Docking Assisted Prediction and Biological Evaluation of Sideritis L. Components with PTP1b Inhibitory Action and Probable Anti-Diabetic Properties

Current Topics in Medicinal Chemistry
Phaedra EleftheriouAnna Micha

Abstract

The main characteristic of Diabetes type II is the impaired activation of intracellular mechanisms triggered by the action of insulin. PTP1b is a Protein Tyrosine Phosphatase that dephosphorylates insulin receptor causing its desensitization. Since inhibition of PTP1b may prolong insulin receptor activity, PTP1b has become a drug target for the treatment of Diabetes II. Although a number of inhibitors have been synthesized during the last decades, the research still continues for the development of more effective and selective compounds. Moreover, several constituents of plants and edible algae with PTP1b inhibitory action have been found, adding this extra activity at the pallet of properties of the specific natural products. Sideritis L. (Lamiaceae) is a herbal plant growing around the Mediterranean sea which is included in the Mediterranean diet for centuries. The present study is the continuation of a previous work where the antioxidant and anti-inflammatory activities of the components of Sideritis L. were evaluated and aimed to investigate the potential of some sideritis's components to act as PTP1b inhibitors, thus exhibiting the beneficial effect in the treatment of diabetes II. Docking analysis was done to predict PTP1...Continue Reading

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Citations

Apr 25, 2019·Current Topics in Medicinal Chemistry·Athina Geronikaki

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