Education, The Key Laboratory of Pharmacology and Toxicology for New Drug, Department of Pharmacology, Hebei Medical University, Shijiazhuang, China.
PMID: 32812278 DOI: 10.1096/fj.202000443RR
Abstract

Transmembrane 16A (TMEM16A), also known as anoctamin 1, is the molecular basis of the calcium-activated chloride channels. TMEM16A is present in interstitial cells of Cajal, which are the pacemaker cells that control smooth muscle contraction. TMEM16A is implicated in gastrointestinal disorders. Activation of TMEM16A is believed to promote the gastrointestinal muscle contraction. Here, we report a highly efficient, nontoxic, and selective activator of TMEM16A, canthaxanthin (CX). The study using molecular docking and site-directed mutation revealed that CX-specific binging site in TMEM16A is K769. CX was also found to promote the contraction of smooth muscle cells in gastrointestinal tract through activation of TMEM16A channels, which provides an excellent basis for development of CX as a chemical tool and potential therapeutic for gastrointestinal dysfunction.

Keywords

TMEM16A; activator; binding site; canthaxanthin; ileal contraction.

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