Therapeutically Targeting TGR5 and P2Y Receptors

  • Senthilkumar Rajagopal
  • Murugavel Ponnusamy


A few cell surface receptors of bile acids have been discovered so far. TGR5 is a membrane-bound G-protein-coupled receptor for bile acids that are found in several types of tissues types, including liver. TGR5 is involved in a number of important biological processes, such as controlling the energy balance, insulin and glucose homeostasis, inflammation, bile formation and secretion, intestinal motility and secretion, and bile acid -evoked itch and analgesia. The neurons of the enteric and central nervous system also express TGR5 and it is involved in the intestinal motility and detection of endogenous neurosteroids in response to bile acids. The role of TGR5 against metabolic, inflammatory and digestive diseases is becoming prominent and the agonists of TGR5 may promote energy expenditure and insulin release, inflammation, and promote colon transit. Many of the recent reviews have described the conditions in which TGR5 could be a promising new target for pharmaceutical agents. Hence, it becomes important to delineate how these agonists regulate TGR5. The expression and/or activities of P2Ys are highly altered in cells and tissues during the disease progression and more than one P2Ys are involved in many cases. The growing bodies of evidences from experimental and clinical studies emphasize the potential therapeutic value of members of P2Y. As they are considered to be a new therapeutic strategy, several pharmacological agents targeting P2Y receptors are presently available in the market and many of them are under clinical trials. This present chapter summarize the present knowledge on therapeutic significance of TGR5 and P2Y receptors and to reveal the plausible therapeutic use of agents targeting these receptors in the treatment of human diseases.


Allosteric ligands Bile acids Glucose homeostasis Inflammation Metabolic diseases 


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Copyright information

© Springer Nature Singapore Pte Ltd. 2018

Authors and Affiliations

  • Senthilkumar Rajagopal
    • 1
  • Murugavel Ponnusamy
    • 2
  1. 1.Department of BiochemistryRayalaseema UniversityKurnoolIndia
  2. 2.Center for Developmental Cardiology, Institute for Translational MedicineQingdao UniversityQingdaoChina

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