G007-LK

G007-LK is a potent and selective small-molecule inhibitor of tankyrase 1 (TNKS1) and tankyrase 2 (TNKS2). It functions by binding to the adenosine pocket of the tankyrase PARP domain, which prevents the poly-ADP-ribosylation of AXIN proteins. This stabilization of AXIN leads to the degradation of β-catenin, thereby inhibiting the WNT/β-catenin signaling pathway. G007-LK also modulates YAP signaling. Preclinical research indicates that G007-LK can overcome resistance to immune checkpoint inhibitors, such as anti-PD-1 antibodies, in melanoma by promoting T-cell infiltration and enhancing the anti-tumor immune microenvironment.