6-Oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro

Authors
Brodin, P Pinskaya, M Parsch, U Bischerour, J Leh, H Romanova, E Engels, JW Gottikh, M Mouscadet, JF
Citation
P. Brodin et al., 6-Oxocytidine containing oligonucleotides inhibit the HIV-1 integrase in vitro, NUCLEOS NUC, 20(4-7), 2001, pp. 481-486
Citations number
14
Categorie Soggetti
Biochemistry & Biophysics
Journal title
NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS
ISSN journal
15257770 → ACNP
Volume
20
Issue
4-7
Year of publication
2001
Pages
481 - 486
Database
ISI
SICI code
1525-7770(2001)20:4-7<481:6COITH>2.0.ZU;2-V
Abstract
Integration of the proviral DNA into the genome of infected cells is a key step of HIV-1 replication. Integration is catalyzed by the viral enzyme int egrase (IN). 6-oxocytidine-containing oligonucleotides were found to be eff icient inhibitors of integrase in vitro. The inhibitory effect is sequence- specific and strictly requires the presence of the 6-oxocytidine base. It i s due to the impairment of the integrase binding to its substrate and does not involve an auto-structure of the oligonucleotide.