A Simple Isomerization of the Purine Scaffold of a Kinase Inhibitor, Roscovitine, Affords a Four- to Seven-Fold Enhancement of Its Affinity for Four CDKs. Could This Be Traced Back to Conjugation-Induced Stiffenings/Loosenings of Rotational Barriers?

[Image: see text] Roscovitine is an antitumor purine inhibitor of cyclin-dependent kinase CDK5, for which it displays submicromolar affinity. It reached phase IIb clinical trials in 2007. The search for analogues with improved kinase affinities led recently to an isomer, finisterine, having a nearly...

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Détails bibliographiques
Publié dans:ACS Omega
Auteurs principaux: El Hage, Krystel, Piquemal, Jean-Philip, Oumata, Nassima, Meijer, Laurent, Galons, Hervé, Gresh, Nohad
Format: Artigo
Langue:Inglês
Publié: American Chemical Society 2017
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC6044500/
https://ncbi.nlm.nih.gov/pubmed/30023695
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsomega.7b00471
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