Virtual Screening and Biological Evaluation of Novel Low Molecular Weight Protein Tyrosine Phosphatase Inhibitor for the Treatment of Insulin Resistance.

ABSTRACT:

Purpose

Protein tyrosine phosphatases (PTPs) play an essential way in diseases including cancer, obesity, diabetes and autoimmune disorders. As a member of PTPs, low molecular weight PTP (LMPTP) has been a well-recognized anti-insulin resistance target in obesity. However, the number of reported LMPTP inhibitors is limited. Our research aims to discover a novel LMPTP inhibitor and evaluate its biological activity against insulin resistance.

Methods

A virtual screening pipeline based on the X-ray co-crystal complex of LMPTP was constructed. Enzyme inhibition assay and cellular bioassay were used to evaluate the activity of screened compounds.

Results

The screening pipeline rendered 15 potential hits from Specs chemical library. Enzyme inhibition assay identified compou

SUBMITTER: Feng B 

PROVIDER: S-EPMC10128076 | biostudies-literature | 2023

REPOSITORIES: biostudies-literature