Roscovitine-derived, dual-specificity inhibitors of cyclin-dependent kinases and casein kinases 1

N Oumata, K Bettayeb, Y Ferandin… - Journal of medicinal …, 2008 - ACS Publications
Cyclin-dependent kinases (CDKs) and casein kinases 1 (CK1) are involved in the two key
molecular features of Alzheimer's disease, production of amyloid-β peptides (extracellular …

Potent inhibitors of CDK5 derived from roscovitine: Synthesis, biological evaluation and molecular modelling

L Demange, FN Abdellah, O Lozach, Y Ferandin… - Bioorganic & medicinal …, 2013 - Elsevier
Cyclin dependent kinase 5 (CDK5) is a serine/threonine kinase belonging to the cyclin
dependent kinase (CDK) family. CDK5 is involved in numerous neuronal diseases …

Molecular model of cyclin-dependent kinase 5 complexed with roscovitine

WF de Azevedo Jr, RT Gaspar, F Canduri… - Biochemical and …, 2002 - Elsevier
Here is described a structural model for the binary complex CDK5–roscovitine. Roscovitine
has been shown to potently inhibit cyclin-dependent kinases 1, 2 and 5 (CDK1, 2, and 5) …

Structural basis for the interaction between casein kinase 1 delta and a potent and selective inhibitor

A Long, H Zhao, X Huang - Journal of medicinal chemistry, 2012 - ACS Publications
Casein kinase 1 delta (CK1δ) and its closest homologue CK1ε are key regulators of diverse
cellular growth and survival processes such as Wnt signaling, DNA repair, and circadian …

Inhibition of cyclin‐dependent kinases by purine analogues: crystal structure of human cdk2 complexed with roscovitine

WF De Azevedo, S Leclerc, L Meijer… - European journal of …, 1997 - Wiley Online Library
Cyclin‐dependent kinases (cdk) control the cell division cycle (cdc). These kinases and their
regulators are frequently deregulated in human tumours. A potent inhibitor of cdks …

Mechanism of CDK5/p25 binding by CDK inhibitors

M Mapelli, L Massimiliano, C Crovace… - Journal of medicinal …, 2005 - ACS Publications
The cyclin-dependent kinases (CDK) CDK1, CDK2, CDK4, and CDK6 are serine/threonine
protein kinases targeted in cancer therapy due to their role in cell cycle progression. The …

A review on cyclin-dependent kinase 5: An emerging drug target for neurodegenerative diseases

S Batra, S Jahan, A Ashraf, B Alharby, T Jawaid… - International Journal of …, 2023 - Elsevier
Abstract Cyclin-dependent kinase 5 (CDK5) is the serine/threonine-directed kinase mainly
found in the brain and plays a significant role in developing the central nervous system …

Pyrazolo[1,5-a]-1,3,5-triazine as a Purine Bioisostere: Access to Potent Cyclin-Dependent Kinase Inhibitor (R)-Roscovitine Analogue

F Popowycz, G Fournet, C Schneider… - Journal of medicinal …, 2009 - ACS Publications
Pharmacological inhibitors of cyclin-dependent kinases (CDKs) have a wide therapeutic
potential. Among the CDK inhibitors currently under clinical trials, the 2, 6, 9-trisubstituted …

Structure-based design of a potent purine-based cyclin-dependent kinase inhibitor

TG Davies, J Bentley, CE Arris, FT Boyle… - Nature structural …, 2002 - nature.com
Aberrant control of cyclin-dependent kinases (CDKs) is a central feature of the molecular
pathology of cancer. Iterative structure-based design was used to optimize the ATP …

CR8, a potent and selective, roscovitine-derived inhibitor of cyclin-dependent kinases

K Bettayeb, N Oumata, A Echalier, Y Ferandin… - Oncogene, 2008 - nature.com
Among the ten pharmacological inhibitors of cyclin-dependent kinases (CDKs) currently in
clinical trials, the purine roscovitine (CYC202, Seliciclib) is undergoing phase 2 trials against …