Abstract:
:Screening for inhibitors of DNA-dependent protein kinase (DNA-PK) revealed 3-cyano-5-(4-pyridyl)-6-hydrazonomethyl-2-pyridone, designated OK-1035, to be a potent and selective inhibitor. When a synthetic peptide was used as a substrate, OK-1035 caused 50% inhibition of DNA-PK activity at 8 microM, a concentration more than 50 times lower than those required against seven other protein kinases tested. OK-1035 inhibited the phosphorylation by DNA-PK of consensus peptide as well as that of recombinant human wild type-p53. Kinetic studies indicated that OK-1035 inhibited DNA-PK activity in an ATP-competitive manner.
journal_name
Biochem Biophys Res Communjournal_title
Biochemical and biophysical research communicationsauthors
Take Y,Kumano M,Hamano Y,Fukatsu H,Teraoka H,Nishimura S,Okuyama Adoi
10.1006/bbrc.1995.2431subject
Has Abstractpub_date
1995-10-04 00:00:00pages
41-7issue
1eissn
0006-291Xissn
1090-2104pii
S0006-291X(85)72431-Xjournal_volume
215pub_type
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