Recent advances in the structure-based rational design of TNKSIs
Abstract
Human tankyrases 1 and 2 (TNKS1/2) are attractive pharmacological biotargets, especially for the treatment of specific types of cancer. This article provides a fairly comprehensive overview of the structural biology of the TNKS–inhibitor complex and the current medicinal chemistry strategies being used in the structure-based rational design of tankyrase-specific inhibitors.