benzothiazole scaffold as versatile nicotinamide mimic allowing nanomolar inhibition of different PARP enzymes
S. Murthy, M. G. Nizi, M. M. Maksimainen, S. Massari, J. Alaviuhkola, B. E. Lippok, C. Vagaggini, S. T. Sowa, A. Galera-Prat, Y. Ashok, H. Venkannagari, R. Prunskaite-Hyyryläinen, E. Dreassi, B. Lüscher, P. Korn, , L. Lehtiö
The paper identifies a benzothiazole scaffold that inhibits multiple PARP enzymes with nanomolar potency, showing selectivity for mono-ARTs and poly-ARTs.
bioRxiv · Aug 29, 2022Biochemistry