Abstract:
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 treatments of type 2 diabetes. PTP1B inhibitors enhance the sensibility of insulin receptor, and has favourable 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.
Area 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 insulin receptor by restricting the activity of enzyme and have favourable curing effects. However, structural homologies in the catalytic domain of PTP1B with other PTPs like LAR, CD45, SHP-2, and TC-PTP presents 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.
