Kinases and HIV
at kinase inhibitors as treatments for HIV; assays and lead
compounds identified.
Two European drug discovery companies - BioFocus and Axxima Pharmaceuticals - claim to have made an advance in the fight against HIV with the development of assays for novel drug targets.
UK-based BioFocus and Germany's Axxima have been collaborating on HIV research since July 2002 in a project focusing on the identification of kinases that could act as targets for small-molecule HIV drugs. They have developed a number of assays for the kinases and identified lead compounds against one of the most promising kinase targets.
The leads originated from BioFocus' SoftFocus kinase-directed compound collection. The milestone was triggered by Axxima's acceptance of the compounds identified in the collaboration and its decision to pursue a programme of lead optimisation with BioFocus.
The goal of the collaboration is to generate pre-clinical anti-HIV candidates on which Axxima can perform further development. Achievement of this key research milestone will result in a cash payment to BioFocus, which is also entitled to receive ongoing research fees, milestone payments and royalties should any products reach the market.
Kinases are emerging as a new target for HIV drugs, which to date are treated with enzyme inhibitors (targeting HIV protease and reverse transcriptase) and latterly Roche and Trimeris' Fuzeon (enfuvirtide), which acts by blocking the binding of HIV particles to a receptor on the surface of host cells.
Cyclin-dependent kinases, for example, are known to be involved in HIV replication, and two inhibitors of these enzymes (flavopiridol and roscovitine) are already in clinical trials for cancer and could be looked at as anti-viral agents.