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A comprehensive review on the research progress of PTP1B inhibitors as antidiabetics

Neetu Agrawal1, Parth Dhakrey1, Shilpi Pathak1

  • 1Institute of Pharmaceutical Research, GLA University, Mathura, Uttar Pradesh, India.

Chemical Biology & Drug Design
|May 26, 2023
PubMed

Insights

New protein tyrosine phosphatase 1B (PTP1B) inhibitors show promise for treating type 2 diabetes. These compounds enhance insulin sensitivity and energy expenditure, offering a novel therapeutic approach for this metabolic disease.

Area of Science:

  • Metabolic disorders
  • Pharmacology
  • Drug discovery

Background:

  • Diabetes mellitus (DM), particularly Type 2 DM, is a major global health issue affecting over 500 million people.
  • Insulin resistance is the primary driver of Type 2 DM, a condition with severe health consequences if left untreated.
  • Current oral hypoglycemic agents target various pathways, but novel therapeutic strategies are needed.

Purpose of the Study:

  • To review recent advances in synthetic protein tyrosine phosphatase 1B (PTP1B) inhibitors.
  • To explore the potential of PTP1B inhibitors as clinical antidiabetic drugs.
  • To highlight PTP1B inhibitors as a novel approach for managing type 2 diabetes and obesity.

Main Methods:

  • Literature review of synthetic PTP1B inhibitors published between 2015 and 2022.
  • Analysis of PTP1B's role as a negative regulator of insulin and leptin signaling.
  • Evaluation of PTP1B inhibitors' impact on insulin sensitivity, glucose uptake, and energy expenditure.

Main Results:

  • PTP1B inhibitors represent a promising therapeutic strategy for type 2 diabetes.
  • Inhibition of PTP1B enhances insulin sensitivity and glucose absorption.
  • PTP1B inhibitors also positively influence leptin signaling and may target obesity.

Conclusions:

  • Synthetic PTP1B inhibitors developed between 2015-2022 show significant potential for clinical application in treating type 2 diabetes.
  • Targeting PTP1B offers a novel mechanism to improve insulin sensitivity and energy metabolism.
  • Further development of these inhibitors could lead to effective treatments for both diabetes and obesity.
Keywords:
PTP1Bdiabetes mellitusheterocycleprotein tyrosine phosphatasesynthetic compound

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