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Updated: May 7, 2025
Assessing Cellular Target Engagement by SHP2 PTPN11 Phosphatase Inhibitors
Published on: July 17, 2020
Research progress of SHP-1 agonists as a strategy for tumor therapy
Xiaoyue Liu1, Qindi He1, Shuding Sun2
1School of Science, China Pharmaceutical University, Nanjing, 211198, People's Republic of China.
Abstract:
Src homology-2 domain-containing protein tyrosine phosphatase 1 (SHP-1) is a member of protein tyrosine phosphatase (PTP) family, and serves as a crucial negative regulator of various oncogenic signaling pathways. The development of SHP-1 agonists has garnered extensive research attention and is considered as a promising strategy for treating tumors. In this review, we comprehensively analyze the advancements of SHP-1 agonists, focusing on their structures and biological activities. Based on the structure skeletons, we classify these SHP-1 agonists as kinase inhibitors, sorafenib derivatives, obatoclax derivatives, lithocholic acid derivatives and thieno[2,3-b]quinoline derivatives. Additionally, we discuss the potential opportunities and challenges for developing SHP-1 agonists. It is hoped that this review will provide inspiring insights into the discovery of drugs targeting SHP-1.
Insights
Src homology-2 domain-containing protein tyrosine phosphatase 1 (SHP-1) agonists are promising cancer treatments. This review details SHP-1 agonist structures, biological activities, and development challenges, offering insights for future drug discovery.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- SHP-1 is a protein tyrosine phosphatase (PTP) that negatively regulates oncogenic signaling pathways.
- SHP-1 agonists represent a promising therapeutic strategy for cancer treatment.
Purpose of the Study:
- To comprehensively review advancements in SHP-1 agonists.
- To analyze the structures and biological activities of SHP-1 agonists.
- To discuss opportunities and challenges in developing SHP-1 targeting drugs.
Main Methods:
- Classification of SHP-1 agonists based on structural skeletons.
- Analysis of structure-activity relationships.
- Review of existing literature on SHP-1 agonists.
Main Results:
- SHP-1 agonists were categorized into five classes: kinase inhibitors, sorafenib derivatives, obatoclax derivatives, lithocholic acid derivatives, and thieno[2,3-b]quinoline derivatives.
- Detailed analysis of the structural features and biological activities of each class was performed.
Conclusions:
- SHP-1 agonists hold significant therapeutic potential for various cancers.
- Further research into the development of SHP-1 agonists is warranted to overcome existing challenges and optimize drug discovery.
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