2019
DOI: 10.3389/fendo.2019.00376
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Abstract: In the 1990s it was discovered that the enzyme dipeptidyl peptidase-4 (DPP-4) inactivates the incretin hormones glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). DPP-4 inhibition results in raised levels of the two incretin hormones which in turn result in lowering of circulating glucose through stimulation of insulin secretion and inhibition of glucagon secretion. Since then, several small orally available molecules have been developed with DPP-4 inhibitory action. Early … Show more

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Cited by 51 publications
(28 citation statements)
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References 145 publications
(198 reference statements)
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“…Heterocyclic nitrogenous compounds were tested broadly as anti-QS inhibitors [18][19][20], particularly pyrazine derivatives that were successfully used to modulate QS in Vibrio cholerae [18] and triazole derivatives that showed efficient anti-QS activity [21][22][23]. Sitagliptin, a pyrazine derivative with triazole moiety, is a hypoglycaemic agent for type II diabetes patients via inhibition of dipeptidyl-peptidase IV [35]. In this study, augmented resistance of S. marcescens isolated from endotracheal aspiration of diabetic patient admitted to intensive care unit was found.…”
Section: Discussionmentioning
confidence: 99%
“…DPP-4 inhibitors are known to augment beta-cell function [2,3], however, their effects on insulin resistance (sensitivity) remain elu-▶table 2 Link between the A1c index and glyemic and non-glycemic parameters. Simple regression analysis was performed between the A1c index and the baseline levels or changes of the indicated parameters (overall subjects).…”
Section: Effect Of Sitagliptin On Beta-cell Function and Insulin Sensmentioning
confidence: 99%
“…Subsequent clinical studies during the 2000s showed a glucose-lowering authority of DPP4 inhibitors in humans with type 2 diabetes as monotherapy or as combination with other therapies, i.e., metformin, sulfonylureas, tiazolidinediones or exogenous insulin. Five DPP-4 inhibitors (sitagliptin, vildagliptin, alogliptin, saxagliptin and linagliptin) were approved by regulatory authorities for treatment of type 2 diabetes and entered the market between 2006 and 2013 (22).…”
Section: Discussionmentioning
confidence: 99%
“…Interestingly, a correlation between DPP4 and ACE2 was found suggesting that both membrane proteins are relevant for the virus entry (21). DPP4 inhibitors are small molecules, which enter the catalytic pocket of the dimeric structure of DPP4 and bind to the catalytic site, thereby preventing the proteolytic activity (22). The coexpression of ACE2 and DPP4 as receptors of spike glycoproteins postulates that different human CoVs target similar cell types across different human tissues and explain the presence of comparable clinical features in patients infected with different CoVs.…”
Section: Introductionmentioning
confidence: 99%
“…A systematic review of the differences and similarities among DPP-4 inhibitors has been published previously (1). The therapeutic utility of DPP-4 inhibitors including vildagliptin is discussed in an accompanying article (11). The safety of vildagliptin has been reviewed previously (12); briefly the profile includes rare cases of mild to moderate elevations in hepatic enzymes, rare cases of angioedema (mostly in patients taking a concomitant ACE inhibitor) that resolved with ongoing treatment, and rare adverse drug reactions, including pancreatitis, bullous or exfoliative skin lesions, and arthralgia.…”
Section: Introductionmentioning
confidence: 99%