Toward the Identification of Extra-Oral TAS2R Agonists as Drug Agents for Muscle Relaxation Therapies via Bioinformatics-Aided Screening of Bitter Compounds in Traditional Chinese Medicine

Frontiers in Physiology
Mingzhi LuoLinhong Deng

Abstract

Significant advances have been made in the past decade in mapping the distributions and the physiological functions of extra-oral bitter taste receptors (TAS2Rs) in non-gustatory tissues. In particular, it has been found that TAS2Rs are expressed in various muscle tissues and activation of TAS2Rs can lead to muscle cell relaxation, which suggests that TAS2Rs may be important new targets in muscle relaxation therapy for various muscle-related diseases. So far, however, there is a lack of potent extra-oral TAS2R agonists that can be used as novel drug agents in muscle relaxation therapies. Interestingly, traditional Chinese medicine (TCM) often characterizes a drug's property in terms of five distinct flavors (bitter, sweet, sour, salty, and pungent) according to its taste and function, and commonly regards "bitterness" as an intrinsic property of "good medicine." In addition, many bitter flavored TCM are known in practice to cause muscle relaxation after long term use, and in lab experiments the compounds identified from some bitter flavored TCM do activate TAS2Rs and thus relax muscle cells. Therefore, it is highly possible to discover very useful extra-oral TAS2R agonists for muscle relaxation therapies among the abundant bitt...Continue Reading

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Citations

May 15, 2020·Biological & Pharmaceutical Bulletin·Mingzhi LuoLinhong Deng
Jan 23, 2020·Journal of Clinical Medicine·Laura GoverniniPaola Piomboni
Feb 15, 2021·International Journal of Biological Macromolecules·Shima ParsaNaser Hatami
Mar 22, 2021·International Journal of Pharmaceutics·Gerardo De LeónSharareh Salar-Behzadi

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Software Mentioned

BitterX
BitterPredict
Bitter
GOMoDo
BitterSweet Forest

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