Novel Cathepsin Targeted Agents for Molecular Imaging of Cancer and Atherosclerosis

Blum Galia, HUJI, School of Medicine - IMRIC, School of Pharmacy- Institute for Drug Research


X-ray computed tomography (CT) instruments are among the most available, efficient and cost-effective imaging modalities in hospitals. The field of CT molecular imaging agents is emerging relying mainly on detection of gold and bismuth nanoparticles, iodine and gadolinium labeled compounds. However, the low sensitivity of CT scanners to contrast reagents makes this a challenging task.

Our Innovation

The inventors have developed novel chemical routes for the synthesis of compounds that involve solid and solution phase chemistries, which provides the means for increasing the number of imaging moieties on a single compound, and achieve an informative and accurate CT signal. 

Application for use:

The major causes of death in the Western world are cardiovascular diseases and cancer. More accurate detection of these diseases will improve clinical outcomes.

The compounds of the invention may be utilized in a variety of applications: in CT imaging, in the diagnosis of a pathological condition characterized by increased cathepsin, and others. The compound also be utilized for imaging a region or organ after or during treatment. This helps to assess the severity of the disease (e.g. enabling determination of treatment effectiveness and continued treatment approach). 


These novel probes enable detection of the elevated cathepsin activity within cancerous tissue using a CT instrument.           


Figure 1 GNP–based compounds; TEM images of 100nm                                    

Research Outlook

Compounds of the invention selectively recognize a target enzyme, present either within a cell or secreted from cells, and undergo interaction with the target enzyme. By conjugation or enzyme association at locations of high enzyme expression, a sufficient CT signal (above normal tissue background) from multiple imaging moieties may be detected, enabling accurate localization of the target enzyme. The enzyme localities are typically indicative of a condition associated with increased expression of the enzyme, e.g., a cathepsin. Such accumulation of compounds of the invention in such locations results in an amplified imaging signal, which provides an indication of a pathology.


Figure 2 Docking of a novel fluorescent probes to its target cathepsin L



Patent Status

Granted Europe

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Mel Larrosa
VP Business Development Healthcare
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