From Roscovitine to CYC202 to Seliciclib – from bench to bedside: discovery and development

• Main Authors: Nikolai Zhelev, Dimitar Trifonov, Shudong Wang, Moustapha Hassan, Ibrahim El Serafi
• Format: Article
• Language: English
• Published: Pensoft Publishers 2013-12-01
• Series: BioDiscovery
• Subjects: Roscovitine; CYC202; Seliciclib; drug discovery an
• Online Access: https://biodiscovery.pensoft.net/article/8956/download/pdf/

This monograph reviews the discovery and development of the cyclin-dependent kinase inhibitor roscovitine (R-roscovitine, CYC202, Seliciclib). The authors summarise the in vitro and in vivo data that have formed the basis for clinical investigation of Seliciclib as an anti-cancer drug. Kinase selectivity, cellular effects and the pharmacological properties of the drug are discussed in addition to the clinical results of Seliciclib being reviewed. Novel results on the effect of the drug in cardiac hypertrophy are summarized and potential applications of Seliciclib in other therapeutic areas, including, inflammation, virology, glomerulonephritis and polycystic kidney disease, are discussed. Finally the authors argue that optimisation of the therapeutic effect of kinase inhibitors such as Seliciclib can be enhanced using a systems biology approach involving mathematical modelling of the molecular pathways regulating cell growth and division.