Abstract
The G-protein coupled receptors (GPCRs) activated by free fatty acids (FFAs) have emerged as new and exciting drug targets, due to their plausible translation from pharmacology to medicines. This perspective aims to report recent research about GPR120/FFAR4 and its involvement in several diseases, including cancer, inflammatory conditions, and central nervous system disorders. The focus is to highlight the importance of GPR120 in Type 2 diabetes mellitus (T2DM). GPR120 agonists, useful in T2DM drug discovery, have been widely explored from a structure–activity relationship point of view. Since the identification of the first reported synthetic agonist TUG-891, the research has paved the way for the development of TUG-based molecules as well as new and different chemical entities. These molecules might represent the starting point for the future discovery of GPR120 agonists as antidiabetic drugs.
Highlights
Type 2 diabetes mellitus (T2DM) is one of the metabolic diseases that is expected to see a doubling in global prevalence to over 350 million people worldwide in the first three decades of the third millennium.[1]
New drugs have emerged such as sodiumglucose cotransporter-2 (SGLT2) inhibitors, which decrease the reabsorption of glucose in the kidney and, lower blood sugar,[2] and glucagon-like peptide-1 (GLP-1) receptor agonists, such as exenatide, liraglutide, and lixisenatide.[3]
GLP-1 receptor agonists can promote the functional role of GLP-1, a gut hormone produced by the small intestine in response to oral ingestion of glucose, which promotes a glucoregulatory effect by increasing insulin and suppressing glucagon secretion.[4]
Summary
Type 2 diabetes mellitus (T2DM) is one of the metabolic diseases that is expected to see a doubling in global prevalence to over 350 million people worldwide in the first three decades of the third millennium.[1]. New drugs have emerged such as sodiumglucose cotransporter-2 (SGLT2) inhibitors, which decrease the reabsorption of glucose in the kidney and, lower blood sugar,[2] and glucagon-like peptide-1 (GLP-1) receptor agonists, such as exenatide, liraglutide, and lixisenatide.[3] GLP-1 receptor agonists can promote the functional role of GLP-1, a gut hormone produced by the small intestine in response to oral ingestion of glucose, which promotes a glucoregulatory effect by increasing insulin and suppressing glucagon secretion.[4] DPP-IV inhibitors showed an interesting therapeutic behavior reducing glucagon levels consisting of the ability to promote incretin secretion in turns These drugs were able to reduce blood glucose fluctuations with an enhancement of GLP-1 preservation and expansion of β-cell mass through the inhibition of apoptotic pathways. From a medicinal chemist point of view, a particular emphasis was given to GPR120 agonists’ usefulness in T2DM management, with a discussion on the structure−activity relationships (SARs) that includes the patent literature
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