Author/Authors :
Raj N. Misra، نويسنده , , David B. Rawlins، نويسنده , , Hai-yun Xiao، نويسنده , , Weifang Shan، نويسنده , , Isia Bursuker، نويسنده , , Kristin A. Kellar، نويسنده , , Janet G. Mulheron، نويسنده , , John S. Sack، نويسنده , , John S. Tokarski، نويسنده , , S. David Kimball، نويسنده , , Kevin R. Webster، نويسنده ,
Abstract :
1H-Pyrazolo[3,4-b]pyridine 3 (SQ-67563) has been shown to be a potent, selective inhibitor of CDK1/CDK2 in vitro. In cells 3 acts as a cytotoxic agent with the ability to block cell cycle progression and/or induce apoptosis. The solid state structure of 3 bound to CDK2 shows 3 resides coincident with the ATP purine binding site and forms important H-bonding interactions with Leu83 on the protein backbone.