Dipeptidylpeptidase-4 inhibitor

Sitagliptin is a dipeptidylpeptidase-4 inhibitor that increases insulin secretion and lowers glucagon secretion. Sitagliptin is available for oral administration. It is indicated in patients with type 2 diabetes mellitus in combination with either metformin (biguanide) or a sulphonylurea or a thiazolidinedione. 

L-Dihydroxyphenylalanine 4-Dihydroxyphenylethylamine Dimeric Transcription Factors Dioxins Dipeptidase Dipeptidylpeptidase Dipeptidylpeptidase IV Direct Thrombin Inhibitors Discharge of Neurons... 

Sitagliptin is a selective dipeptidylpeptidase 4 (DPP-4) inhibitor which increases the active form of GLP-1 (glucagon-like-peptide-1) and GIP (glucose-dependent insulinotropic peptide). This enzyme-inhibiting drug is to be used either alone or in combination with metformin or a thiazolidinedione for control of type 2 diabetes mellitus. Adverse effects were as common with sitagliptin (whether used alone or with metformin or pioglitazone) as they were with placebo, except for nausea and common cold-like symptoms. 

Several fluorine-containing drugs are currently in development for the treatment of diabetes. These are peroxisome proliferator-activated nuclear receptor (PPAR) agonists, aldose reductase, and dipeptidylpeptidase IV (DPP-IV) inhibitors. 

The incretin hormone glucagon-like peptide-1 (GLP-1) plays a crucial role in the regulation of insulin by acting on the pancreas to potentiate glucose-induced insulin secretion. GLP-1 is rapidly cleaved by serine protease dipeptidylpeptidase IV. The inhibitors of DDP-IV are new drugs for the oral treatment of type 2 diabetes. 

Dipeptidylpeptidase IV (EC 3.4.11.5 postproline dipeptidyl aminopeptidase CD26) is a serine protease located in the plasma membrane. Notable neuropeptide substrates include substance P. neuropeptide Y, peptide YY and enterostatin. Inhibitors include diprotin A (lle-Pro-lle) and diprotin B (Val-Pro-Leu)... 

Diprosone betamethasone. diprOtin A is a tripeptide that is an ENZYME INHIBITOR with selectivity as an aminopeptidase inhibitor active against dipeptidylpeptidase IV (EC 3.4.11). It can be used as a pharmacological tool in experimental analytical studies, dipyridamole [ban, inn, usan] (Persantin ) is a pyrimidine derivative, a coronary VASODILATOR, a (class la) ANTIARRHYTHMIC, an adenosine UPTAKE INHIBITOR causing indirect adenosine receptor activation, and enhances effects of anticoagulants and is a platelet AGGREGATION INHIBITOR. 

Peptidases. Others members of the serine protease family, cleave oligopeptides and do not necessarily act on proteins. These include two peptidases of particular interest (dipeptidylpeptidase IV and proline endopeptidase). See also AMINOPEPTIDASE INHIBITORS CARBOXYPEPTIDASE INHIBITORS ... 

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