A series of novel small molecule inhibitors of matriptase, a trypsin-like serine protease, might provide a route to prevent tumour metastasis and invasive growth
Curacyte, a Munich-based drug development company focused on novel treatments of inflammatory diseases, thrombotic disorders and cancer, has announced that its scientists have discovered a series of novel small molecule inhibitors of matriptase, a trypsin-like serine protease.
Matriptase is an important mediator in the degradation of the extracellular matrix, a process which plays a key role during metastasis.
Inhibiting this key enzyme produced by tumour cells might provide a route to prevent tumour metastasis and invasive growth.
This compound series thus offers potential as novel anti-tumour agents for the treatment of metastatic malignancies and Curacyte will now move this programme into pre-clinical development.
Since the discovery of the gene in 1999, matriptase has increasingly gained attention as a potential biological target for inhibiting tumour spread.
Today, matriptase is recognised as an innovative anti-cancer target.
In in-vitro assays, the Curacyte inhibitor series exhibit excellent affinity and selectivity towards the target and a pharmacokinetic profile that supports their use as pharmaceutically active substances. Helmut Giersiefen, chief executive officer of Curacyte, commented on the recent scientific success: "The discovery of the matriptase inhibitors corroborates the validity and value of our protease technology.
Based on our proprietary inhibitor libraries and our competence with respect to the chemistry of these substances, we have identified a series of novel potential anti-tumour agents, enabling us to move another important project into preclinical development.
We will continue to derive therapeutically valuable applications from our protease technology that we can leverage with pharmaceutical partners." Curacyte pursues the development of its protease technology in close collaboration with the Center of Vascular Biology and Medicine of the University of Jena (Germany) under the leadership of Jörg Stürzebecher, a well-known pioneer in the area of synthetic inhibitors of serine proteases.
"We are very proud of our collaboration with Curacyte," commented Dr Stürzebecher.
"The successful development of these matriptase inhibitors was possible by combining our knowledge of the structure-function relationship of protease inhibitors that we gained over decades with the competence in drug discovery and pharmaceutical development provided by Curacyte.
Our collaboration on protease inhibitors, including matriptase has been ongoing for over two years and establishes a benchmark for the fruitful synergies that can be created by bringing together academic and commercial competencies."
