- Abstract:
-
The small molecule, 2-(1-hydroxyundecyl)-1-(4-nitrophenylamino)-6-phenyl-6,7a-dihydro-1H-pyrrolo[3,4-b]pyridine-5,7(2H,4aH)-dione (A12B4C3), is a potent inhibitor of the phosphatase activity of human polynucleotide kinase/phosphatase (PNKP) in vitro. Kinetic analysis revealed that A12B4C3 acts as a noncompetitive inhibitor, and this was confirmed by fluorescence quenching, which showed that the inhibitor can form a ternary complex with PNKP and a DNA substrate, i.e. A12B4C3 does not prevent D...
Expand abstract - Publication status:
- Published
- Publisher copy:
- 10.1074/jbc.m109.055764
-
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- Journal:
- The Journal of biological chemistry
- Volume:
- 285
- Issue:
- 4
- Pages:
- 2351-2360
- Publication date:
- 2010-01-05
- DOI:
- EISSN:
-
1083-351X
- ISSN:
-
0021-9258
- URN:
-
uuid:69658b0a-5133-4518-aec4-7f60412e4767
- Source identifiers:
-
131065
- Local pid:
- pubs:131065
- Language:
- English
- Keywords:
- Copyright date:
- 2010
Journal article
Mechanism of action of an imidopiperidine inhibitor of human polynucleotide kinase/phosphatase.
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