[HTML][HTML] Roscovitine in cancer and other diseases

J Cicenas, K Kalyan, A Sorokinas… - Annals of …, 2015 - ncbi.nlm.nih.gov
Abstract Roscovitine [CY-202,(R)-Roscovitine, Seliciclib] is a small molecule that inhibits
cyclin-dependent kinases (CDKs) through direct competition at the ATP-binding site. It is a …

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 …

Roscovitine Targets, Protein Kinases and Pyridoxal Kinase*[Boxs]

S Bach, M Knockaert, J Reinhardt, O Lozach… - Journal of Biological …, 2005 - ASBMB
(R)-Roscovitine (CYC202) is often referred to as a" selective inhibitor of cyclin-dependent
kinases." Besides its use as a biological tool in cell cycle, neuronal functions, and apoptosis …

Roscovitine regulates invasive breast cancer cell (MDA-MB231) proliferation and survival through cell cycle regulatory protein cdk5

S Goodyear, MC Sharma - Experimental and molecular pathology, 2007 - Elsevier
Roscovitine, a purine analogue, has been considered for the treatment of cancer. Anti-
cancer therapeutic efficacy is being evaluated in clinical trials. However, the mechanisms …

The Cyclin-dependent Kinase Inhibitor CYC202 (R-Roscovitine) Inhibits Retinoblastoma Protein Phosphorylation, Causes Loss of Cyclin D1, and Activates the …

SR Whittaker, MI Walton, MD Garrett, P Workman - Cancer research, 2004 - AACR
Deregulation of the cell cycle commonly occurs during tumorigenesis, resulting in
unrestricted cell proliferation and independence from mitogens. Cyclin-dependent kinase …

Phase I evaluation of seliciclib (R-roscovitine), a novel oral cyclin-dependent kinase inhibitor, in patients with advanced malignancies

C Le Tourneau, S Faivre, V Laurence… - European journal of …, 2010 - Elsevier
AIM: Phase I study of seliciclib (CYC202, R-roscovitine), an inhibitor of cyclin-dependent
kinases 2, 7 and 9, causing cell cycle changes and apoptosis in cancer cells. PATIENTS …

Cyclin-dependent kinase inhibitor Roscovitine induces apoptosis in chronic lymphocytic leukemia cells

IN Hahntow, F Schneller, M Oelsner, K Weick… - Leukemia, 2004 - nature.com
A new class of cell cycle inhibitors is currently entering clinical trials. These drugs exert their
activity by inhibition of cyclin-dependent kinases (cdk) and induce cell cycle arrest and …

Pyrazolo[4,3-d]pyrimidine Bioisostere of Roscovitine: Evaluation of a Novel Selective Inhibitor of Cyclin-Dependent Kinases with Antiproliferative Activity

R Jorda, L Havlicek, IW McNae… - Journal of medicinal …, 2011 - ACS Publications
Inhibition of cyclin-dependent kinases (CDKs) with small molecules has been suggested as
a strategy for treatment of cancer, based on deregulation of CDKs commonly found in many …

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 …

[HTML][HTML] Discovery and development of Seliciclib. How systems biology approaches can lead to better drug performance

HS Khalil, V Mitev, T Vlaykova, L Cavicchi… - Journal of …, 2015 - Elsevier
Seliciclib (R-Roscovitine) was identified as an inhibitor of CDKs and has undergone drug
development and clinical testing as an anticancer agent. In this review, the authors describe …