Can enzyme activation convert selective kinase inhibitors into targeted prodrugs?
Hinshaw, Gray et al. develop AKR1C3-activated prodrugs designed as targeted CDK11-inhibitors with potential to reduce cytotoxicity and improve the therapeutic window.
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An AKR1C3-activated kinase inhibitor prodrug
Enzymatically activated prodrugs can enable context-specific target inhibition. AKR1C3 is an NADPH-dependent aldo-ketoreductase involved in androgen metabolism, prostaglandin synthesis, and cell proliferation that is overexpressed in tumors, making it an ideal candidate for tumor-specific prodrug activation. Report
