Structural basis for inhibitor specificity in human poly(ADP-ribose) polymerase-3.
2009 (English)In: Journal of medicinal chemistry, ISSN 1520-4804, Vol. 52, no 9, 3108-11 p.Article in journal (Refereed) Published
Poly(ADP-ribose) polymerases (PARPs) activate DNA repair mechanisms upon stress- and cytotoxin-induced DNA damage, and inhibition of PARP activity is a lead in cancer drug therapy. We present a structural and functional analysis of the PARP domain of human PARP-3 in complex with several inhibitors. Of these, KU0058948 is the strongest inhibitor of PARP-3 activity. The presented crystal structures highlight key features for potent inhibitor binding and suggest routes for creating isoenzyme-specific PARP inhibitors.
Place, publisher, year, edition, pages
2009. Vol. 52, no 9, 3108-11 p.
IdentifiersURN: urn:nbn:se:su:diva-32010DOI: 10.1021/jm900052jISI: 000265911800050PubMedID: 19354255OAI: oai:DiVA.org:su-32010DiVA: diva2:279203