New anti-tumour agents discovered
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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 onnovel treatments of inflammatory diseases, thrombotic disordersand cancer, has announced that its scientists have discovered aseries of novel small molecule inhibitors of matriptase, atrypsin-like serine protease.
Matriptase is an important mediatorin the degradation of the extracellular matrix, a process whichplays a key role during metastasis.
Inhibiting this key enzymeproduced by tumour cells might provide a route to prevent tumourmetastasis and invasive growth.
This compound series thus offerspotential as novel anti-tumour agents for the treatment ofmetastatic malignancies and Curacyte will now move this programmeinto pre-clinical development.
Since the discovery of the gene in1999, matriptase has increasingly gained attention as a potentialbiological target for inhibiting tumour spread.
Today, matriptaseis recognised as an innovative anti-cancer target.
In in-vitroassays, the Curacyte inhibitor series exhibit excellent affinityand selectivity towards the target and a pharmacokinetic profilethat supports their use as pharmaceutically active substances.Helmut Giersiefen, chief executive officer of Curacyte, commentedon the recent scientific success: "The discovery of thematriptase inhibitors corroborates the validity and value of ourprotease technology.
Based on our proprietary inhibitor librariesand our competence with respect to the chemistry of thesesubstances, we have identified a series of novel potentialanti-tumour agents, enabling us to move another important projectinto preclinical development.
We will continue to derivetherapeutically valuable applications from our proteasetechnology that we can leverage with pharmaceuticalpartners." Curacyte pursues the development of its proteasetechnology in close collaboration with the Center of VascularBiology and Medicine of the University of Jena (Germany) underthe leadership of Jörg Stürzebecher, a well-known pioneer in thearea of synthetic inhibitors of serine proteases.
"We arevery proud of our collaboration with Curacyte," commented DrStürzebecher.
"The successful development of thesematriptase inhibitors was possible by combining our knowledge ofthe structure-function relationship of protease inhibitors thatwe gained over decades with the competence in drug discovery andpharmaceutical development provided by Curacyte.
Ourcollaboration on protease inhibitors, including matriptase hasbeen ongoing for over two years and establishes a benchmark forthe fruitful synergies that can be created by bringing togetheracademic and commercial competencies."