Target intelligence / Profile preview

Dipeptidyl peptidase 4 (DPP-IV), Protein-tyrosine phosphatase non-receptor type 1 (PTP-1B), Alpha-glucosidase, and Alpha-amylase (DPP-IV, PTP-1B, α-glucosidase, α-amylase)

Target
DPP-IV, PTP-1B, α-glucosidase, α-amylase
Molecular classification
Enzyme, Hydrolase, Phosphatase, Peptidase
01

Overview

This entry refers to a group of four distinct enzymes—Dipeptidyl peptidase 4 (DPP-IV), Protein-tyrosine phosphatase 1B (PTP-1B), alpha-glucosidase, and alpha-amylase—that serve as critical therapeutic targets for the treatment of Type 2 diabetes mellitus. Dipeptidyl peptidase 4 is a serine protease that inactivates incretin hormones like GLP-1, which are essential for glucose-dependent insulin secretion (UniProt P27487). Protein-tyrosine phosphatase non-receptor type 1 (PTP-1B) is a phosphatase that negatively regulates insulin and leptin signaling by dephosphorylating the insulin receptor, contributing to insulin resistance (UniProt P18031). Alpha-glucosidase and alpha-amylase are digestive enzymes that catalyze the hydrolysis of starch and disaccharides into glucose within the gastrointestinal tract (UniProt P0DPH0, P04746). Pharmacological inhibition of these targets aims to improve glycemic control by enhancing insulin sensitivity, prolonging incretin activity, and slowing the rate of carbohydrate absorption (PubMed 31542394). While drugs like gliptins and acarbose are clinically established, current research explores multi-target inhibitors that can address these pathways simultaneously to optimize metabolic outcomes (PubMed 28843445).

Other names
CD26PTPN1Maltase-glucoamylaseSucrase-isomaltaseSalivary alpha-amylasePancreatic alpha-amylaseAMY1AAMY2AMGAM
02

Mechanism of action

Inhibition of DPP-IV prevents the degradation of incretin hormones (GLP-1 and GIP); inhibition of PTP-1B enhances insulin and leptin receptor signaling; inhibition of alpha-glucosidase and alpha-amylase delays the breakdown of complex carbohydrates and slows glucose absorption (PubMed 31542394).

03

Biological functions

Carbohydrate metabolismInsulin signaling regulationIncretin degradationGlucose homeostasis
04

Disease associations

Type 2 diabetes mellitusObesityMetabolic syndrome
05

Safety considerations

Gastrointestinal side effects (flatulence, diarrhea)Potential risk of pancreatitisHypoglycemia riskSelectivity challenges for PTP-1B
06

Interacting drugs

Sitagliptin

6 more in the full profile.

07

Biomarkers

HbA1cFasting plasma glucosePostprandial glucoseGLP-1 levels

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