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Updated: Jun 18, 2026

Assessing Cellular Target Engagement by SHP2 (PTPN11) Phosphatase Inhibitors
Published on: July 17, 2020
Phosphatases as targets for cancer treatment
1University of Pittsburgh, Department of Pharmacology and Chemical Biology, Drug Discovery Institute, 10051 BST3, 3501 Fifth Avenue, Pittsburgh, PA 15260, USA. lazo@pitt.edu
Abstract:
Although protein kinases are the molecular targets for an increasing number of anticancer agents, there is a notable absence of drugs targeting protein phosphatases, the biochemical counterpart of the protein kinases. This absence is particularly striking because many cancer-relevant pathways are also controlled by protein phosphatases, which can function abnormally in human tumors. Several research groups are searching for drug-like inhibitors of phosphatase-based cancer targets. This review examines several protein phosphatases for which investigational anticancer agents have been identified and are being investigated.
Insights
Anticancer drug development has overlooked protein phosphatases, crucial regulators of cancer pathways. This review explores investigational drugs targeting these phosphatases for cancer therapy.
Area of Science:
- Biochemistry
- Oncology
- Pharmacology
Background:
- Protein kinases are established anticancer drug targets.
- Protein phosphatases, the counterparts to kinases, are underrepresented as therapeutic targets in oncology.
- Dysregulated protein phosphatase activity is implicated in human tumor development and progression.
Purpose of the Study:
- To review the current landscape of investigational anticancer agents targeting protein phosphatases.
- To highlight the therapeutic potential of targeting protein phosphatases in cancer treatment.
- To identify key protein phosphatases that are targets for novel anticancer drug discovery.
Main Methods:
- Literature review of scientific databases.
- Analysis of research on protein phosphatases and their role in cancer.
- Examination of identified investigational anticancer agents targeting protein phosphatases.
Main Results:
- Several protein phosphatases have been identified as viable targets for anticancer drug development.
- Investigational agents targeting these phosphatases are under active research.
- The development of phosphatase inhibitors presents a promising avenue for novel cancer therapies.
Conclusions:
- Targeting protein phosphatases represents a significant, yet largely untapped, strategy in anticancer drug discovery.
- Further research into phosphatase inhibitors could lead to new treatments for various human tumors.
- The development of specific and effective phosphatase inhibitors is crucial for advancing cancer therapy.
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