| Autor: |
Dimitra K. Georgiou, Victoria C. Yan, Florian L. Muller, Kristine L. Yang, Kenisha Arthur, Elliot S. Ballato |
| Rok vydání: |
2020 |
| Předmět: |
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| DOI: |
10.26434/chemrxiv.12033303.v1 |
| Popis: |
Glycolysis inhibition remains aspirational in cancer therapy. We recently described a promising phosphonate inhibitor of Enolase for cancers harboring deletions in ENO1. Here, we describe the application of nitroheterocycle pro-drugs capitalizing on tumor hypoxia. These bioreducible pro-drugs exhibit up to 14-fold greater potency under hypoxic conditions compared to normoxia and exhibit robust stability in biological fluids. Our work provides strong proof-of-concept for using bioreduction as a pro-drug delivery strategy in the context of Enolase inhibition. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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