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Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
Published on: July 17, 2020
Recent advances in the development of protein tyrosine phosphatase 1B inhibitors for Type 2 diabetes
Shan Qian1, Man Zhang1, Yanying He1
1School of Food & Biotechnology, Xihua University, Chengdu 610039, PR China.
Abstract:
Diabetes mellitus is the most serious and prevalent metabolic disorders worldwide, complications of which can decrease significantly the quality of life and contribute to premature death. Resistance to insulin is a predominant pathophysiological factor of Type 2 diabetes (T2D). Protein tyrosine phosphatase 1B (PTP1B) is an important negative factor of insulin signal and a potent therapeutic target in T2D patients. This review highlights recent advances (2012-2015) in research related to the role of PTP1B in signal transduction processes implicated in pathophysiology of T2D, and novel PTP1B inhibitors with an emphasis on their chemical structures and modes of action.
Insights
Type 2 diabetes (T2D) involves insulin resistance, where Protein Tyrosine Phosphatase 1B (PTP1B) plays a key role. Recent research focuses on PTP1B inhibitors as a therapeutic strategy for T2D.
Area of Science:
- Biochemistry
- Metabolic Disorders
- Pharmacology
Background:
- Diabetes mellitus is a global health concern, with Type 2 diabetes (T2D) characterized by insulin resistance.
- Protein Tyrosine Phosphatase 1B (PTP1B) is a critical negative regulator of insulin signaling pathways.
- Dysregulation of PTP1B contributes significantly to the pathophysiology of T2D.
Purpose of the Study:
- To review recent research (2012-2015) on the role of PTP1B in T2D.
- To highlight novel PTP1B inhibitors as potential therapeutic agents for T2D.
- To discuss the chemical structures and mechanisms of action of these inhibitors.
Main Methods:
- Literature review of scientific publications from 2012-2015.
- Analysis of research on PTP1B's role in insulin signal transduction.
- Examination of novel PTP1B inhibitors, their structures, and modes of action.
Main Results:
- PTP1B is confirmed as a key player in T2D pathogenesis through its modulation of insulin signaling.
- Several novel PTP1B inhibitors have been identified and characterized.
- These inhibitors show promise in preclinical studies for managing T2D.
Conclusions:
- PTP1B remains a significant therapeutic target for Type 2 diabetes.
- Ongoing research into PTP1B inhibitors offers potential for improved T2D management.
- Understanding PTP1B's role in signal transduction is crucial for developing effective treatments.
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