Drug intelligence / Profile preview

TZ-POR 7f

Development stage
Preclinical
Lead developer
The University of Auckland
Modality
Small Molecules
01

Overview

TZ-POR 7f is a potent and selective small-molecule inhibitor of **Cytochrome P450 oxidoreductase (POR)**, characterized by a triazole-based scaffold. POR is a critical diflavin enzyme that serves as the obligatory electron donor for all microsomal cytochrome P450 (CYP) enzymes, as well as other redox partners like heme oxygenase and squalene monooxygenase. TZ-POR 7f was developed as a chemical tool to investigate the role of POR in drug metabolism and the activation of **hypoxia-activated prodrugs (HAPs)**, such as evofosfamide and tirapazamine. By binding to POR and disrupting the electron transport chain from NADPH to its redox partners, TZ-POR 7f effectively suppresses POR-dependent enzymatic activities. This inhibition can be used to modulate CYP-mediated drug metabolism or to prevent the off-target reductive activation of HAPs in normoxic tissues, potentially reducing systemic toxicity in cancer therapy.

Other names
Compound 7fCompound7fCompound-7fPOR inhibitor 7f
02

Targets

POR (NADPH-cytochrome P450 oxidoreductase)

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