Reliable Cancer Therapies

Location: University of Crete (Greece)
Collaboration: Dr. Vasilis Androutsopoulos

Cytochrome P450 (often called CYP) is a large and diverse group of enzymes. They are known to metabolize xenobiotics to conversion products. Cytochrome P450 CYP1A1 and CYP1B1 are two enzymes belonging to this family. It has been shown that CYP1A1 and CYP1B1 are overexpressed in several human cancers and that they are almost not expressed in the corresponding normal tissue. It is clear that these enzymes could become an important target in cancer therapy. Today, there is no specific assay to detect the enzymatic activity of either CYP1A1 or CYP1B1 alone. The final goal is to find molecules which are harmless in their original form, but are converted to cytotoxic molecule by CYP1A1 of CYP1B1 (prodrugs). Therefore, these molecules will only be toxic to cancer cells.

RCT is funding a project in which the potential differences in overexpression between CYP1A1 and CYP1B1 in human tumors is evaluated. The project is based on the development of a CYP1-specific HPLC-assay that can detect active CYP1A1 or CYP1B1 in human tissues, using CYP1-selective substrates. The project will involve determination of specific enzymatic activity of CYP1A1 and CYP1B1 in human tumors.

The project is coordinated by Dr Vasilis Androutsopoulos at the University of Crete (Greece). In this project a number of human tissues derived from endometrial, bladder, breast and colon carcinomas from patients with primary non-metastatic cancer are used for CYP1-activity screening. In vitro experiments are performed at the Medical School of the University of Crete.

The data are currently being analyzed and final results are expected March 2012.

The tumor-specific expression of CYP1A1 and CYP1B1 is the basic concept on which the so called “anti-cancer activity” of salvestroles is based. Since the latter product is heavily marketed, RCT decided it was of prime importance to confirm or contradict the underlying assumption.