June 20, 2019

Potential probe for early ovarian cancer

Larry Marnett and colleagues have developed what may become the first agent for targeted PET imaging of cancer tissues, such as ovarian cancer, that express high levels of the COX-1 enzyme.

Ovarian cancer is the fifth leading cause of cancer death in women and one of the most difficult malignancies to detect at an early stage.

Emerging clinical evidence suggests that the enzyme cyclooxygenase-1 (COX-1) contributes significantly to tumorigenesis in ovarian cancer. Thus COX-1 could serve as a novel target for molecular imaging probes to improve early detection and response to treatment.

Now in the American Chemical Society journal ACS Omega, Md. Jashim Uddin, PhD, Lawrence Marnett, PhD, and colleagues report the discovery of FDF, a furanone-based novel COX-1 selective inhibitor with adequate properties to enable its use for in vivo imaging.

In two distinct animal models of ovarian cancer, xenografts expressing high levels of COX-1 demonstrated targeted uptake of the compound containing the F-18 radioisotope (18F-FDF) compared to tissues expressing low protein levels.

This indicates that 18F-FDF may be the first feasible radiotracer validated for targeted PET/CT imaging of neoplastic tissues that express elevated levels of the COX-1 enzyme.

The work was featured in the journal as an ACS Editors’ Choice and was supported by grants from the National Institutes of Health (CA128323, CA182850, CA136465, CA089450) and Kay Yow Cancer Fund/V Foundation.