Medicinal Aspects of PTP 1B Inhibitors as Anti-Breast Cancer Agents: An Overview

Author:

Khator Rakesh1ORCID,Biharee Avadh1ORCID,Bhatia Neha1ORCID,Kulkarni Swanand1ORCID,Singh Yogesh1ORCID,Karthikeyan Chandrabose2ORCID,Jain Akhlesh Kumar3ORCID,Thareja Suresh1ORCID

Affiliation:

1. Department of Pharmaceutical Sciences and Natural Products, Central University of Punjab, Ghudda, Bathinda (Punjab)-1514 01, India

2. Department of Pharmacy, Indira Gandhi National Tribal University, Amarkantak (M. P.) – 484886, India

3. School of Pharmaceutical Sciences, Guru Ghasidas Central University, Bilaspur (C.G.) - 495009, India

Abstract

Abstract: Protein tyrosine phosphatase 1B (PTP1B) has gained interest as a therapeutic target for type 2 diabetes and obesity. Besides metabolic signalling, PTP1B is a positive regulator of signalling pathways linked to ErbB2-induced breast tumorigenesis. Substantial evidence proves that its overexpression is involved in breast cancer, which suggests that selective PTP1B inhibition might be effective in breast cancer treatment. Therefore, huge research is being carried out on PTP1B inhibitors and their activity against breast cancer development. To date, only two PTP1B inhibitors, viz. ertiprotafib and trodusquemine, have entered clinical trials. The discovery of selective inhibitors of PTP1B could open a new avenue in breast cancer treatment. In this review, we provide an extensive overview on the involvement of PTP1B in breast cancer, its pathophysiology, with special attention on the discovery and development of various natural as well as synthetic PTP1B inhibitors. This study will provide significant information to the researchers developing PTP1B inhibitors for breast cancer treatment.

Publisher

Bentham Science Publishers Ltd.

Subject

Pharmacology,Molecular Medicine,Drug Discovery,Biochemistry,Organic Chemistry

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