[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 …
development and clinical testing as an anticancer agent. In this review, the authors describe …
[PDF][PDF] From Roscovitine to CYC202 to Seliciclib–from bench to bedside: discovery and development
This monograph reviews the discovery and development of the cyclin-dependent kinase
inhibitor roscovitine (R-roscovitine, CYC202, Seliciclib). The authors summarise the in vitro …
inhibitor roscovitine (R-roscovitine, CYC202, Seliciclib). The authors summarise the in vitro …
The cyclin-dependent kinase inhibitor seliciclib (R-roscovitine; CYC202) decreases the expression of mitotic control genes and prevents entry into mitosis
SR Whittaker, RH Te Poele, F Chan, S Linardopoulos… - Cell Cycle, 2007 - Taylor & Francis
The cyclin-dependent kinase (CDK) inhibitor seliciclib (R-roscovitine, CYC202) shows
promising antitumor activity in preclinical models and is currently undergoing phase II …
promising antitumor activity in preclinical models and is currently undergoing phase II …
Seliciclib in malignancies
Cyclins and cyclin-dependent kinases (CDK) form a key part of the regulatory proteins that
govern the cell cycle. Aberrancy in their function can lead to uncontrolled growth and …
govern the cell cycle. Aberrancy in their function can lead to uncontrolled growth and …
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 …
kinases 2, 7 and 9, causing cell cycle changes and apoptosis in cancer cells. PATIENTS …
Seliciclib, a cell-cycle modulator that acts through the inhibition of cyclin-dependent kinases
RC Jackson, AL Barnett, SJ McClue… - Expert Opinion on Drug …, 2008 - Taylor & Francis
Seliciclib is an inhibitor of cyclin-dependent kinases 2, 7 and 9. Its primary mechanism of
action is the inhibition of transcription, resulting in the selective downregulation of rapidly …
action is the inhibition of transcription, resulting in the selective downregulation of rapidly …
[HTML][HTML] Roscovitine in cancer and other diseases
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 …
cyclin-dependent kinases (CDKs) through direct competition at the ATP-binding site. It is a …
A phase I trial of the selective oral cyclin-dependent kinase inhibitor seliciclib (CYC202; R-Roscovitine), administered twice daily for 7 days every 21 days
C Benson, J White, J De Bono, A O'Donnell… - British journal of …, 2007 - nature.com
Abstract Seliciclib (CYC202; R-roscovitine) is the first selective, orally bioavailable inhibitor
of cyclin-dependent kinases 1, 2, 7 and 9 to enter clinical trial. Preclinical studies showed …
of cyclin-dependent kinases 1, 2, 7 and 9 to enter clinical trial. Preclinical studies showed …
Metabolism of the trisubstituted purine cyclin-dependent kinase inhibitor seliciclib (R-roscovitine) in vitro and in vivo
SJ McClue, I Stuart - Drug metabolism and disposition, 2008 - ASPET
Seliciclib (R-roscovitine, CYC202) is a small molecule inhibitor of cyclin-dependent kinases
currently in phase II clinical trials as an anticancer agent. We examined the metabolism of …
currently in phase II clinical trials as an anticancer agent. We examined the metabolism of …
Seliciclib (CYC202, R‐roscovitine) enhances the antitumor effect of doxorubicin in vivo in a breast cancer xenograft model
MVCL Appleyard, MA O'Neill, KE Murray… - … journal of cancer, 2009 - Wiley Online Library
We sought to determine whether seliciclib (CYC202, R‐roscovitine) could increase the
antitumor effects of doxorubicin, with no increase in toxicity, in an MCF7 breast cancer …
antitumor effects of doxorubicin, with no increase in toxicity, in an MCF7 breast cancer …