CAK—cyclin-dependent activating kinase: a key kinase in cell cycle control and a target for drugs?

G Lolli, LN Johnson - Cell cycle, 2005 - Taylor & Francis
The Cyclin-dependent kinase (CDK) Activating Kinase (CAK) is responsible for the
activating phosphorylation of CDK1, CDK2, CDK4 and CDK6 and regulation of the cell …

Recent progress in CDK4/6 inhibitors and PROTACs

H Wang, J Ba, Y Kang, Z Gong, T Liang, Y Zhang, J Qi… - Molecules, 2023 - mdpi.com
Cell division in eukaryotes is a highly regulated process that is critical to the life of a cell.
Dysregulated cell proliferation, often driven by anomalies in cell Cyclin-dependent kinase …

Novel mutant-selective EGFR kinase inhibitors against EGFR T790M

W Zhou, D Ercan, L Chen, CH Yun, D Li, M Capelletti… - Nature, 2009 - nature.com
The clinical efficacy of epidermal growth factor receptor (EGFR) kinase inhibitors in EGFR-
mutant non-small-cell lung cancer (NSCLC) is limited by the development of drug-resistance …

Specific inhibition of cyclin-dependent kinase 4/6 by PD 0332991 and associated antitumor activity in human tumor xenografts

DW Fry, PJ Harvey, PR Keller, WL Elliott… - Molecular cancer …, 2004 - AACR
PD 0332991 is a highly specific inhibitor of cyclin-dependent kinase 4 (Cdk4)(IC50, 0.011
μmol/L) and Cdk6 (IC50, 0.016 μmol/L), having no activity against a panel of 36 additional …

N-(5-Chloro-1,3-benzodioxol-4-yl)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5- (tetrahydro-2H-pyran-4-yloxy)quinazolin-4-amine, a Novel, Highly Selective, Orally …

LF Hennequin, J Allen, J Breed, J Curwen… - Journal of medicinal …, 2006 - ACS Publications
Src family kinases (SFKs) are nonreceptor tyrosine kinases that are reported to be critical for
cancer progression. We report here a novel subseries of C-5-substituted anilinoquinazolines …

Substantial improvements in large-scale redocking and screening using the novel HYDE scoring function

N Schneider, S Hindle, G Lange, R Klein… - Journal of computer …, 2012 - Springer
The HYDE scoring function consistently describes hydrogen bonding, the hydrophobic effect
and desolvation. It relies on HYdration and DEsolvation terms which are calibrated using …

The crystal structure of human CDK7 and its protein recognition properties

G Lolli, ED Lowe, NR Brown, LN Johnson - Structure, 2004 - cell.com
CDK7, a member of the cyclin-dependent protein kinase family, regulates the activities of
other CDKs through phosphorylation on their activation segment and hence contributes to …

In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00

KS Joshi, MJ Rathos, RD Joshi, M Sivakumar… - Molecular cancer …, 2007 - AACR
Cyclin-dependent kinases (Cdk) and their associated pathways represent some of the most
attractive targets for the development of anticancer therapeutics. Based on antitumor activity …

A class of 2, 4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B

I Aliagas-Martin, D Burdick, L Corson… - Journal of medicinal …, 2009 - ACS Publications
The two major Aurora kinases carry out critical functions at distinct mitotic stages. Selective
inhibitors of these kinases, as well as pan-Aurora inhibitors, show antitumor efficacy and are …

Probing cell-division phenotype space and Polo-like kinase function using small molecules

U Peters, J Cherian, JH Kim, BH Kwok… - Nature chemical …, 2006 - nature.com
Cell-permeable small molecules that inhibit their targets on fast timescales are powerful
probes of cell-division mechanisms. Such inhibitors have been identified using phenotype …