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Curr Drug Targets. 2018;19(5):551-575. doi: 10.2174/1389450118666170222143739.

Recent Advances in Protein Tyrosine Phosphatase 1B Targeted Drug Discovery for Type II Diabetes and Obesity.

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School of Pharmaceutical Sciences, Rajiv Gandhi Proudyogiki Vishwavidyalaya, Airport Bypass Road, Gandhi Nagar, Bhopal (MP)-462036, India.
Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak (MP)-484887, India.



Protein tyrosine phosphatase 1B (PTP1B) is an important therapeutic target for type II diabetes and obesity because of its pivotal role as a negative modulator in both insulin and leptin signalling pathways.


The discovery of PTP1B inhibitors has been the focus of researchers in both academia and pharmaceutical industry over the last two decades.


Though, intense pharmaceutical research in this area has resulted in many potent PTP1B inhibitors, a vast majority of them possessed pTyr mimetic group such as phosphonates, carboxylic acids and sulphamic acids, which led to poor PTP1B selectivity and insufficient in vivo efficacy due to low cell permeability and bioavailability. The availability of X-ray crystallographic structures of PTP1B together with the application of molecular modelling and other innovative strategies led to the development of many potent and selective PTP1B inhibitors with desirable physicochemical properties. This review traces the development of PTP1B inhibitors over the last decade and also records novel PTP1B inhibitors developed recently with greater emphasis on their selectivity and cell permeability.


Diabetes; PTP1B inhibitors; drug discovery; molecular modelling; obesity; signalling pathways

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