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. 2025 Jul 3;16(1):1257.
doi: 10.1007/s12672-025-03083-0.

Selective targeting of the AKT1 (E17K) mutation: advances in precision oncology and therapeutic design

Xiaoyan Chen #  1   2 , Danfeng Zhang #  3 , Jiapeng Xue  4 , Zhi Li  5   6
Affiliations

Selective targeting of the AKT1 (E17K) mutation: advances in precision oncology and therapeutic design

Xiaoyan Chen et al. Discov Oncol. .

Abstract

The AKT1 (E17K) mutation, associated with unfavourable outcomes in solid tumours, promotes cancer proliferation and persistence. A recent study by Gregory et al. discovered a reversible covalent inhibitor targeting this mutation, exhibiting significant anti-tumor action with little effects on normal cells. This advancement provides a targeted therapeutic approach for AKT-mutant malignancies and informs further inhibitor research.

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Conflict of interest statement

Declarations. Ethics approval and consent to participate: Not applicable. Consent for publication: Not applicable. Competing interests: The authors declare no competing interests.

Figures

Fig. 1
Fig. 1
Domain structure of the AKT protein in humans. A AKT1; B AKT2; C AKT3
Fig. 2
Fig. 2
Common genetic mutations associated with AKT signaling in cancer. These mutations are involved in cell proliferation, survival, angiogenesis, tumorigenesis, and genomic instability, making them key targets for cancer therapy. Created with BioRender.com
See this image and copyright information in PMC

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