EP 1042509 A1 20001011 - METHODS OF USING OLIGONUCLEOTIDE ARRAYS TO SEARCH FOR NEW KINASE INHIBITORS
Title (en)
METHODS OF USING OLIGONUCLEOTIDE ARRAYS TO SEARCH FOR NEW KINASE INHIBITORS
Title (de)
VERFAHREN DURCH GEBRAUCH AN OLIGONUKLEOTIDARRAYS ZUM SUCHEN VON NEUEN KINASE-INHIBITOREN
Title (fr)
TECHNIQUES PERMETTANT D'UTILISER DES BANQUES CHIMIQUES POUR RECHERCHER DE NOUVEAUX INHIBITEURS DES KINASES
Publication
Application
Priority
- US 9827405 W 19981223
- US 6879897 P 19971224
Abstract (en)
[origin: WO9934018A1] The generation of selective inhibitors for specific protein kinases would provide new tools for analyzing signal transduction pathways and possibly new therapeutic agents. We have invented an approach to the development of selective protein kinase inhibitors based on the unexpected binding mode of 2,6,9-trisubstituted purines to the ATP binding site of human CDK2. The most potent inhibitor, purvalanol B (IC50 = 6 nM), binds with a 30-fold greater affinity than the known CDK2 inhibitor, flavopiridol. The cellular effects of this class of compounds were examined and compared to those of flavopiridol by monitoring changes in mRNA expression levels for all genes in treated cells of Saccharomyces cerevisiae using high-density oligonucleotide probe arrays.
IPC 1-7
IPC 8 full level
A61K 31/52 (2006.01); C07D 473/16 (2006.01); C12Q 1/68 (2006.01); C12Q 1/6809 (2018.01); C12Q 1/6837 (2018.01); C12Q 1/6886 (2018.01)
CPC (source: EP)
A61K 31/52 (2013.01); C07D 473/16 (2013.01); C12Q 1/6809 (2013.01); C12Q 1/6837 (2013.01); C12Q 1/6886 (2013.01); C12Q 2600/136 (2013.01); C12Q 2600/158 (2013.01)
Citation (search report)
See references of WO 9934018A1
Designated contracting state (EPC)
AT BE CH CY DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE
DOCDB simple family (publication)
WO 9934018 A1 19990708; AU 2010399 A 19990719; EP 1042509 A1 20001011
DOCDB simple family (application)
US 9827405 W 19981223; AU 2010399 A 19981223; EP 98964881 A 19981223