Targeting Tumor-Associated Hypoxia with Bioreductively Activatable Prodrug Conjugates Derived from Dihydronaphthalene, Benzosuberene, and Indole-based Inhibitors of Tubulin Polymerization

Zhe Shi; Rajsekhar Guddneppanavar; Blake A. Winn; Matthew T. MacDonough; Clinton S. George; Yifan Wang; Mariusz Zimmer; Jeni Gerberich; Alex Winters; Elisa Lin; Casey J. Maguire; Jacob W. Ford; Ernest Hamel; Ralph P. Mason; Mary Lynn Trawick; Kevin G. Pinney

doi:10.1039/d5md00564g

January 1, 2025RSC Medicinal ChemistryOpen Access

Targeting Tumor-Associated Hypoxia with Bioreductively Activatable Prodrug Conjugates Derived from Dihydronaphthalene, Benzosuberene, and Indole-based Inhibitors of Tubulin Polymerization

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Key Points

This strategy improves drug activation in regions of hypoxia, enhancing therapeutic efficacy.
The approach exploits reductase enzymes to convert inert prodrugs into active agents selectively.
Targeting tumor-associated hypoxia can lead to significant advancements in cancer treatment effectiveness.
Tissues with pronounced hypoxia provide an ideal environment for activating bioreductively designed prodrugs.

Implication

This approach utilizes reductase enzyme-mediated cleavage to activate prodrugs in hypoxic areas, suggesting a novel therapeutic strategy.

Abstract

A strategy for targeting tumor-associated hypoxia utilizes reductase enzyme-mediated cleavage to convert biologically inert prodrugs to their corresponding biologically active parent therapeutic agents selectively in areas of pronounced hypoxia. Small-molecule...

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Cite This Study

Shi et al. (2025) studied this question.

synapsesocial.com/papers/68bb3d682b87ece8dc9568b0 https://doi.org/10.1039/d5md00564g

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Targeting Tumor-Associated Hypoxia with Bioreductively Activatable Prodrug Conjugates Derived from Dihydronaphthalene, Benzosuberene, and Indole-based Inhibitors of Tubulin Polymerization

Key Points

Implication

Abstract

Discussion

Cite This Study

Targeting Tumor-Associated Hypoxia with Bioreductively Activatable Prodrug Conjugates Derived from Dihydronaphthalene, Benzosuberene, and Indole-based Inhibitors of Tubulin Polymerization

Key Points

Implication

Abstract

Discussion

Cite This Study

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