Journal
CATALYSTS
Volume 10, Issue 10, Pages -Publisher
MDPI
DOI: 10.3390/catal10101153
Keywords
aptamer; cancer; G-quadruplex; ion-responsive inhibitor; IRDAptamer; phosphatase; PPM1D
Categories
Funding
- Japanese Society for the Promotion of Sciences [15K05560, 19H03512]
- JSPS [18J20422]
- Niigata University
- Grants-in-Aid for Scientific Research [19H03512, 15K05560, 18J20422] Funding Source: KAKEN
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(1) Background: Ser/Thr protein phosphatase PPM1D is an oncogenic protein. In normal cells, however, PPM1D plays essential roles in spermatogenesis and immune response. Hence, it is necessary to develop novel PPM1D inhibitors without side effects on normal cells. Stimuli-responsive molecules are suitable for the spatiotemporal regulation of inhibitory activity. (2) Methods: In this study, we designed an ion-responsive DNA aptamer library based on G-quadruplex DNA that can change its conformation and function in response to monovalent cations. (3) Results: Using this library, we identified the PPM1D specific inhibitor M1D-Q5F aptamer. The M1D-Q5F aptamer showed anti-cancer activity against breast cancer MCF7 cells. Interestingly, the induction of the structural change resulting in the formation of G-quadruplex upon stimulation by monovalent cations led to the enhancement of the inhibitory activity and binding affinity of M1D-Q5F. (4) Conclusions: These data suggest that the M1D-Q5F aptamer may act as a novel stimuli-responsive anti-cancer agent.
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