NUCLEOSIDE KINASES

Kinases, including Nucleoside Kinases, represent a priority line of action in Medicinal Chemistry. Our research group has developed a family of acyclic nucleosides as human TK-2 inhibitors. This enzyme plays an important role in the mitochondrial DNA synthesis and has been associated with severe mitochondrial disorders that are being intensively studied. Regarding this issue, one of our inhibitors, namely KIN109, has been considered as a valuable tool to determine TK-2 levels in different cellular extracts.

We have also described different acyclic nucleoside derivatives showing inhibitory activity in the submicromolar range against other therapeutically attractive kinase, the thymidine monophosphate kinase from Mycobacterium tuberculosis (TMPKmt).

Relevant publications:

• 2010 - Familiar,O.; Munier-Lehman, H.; Aínsa, J. A.; Camarasa, M. J.; Pérez-Pérez, M. J.

  Design, synthesis and inhibitory activity against M. tuberculosis thymidine monophosphate kinase of acyclic nucleoside analogues with a distal imidazoquinolinone. Eur. J. Med. Chem. 2010, 45, 5910-5918.