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Updated: Aug 9, 2026

A Mass Spectrometry-Based Approach to Identify Phosphoprotein Phosphatases and their Interactors
Published on: April 29, 2022
Protein kinases and phosphatases as therapeutic targets in cancer
Juan-José Ventura1, Angel R Nebreda
1Spanish National Cancer Center (CNIO), Madrid, Spain. jjventura@cnio.es
Abstract:
Protein phosphorylation plays key roles in many physiological processes and is often deregulated in pathological conditions. Our current understanding of how protein kinases and phosphatases orchestrate the phosphorylation changes that control cellular functions has made these enzymes potential drug targets for the treatment of many diseases. The success of the tyrosine kinase inhibitor Gleevec in the treatment of some cancers has further invigorated the development of kinase inhibitors as anti-cancer drugs. A large number of these compounds are currently undergoing clinical trials and there is much expectation on the therapeutic potential of these molecules, as more specific and less toxic drugs than currently used generic chemotherapeutic agents. In this manuscript, we review the current status of more than 30 protein kinase inhibitors with proven or potential therapeutic value for cancer treatment. These include inhibitors of receptor and cytosolic tyrosine kinases as well as compounds that target different families of serine/threonine kinases involved in signalling and cell cycle regulation. We also briefly touch on the prospects of phosphatase inhibitors. The combination of kinase inhibitors to target different components of signalling pathways that are found deregulated in tumours is also emerging as an interesting approach for cancer therapy.
Insights
Protein kinase inhibitors are promising cancer drugs, offering targeted therapy with fewer side effects than traditional chemotherapy. This review covers over 30 kinase inhibitors, including tyrosine and serine/threonine kinase inhibitors, for cancer treatment.
Area of Science:
- Biochemistry
- Pharmacology
- Oncology
Background:
- Protein phosphorylation is crucial for cellular functions, and its dysregulation is linked to diseases.
- Protein kinases and phosphatases are key regulators of phosphorylation, making them important drug targets.
- The success of Gleevec has spurred the development of kinase inhibitors as targeted cancer therapies.
Purpose of the Study:
- To review the current status of protein kinase inhibitors for cancer treatment.
- To highlight the therapeutic potential of these targeted agents.
- To briefly discuss phosphatase inhibitors and combination therapies.
Main Methods:
- Review of over 30 protein kinase inhibitors.
- Inclusion of inhibitors targeting receptor and cytosolic tyrosine kinases.
- Inclusion of inhibitors targeting serine/threonine kinases involved in signaling and cell cycle regulation.
Main Results:
- Numerous kinase inhibitors show proven or potential therapeutic value in cancer.
- These inhibitors offer more specificity and reduced toxicity compared to generic chemotherapeutics.
- Combination therapy targeting deregulated signaling pathways is an emerging strategy.
Conclusions:
- Protein kinase inhibitors represent a significant advancement in targeted cancer therapy.
- Further development of kinase and phosphatase inhibitors holds great promise for oncology.
- Combination strategies may enhance treatment efficacy for various cancers.
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