Druggable cancer phosphatases

The phosphorylation status of oncoproteins is regulated by both kinases and phosphatases. Kinase inhibitors are rarely sufficient for successful cancer treatment, and phosphatases have been considered undruggable targets for cancer drug development. However, innovative pharmacological approaches for...

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Bibliographic Details
Published in:Science translational medicine 2021-04, Vol.13 (588), p.1
Main Authors: Vainonen, Julia P, Momeny, Majid, Westermarck, Jukka
Format: Article
Language:English
Subjects:
Antineoplastic Agents - pharmacology
Antineoplastic Agents - therapeutic use
Cancer
Drug development
Genes, Tumor Suppressor
Homology
Humans
Kinases
Medical innovations
Neoplasms - drug therapy
Neoplasms - genetics
Phosphatase
Phosphoprotein phosphatase
Phosphorylation
Protein phosphatase
Protein Phosphatase 2 - metabolism
SH2 Domain-Containing Protein Tyrosine Phosphatases - metabolism
Therapeutic targets
Tumor suppressor genes
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Summary:The phosphorylation status of oncoproteins is regulated by both kinases and phosphatases. Kinase inhibitors are rarely sufficient for successful cancer treatment, and phosphatases have been considered undruggable targets for cancer drug development. However, innovative pharmacological approaches for targeting phosphatases have recently emerged. Here, we review progress in the therapeutic targeting of oncogenic Src homology region 2 domain-containing phosphatase-2 (SHP2) and tumor suppressor protein phosphatase 2A (PP2A) and select other druggable oncogenic and tumor suppressor phosphatases. We describe the modes of action for currently available small molecules that target phosphatases, their use in drug combinations, and advances in clinical development toward future cancer therapies.
ISSN:1946-6234
1946-6242
1946-3242
DOI:10.1126/scitranslmed.abe2967