Related Experiment Video
Updated: Apr 25, 2026
An In Ovo Model for Testing Insulin-mimetic Compounds
Published on: April 23, 2018
PTP1B inhibitors for type 2 diabetes treatment: a patent review (2011 - 2014)
Akhilesh Kumar Tamrakar1, Chandan K Maurya, Amit K Rai
1CSIR-Central Drug Research Institute, Division of Biochemistry , Sector-10, Jankipuram Extension, Sitapur Road, Lucknow-226001 , India +91 0522 2772550 Ext. 4635 ; +91 0522 2771941 ; akhilesh_tamrakar@cdri.res.in CSIR-CDRI communication number: 8743.
Introduction:
Protein tyrosine phosphatase 1B (PTP1B) plays an important role in the negative regulation of insulin signal transduction pathway and has emerged as novel therapeutic strategy for the treatment of type 2 diabetes. PTP1B inhibitors enhance the sensibility of insulin receptor (IR) and have favorable curing effect for insulin resistance-related diseases. A large number of PTP1B inhibitors, either synthetic or isolated as bioactive agents from natural products, have developed and investigated for their ability to stimulate insulin signaling.
Areas Covered:
This review includes an updated summary (2011 - 2014) of PTP1B inhibitors that have been published in patent applications, with an emphasis on their chemical structure, mode of action and therapeutic outcomes. The usefulness of PTP1B inhibitors as pharmaceutical agents for the treatment of type 2 diabetes is also discussed.
Expert Opinion:
PTP1B inhibitors show beneficial effects to enhance sensibility of IR by restricting the activity of enzyme and have favorable curing effects. However, structural homologies in the catalytic domain of PTP1B with other protein tyrosine phosphatases (PTPs) like leukocyte common antigen-related, CD45, SHP-2 and T-cell-PTP present a challenging task of achieving selectivity. Thus, for therapeutic application of PTP1B inhibitors, highly selective molecules exhibiting desired effects without side effects are expected to find clinical application.
Insights
Protein tyrosine phosphatase 1B (PTP1B) inhibitors improve insulin sensitivity for type 2 diabetes treatment. Developing selective PTP1B inhibitors is crucial for effective therapeutic applications with minimal side effects.
Area of Science:
- Biochemistry
- Pharmacology
- Drug Discovery
Background:
- Protein tyrosine phosphatase 1B (PTP1B) negatively regulates insulin signaling.
- PTP1B inhibitors enhance insulin receptor (IR) sensitivity, offering therapeutic potential for type 2 diabetes and insulin resistance.
- Numerous synthetic and natural PTP1B inhibitors have been explored to stimulate insulin signaling.
Purpose of the Study:
- To review PTP1B inhibitors published in patent applications from 2011-2014.
- To analyze chemical structures, mechanisms of action, and therapeutic outcomes of these inhibitors.
- To discuss the pharmaceutical utility of PTP1B inhibitors for type 2 diabetes.
Main Methods:
- Literature review of patent applications (2011-2014).
- Analysis of chemical structures and modes of action.
- Evaluation of therapeutic outcomes and potential side effects.
Main Results:
- PTP1B inhibitors demonstrate beneficial effects by enhancing IR sensitivity.
- Inhibitors restrict PTP1B enzyme activity, showing promise for treating insulin resistance-related diseases.
- The review summarizes various PTP1B inhibitors and their reported efficacy.
Conclusions:
- PTP1B inhibitors offer a promising therapeutic strategy for type 2 diabetes.
- Achieving selectivity is challenging due to structural similarities with other protein tyrosine phosphatases (PTPs).
- Highly selective PTP1B inhibitors are needed for clinical application to maximize benefits and minimize adverse effects.
