Bioreducible Phosphonoamidate Pro-drug Inhibitor ofEnolase: Proof of Concept Study
2020
Glycolysis
inhibition remains aspirational in cancer therapy. We
recently described a promising phosphonate inhibitor of enolase for
cancers harboring homozygous deletions of ENO1. Here,
we describe the application of a nitroheterocycle phosphonoamidate
pro-drug pair to capitalize on tumor hypoxia. This bioreducible prodrug
exhibits greater-than 2-fold potency under hypoxic conditions compared
to normoxia and exhibits robust stability in biological fluids. Our
work provides strong in vitro proof-of-concept for
using bioreduction as a pro-drug delivery strategy in the context
of enolase inhibition.
Keywords:
- Correction
- Source
- Cite
- Save
- Machine Reading By IdeaReader
30
References
1
Citations
NaN
KQI