Pharmacological inhibitors of cyclin-dependent kinases

M Knockaert, P Greengard, L Meijer - Trends in pharmacological sciences, 2002 - cell.com
Cyclin-dependent kinases (CDKs) regulate the cell division cycle, apoptosis, transcription
and differentiation in addition to functions in the nervous system. Deregulation of CDKs in …

Structural biology in drug design: selective protein kinase inhibitors

G Scapin - Drug discovery today, 2002 - Elsevier
Protein kinases have a fundamental role in signal transduction pathways, and aberrant
kinase activity has been observed in many diseases. In recent years, kinase inhibition has …

Discovery of a potent and selective inhibitor of cyclin-dependent kinase 4/6

PL Toogood, PJ Harvey, JT Repine… - Journal of medicinal …, 2005 - ACS Publications
A pharmacological approach to inhibition of cyclin-dependent kinases 4 and 6 (Cdk4/6)
using highly selective small molecule inhibitors has the potential to provide novel cancer …

Paullones are potent inhibitors of glycogen synthase kinase‐3β and cyclin‐dependent kinase 5/p25

M Leost, C Schultz, A Link, YZ Wu… - European journal of …, 2000 - Wiley Online Library
Paullones constitute a new family of benzazepinones with promising antitumoral properties.
They were recently described as potent, ATP‐competitive, inhibitors of the cell cycle …

Structural characterization of the GSK-3β active site using selective and non-selective ATP-mimetic inhibitors

JA Bertrand, S Thieffine, A Vulpetti, C Cristiani… - Journal of molecular …, 2003 - Elsevier
GSK-3β is a regulatory serine/threonine kinase with a plethora of cellular targets.
Consequently, selective small molecule inhibitors of GSK-3β may have a variety of …

Genomic-scale measurement of mRNA turnover and the mechanisms of action of the anti-cancer drug flavopiridol

LT Lam, OK Pickeral, AC Peng, A Rosenwald, EM Hurt… - Genome biology, 2001 - Springer
Background Flavopiridol, a flavonoid currently in cancer clinical trials, inhibits cyclin-
dependent kinases (CDKs) by competitively blocking their ATP-binding pocket. However …

Oxindole-based inhibitors of cyclin-dependent kinase 2 (CDK2): design, synthesis, enzymatic activities, and X-ray crystallographic analysis

HN Bramson, J Corona, ST Davis… - Journal of medicinal …, 2001 - ACS Publications
Two closely related classes of oxindole-based compounds, 1 H-indole-2, 3-dione 3-
phenylhydrazones and 3-(anilinomethylene)-1, 3-dihydro-2 H-indol-2-ones, were shown to …

Pyrido[2,3-d]pyrimidin-7-ones as Specific Inhibitors of Cyclin-Dependent Kinase 4

SN VanderWel, PJ Harvey, DJ McNamara… - Journal of medicinal …, 2005 - ACS Publications
Inhibition of the cell cycle kinase, cyclin-dependent kinase-4 (Cdk4), is expected to provide
an effective method for the treatment of proliferative diseases such as cancer. The pyrido [2 …

Regulation of CK2 by phosphorylation and O-GlcNAcylation revealed by semisynthesis

MK Tarrant, HS Rho, Z Xie, YL Jiang, C Gross… - Nature chemical …, 2012 - nature.com
Protein serine-threonine kinase casein kinase II (CK2) is involved in a myriad of cellular
processes including cell growth and proliferation through its phosphorylation of hundreds of …

1-Azakenpaullone is a selective inhibitor of glycogen synthase kinase-3β

C Kunick, K Lauenroth, M Leost, L Meijer… - Bioorganic & medicinal …, 2004 - Elsevier
Kenpaullone derivatives with a modified parent ring system were synthesized in order to
develop kinase inhibitors with enhanced selectivity. Among the novel structures, 1 …