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De Montfort University

Michael Danny Burke

Lawrence Hylton Patterson

Gerard Andrew Potter

William Thomas Melvin

Graeme Ian Murray

Paul Crispin Butler

Gerald Andrew Potter

William Frank Greenlee

The present invention concerns prodrugs whose aromatic oxidation, particularly their enzymatic aromatic hydroxylation, results in their activation by the release of a drug moiety. It particularly concerns anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the P-450 enzyme CYP1B1. Also provided are methods of detection of aromatic oxidation activity.

Hydroxylation activated drug release

The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.

Hydroxylation activated prodrugs

The present invention concerns enzymatic aromatic hydroxylation-activated prodrugs, particularly anti-tumour prodrugs and those which are specifically activated by the hydroxylation activity of the enzyme CYP1B1.

The discovery that Cyp1B1 protein is detectable in a wide range of human cancers of different histogenetic types, but is not detectable in non-cancerous tissues, gives rise to diagnostic methods for detecting tumors based on this protein as a marker, and to the possibility of tumor therapies involving the protein. A diagnostic method may include the steps of: (a) obtaining from a patient a tissue sample to be tested for the presence of cancer cells; (b) producing a prepared sample in a sample preparation process; (c) contacting the prepared sample with an antibody that reacts with human Cyp1B1 protein; and (d) detecting binding of the antibody to CYP1B1 protein in the prepared sample.

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Leicester, United Kingdom

Michael Danny Burke