A Novel Trigger Molecule for the Detection and Treatment of Cancer

University of California System: University of California, San Francisco
posted on 07/01/2010

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BACKGROUND:   In the United States, over 1.5 million new cancer cases are expected to be diagnosed in 2010. It has been long established that early cancer detection is key to successful treatment. However, current methods remain non-specific and insensitive. And unfortunately, even if cancer is detected, there exists few effective cancer therapies that prevent cancer growth and progression. Treatments are needed that can home in on cancer cells and kill them before they proliferate and spread.   A key strategy for advancing the treatment of cancer is to address two large unmet needs – accurate cancer detection and effective targeted therapeutics.   TECHNOLOGY:   Investigators at UCSF have developed a COX-2 sensitive trigger molecule capable of detecting cancerous cells and releasing therapeutic agents to carcinomas and tumors. The trigger molecule has been functionalized and modified to release either activatable fluorescent moieties or anti-cancer agents upon enzymatic catalysis by COX-2, a cyclooxygenase enzyme previously shown to be expressed in a variety of tumors including head and neck, colon, lung, pancreatic and breast cancers.   When activatable fluorescent compounds, bound to the trigger molecule, undergo COX-2 directed cleavage from the trigger, they selectively label the cancerous cells within a tissue or organ. This technology has the added advantage of a high signal to noise ratio, which essential for cancer detection.   UCSF investigators have also taken advantage of the versatility of the novel trigger molecule to develop a novel targeted cancer treatment platform. They have created a method of binding anti-cancer drugs to COX-2 sensitive trigger molecules. This allows for the release of multiple drug molecules into a cancerous cell.

•        Therapeutic agent selectively targets cancer cells to deliver a high payload of cytotoxic drugs
•        Noninvasive optical imaging for early cancer detection and monitoring progression

• Selectively targets COX-2 expressing cancer cells in tissues and organs
• Activatable optical probe with a low signal to noise ratio that improves cancer detection
• Capable of carrying large therapeutic payloads which can be released after a single enzyme interaction