RGD Reference Report - Roscovitine targets, protein kinases and pyridoxal kinase. - Rat Genome Database

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Roscovitine targets, protein kinases and pyridoxal kinase.

Authors: Bach, S  Knockaert, M  Reinhardt, J  Lozach, O  Schmitt, S  Baratte, B  Koken, M  Coburn, SP  Tang, L  Jiang, T  Liang, DC  Galons, H  Dierick, JF  Pinna, LA  Meggio, F  Totzke, F  Schachtele, C  Lerman, AS  Carnero, A  Wan, Y  Gray, N  Meijer, L 
Citation: Bach S, etal., J Biol Chem. 2005 Sep 2;280(35):31208-19. Epub 2005 Jun 23.
RGD ID: 2303026
Pubmed: PMID:15975926   (View Abstract at PubMed)
DOI: DOI:10.1074/jbc.M500806200   (Journal Full-text)

(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 studies, it is currently evaluated as a potential drug to treat cancers, neurodegenerative diseases, viral infections, and glomerulonephritis. We have investigated the selectivity of (R)-roscovitine using three different methods: 1) testing on a wide panel of purified kinases that, along with previously published data, now reaches 151 kinases; 2) identifying roscovitine-binding proteins from various tissue and cell types following their affinity chromatography purification on immobilized roscovitine; 3) investigating the effects of roscovitine on cells deprived of one of its targets, CDK2. Altogether, the results show that (R)-roscovitine is rather selective for CDKs, in fact most kinases are not affected. However, it binds an unexpected, non-protein kinase target, pyridoxal kinase, the enzyme responsible for phosphorylation and activation of vitamin B6. These results could help in interpreting the cellular actions of (R)-roscovitine but also in guiding the synthesis of more selective roscovitine analogs.



Gene Ontology Annotations    Click to see Annotation Detail View

Molecular Function

  
Object SymbolSpeciesTermQualifierEvidenceWithNotesSourceOriginal Reference(s)
PdxkRatorganic cyclic compound binding enablesIPIseliciclib RGD 
PdxkRatsmall molecule binding  IPIseliciclib RGD 

Objects Annotated

Genes (Rattus norvegicus)
Pdxk  (pyridoxal kinase)


Additional Information