Tankyrases (TNKSs) are poly(ADP-ribose)polymerases (PARPs) that are overexpressed in several clinical cancers. They regulate elongation of telomeres, regulate the Wnt system, and are essential for the function of the mitotic spindle. A set of 2-arylquinazolin-4-ones has been designed and identified as potent and selective TNKS inhibitors, some being more potent and selective than the lead inhibitor XAV939, with IC50 = 3 nM vs. TNKS-2. Methyl was preferred at the 8-position and modest bulk at the 4-position of the 2-phenyl group; electronic effects and H-bonding were irrelevant, but charge in the 4′-substituent must be avoided. Molecular modeling facilitated initial design of the compounds and rationalization of the SAR of binding into the...
Tankyrases 1 and 2 are members of the poly(ADP-ribose) polymerase (PARP) family of enzymes that mod...
The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis...
Tankyrase 1 and 2 (TNKS1/2) catalyze post-translational modification by poly-ADP-ribosylation of a p...
Tankyrases (TNKSs) are poly(ADP-ribose)polymerases (PARPs) that are overexpressed in several clini...
Tankyrases (TNKSs), members of the PARP (Poly(ADP-ribose)polymerases) superfamily of enzymes, have g...
Tankyrases-1 and -2 (TNKS-1 and TNKS-2) have three cellular roles which make them important targets ...
Tankyrases-1 and -2 (TNKS-1 and TNKS-2) have three cellular roles which make them important targets ...
Tankyrases (TNKSs) have recently gained great consideration as potential targets in Wnt/β-catenin pa...
Tankyrase (TNKS1 and TNKS2) is a promising target in anti-cancer drug discovery due to its role in r...
Abstract Tankyrases (TNKSs) are enzymes specialized in catalyzing poly-ADP-ribosylation of target p...
Tankyrases (TNKS1 and TNKS2) are proteins in the poly ADP-ribose polymerase (PARP) family. They have...
Tankyrase (TNKS) is a poly-ADP-ribosylating protein (PARP) whose activity suppresses cellular axin p...
The canonical WNT pathway plays an important role in cancer pathogenesis. Inhibition of poly(ADP-ri...
Aberrant activation of the Wnt pathway has been implicated in the development and formation of many ...
Tankyrase 1 and 2 (TNKS1/2) catalyze post-translational modification by poly-ADP-ribosylation of a p...
Tankyrases 1 and 2 are members of the poly(ADP-ribose) polymerase (PARP) family of enzymes that mod...
The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis...
Tankyrase 1 and 2 (TNKS1/2) catalyze post-translational modification by poly-ADP-ribosylation of a p...
Tankyrases (TNKSs) are poly(ADP-ribose)polymerases (PARPs) that are overexpressed in several clini...
Tankyrases (TNKSs), members of the PARP (Poly(ADP-ribose)polymerases) superfamily of enzymes, have g...
Tankyrases-1 and -2 (TNKS-1 and TNKS-2) have three cellular roles which make them important targets ...
Tankyrases-1 and -2 (TNKS-1 and TNKS-2) have three cellular roles which make them important targets ...
Tankyrases (TNKSs) have recently gained great consideration as potential targets in Wnt/β-catenin pa...
Tankyrase (TNKS1 and TNKS2) is a promising target in anti-cancer drug discovery due to its role in r...
Abstract Tankyrases (TNKSs) are enzymes specialized in catalyzing poly-ADP-ribosylation of target p...
Tankyrases (TNKS1 and TNKS2) are proteins in the poly ADP-ribose polymerase (PARP) family. They have...
Tankyrase (TNKS) is a poly-ADP-ribosylating protein (PARP) whose activity suppresses cellular axin p...
The canonical WNT pathway plays an important role in cancer pathogenesis. Inhibition of poly(ADP-ri...
Aberrant activation of the Wnt pathway has been implicated in the development and formation of many ...
Tankyrase 1 and 2 (TNKS1/2) catalyze post-translational modification by poly-ADP-ribosylation of a p...
Tankyrases 1 and 2 are members of the poly(ADP-ribose) polymerase (PARP) family of enzymes that mod...
The canonical Wnt pathway plays an important role in embryonic development, adult tissue homeostasis...
Tankyrase 1 and 2 (TNKS1/2) catalyze post-translational modification by poly-ADP-ribosylation of a p...