G-protein coupled receptor 40 agonists as novel therapeutics for type 2 diabetes.
With growing needs for new antidiabetic drugs which are safe and effective alone or in combination with existing drugs, G-protein coupled receptor 40 (GPR40) has drawn a considerable attention as a potential therapeutic target for type 2 diabetes. As GPR40 agonist may offer advantages to commonly used agents, by acting ambient glucose dependent manner which mechanistically leads to reduced risk of developing hypoglycemia. Since deorphanization in 2003, development of small molecule GPR40 agonists has been spurred by several research groups. There are a number of lead molecules targeting GPR40, and among these molecules TAK-875 (full agonist) and AMG 837 (partial agonist) advanced into clinical stage.
Yun Jung
YJ
Choi
Dongyun
D
Shin
Ju-Yeun
JY
Lee
D001572:Benzofurans / Q000494:pharmacology / Q000627:therapeutic use; D001713:Biphenyl Compounds / Q000494:pharmacology / Q000627:therapeutic use; D003924:Diabetes Mellitus, Type 2 / Q000188:drug therapy*; D055808:Drug Discovery; D015507:Drugs, Investigational / Q000494:pharmacology* / Q000627:therapeutic use; D006801:Humans; D007004:Hypoglycemic Agents / Q000494:pharmacology* / Q000627:therapeutic use*; D043562:Receptors, G-Protein-Coupled / Q000819:agonists*; D015398:Signal Transduction / Q000187:drug effects; D013450:Sulfones / Q000494:pharmacology / Q000627:therapeutic use; D000480:Alkynes; D010666:Phenylpropionates
D001572:Benzofurans; D001713:Biphenyl Compounds; D015507:Drugs, Investigational; D007004:Hypoglycemic Agents; D043562:Receptors, G-Protein-Coupled; D013450:Sulfones; C473034:FFAR1 protein, human; C557331:TAK-875; C557933:AMG-837; D000480:Alkynes; D010666:Phenylpropionates