927426-16-2Relevant academic research and scientific papers
Modulating the interaction between CDK2 and cyclin A with a quinoline-based inhibitor
Deng, Yongqi,Shipps Jr., Gerald W.,Zhao, Lianyun,Siddiqui, M. Arshad,Popovici-Muller, Janeta,Curran, Patrick J.,Duca, Jose S.,Hruza, Alan W.,Fischmann, Thierry O.,Madison, Vincent S.,Zhang, Rumin,McNemar, Charles W.,Mayhood, Todd W.,Syto, Rosalinda,Annis, Allen,Kirschmeier, Paul,Lees, Emma M.,Parry, David A.,Windsor, William T.
, p. 199 - 203 (2014/01/17)
A new class of quinoline-based kinase inhibitors has been discovered that both disrupt cyclin dependent 2 (CDK2) interaction with its cyclin A subunit and act as ATP competitive inhibitors. The key strategy for discovering this class of protein-protein disrupter compounds was to screen the monomer CDK2 in an affinity-selection/mass spectrometry-based technique and to perform secondary assays that identified compounds that bound only to the inactive CDK2 monomer and not the active CDK2/cyclin A heterodimer. Through a series of chemical modifications the affinity (Kd) of the original hit improved from 1 to 0.005 μM.
NOVEL HIGH AFFINITY QUINOLINE-BASED KINASE LIGANDS
-
, (2014/01/09)
Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
Novel high affinity quinoline-based kinase ligands
-
Page/Page column 100, (2008/06/13)
Quinoline-based inhibitors of cyclin dependent kinase 2, compositions including the inhibitors, and methods of using the inhibitors and inhibitor compositions are described. The inhibitors and compositions including them are useful for treating disease or disease symptoms. The invention also provides for methods of making CDK-2 inhibitor compounds, methods of inhibiting CDK-2, and methods for treating disease or disease symptoms.
