Academy of Finland
Funding decision
Name Lehtiƶ, Lari
Organisation OY
Project title
ADP-ribosyltransferase inhibitors as chemical probes and drugs
Decision No. 294085
Decision date 10.06.2015
Funding period 01.09.2015 - 31.08.2018
Funding 330 000
WebFOCUS Report
Project description
The project aims to develop selective small molecule inhibitors of human ADP-ribosyltransferases. These signaling enzymes attach ADP-ribose units covalently other proteins and themselves and effect critical signaling pathways in the cell. Though their cellular functions ADP-ribosyltransferases have been linked to many human diseases especially to cancer. The methodologies used in the project include screening of compound libraries, protein X-ray rystallography, computational modeling, improvement of the compounds through analogs, profiling of the inhibitor selectivity and evaluation of cellular effects. Developed potent and selective small molecule inhibitors of the enzymes may be used as chemical probes for studying biology, reveal new therapeutic applications in inhibition of the enzymes and they will be potential candidates for cancer drugs.