Candidate Drug Blocks Enzyme Activity in Pancreatic and Lung Cancer Cells

Cancer researchers have identified a candidate drug that blocks the activity of the serine/threonine-protein kinase TBK1 (TANK-binding kinase 1), an enzyme overexpressed in some pancreatic and non-small-cell lung cancers.

Investigators at the University of Texas Southwestern Medical Center (Dallas, USA) screened more than 250,000 compounds while searching for any that could inhibit this enzyme and eliminate the survival advantage that it gives to cancer cells through its activation of Akt, a serine/threonine protein kinase that plays a key role in multiple cellular processes such as glucose metabolism, cell proliferation, apoptosis, transcription, and cell migration.

A paper published in the February 18, 2011, issue of the journal Molecular Cell identified the potential drug as 6-aminopyrazolopyrimidine, a compound that had been developed in collaboration with the pharmaceutical company Amgen (Thousand Oaks, CA, USA). More...