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The strand transfer oligonucleotide inhibitors of HIV-integrase

SYSNO ASEP	0327524
Document Type	J - Journal Article
R&D Document Type	Journal Article
Subsidiary J	Článek ve WOS
Title	The strand transfer oligonucleotide inhibitors of HIV-integrase
Author(s)	Snášel, Jan (UOCHB-X)_RID Rosenberg, Ivan (UOCHB-X)_{RID, ORCID} Pačes, Ondřej (UOCHB-X) Pichová, Iva (UOCHB-X)_{RID, ORCID}
Number of authors	4
Source Title	Journal of Enzyme Inhibition and Medicinal Chemistry. - : Taylor & Francis - ISSN 1475-6366 Roč. 24, č. 1 (2009), s. 241-246
Number of pages	6 s.
Language	eng - English
Country	GB - United Kingdom
Keywords	HIV-1 integrase ; inhibition ; phosphonate oligonucleotides
Subject RIV	CE - Biochemistry
R&D Projects	1M0508 GA MŠMT - Ministry of Education, Youth and Sports (MEYS)
	GA203/05/0827 GA ČR - Czech Science Foundation (CSF)
	GP203/05/P557 GA ČR - Czech Science Foundation (CSF)
	IAA4055304 GA AV ČR - Academy of Sciences of the Czech Republic (AV ČR)
CEZ	AV0Z40550506 - UOCHB-X (2005-2011)
UT WOS	000262718700034
DOI	10.1080/14756360802051578
Annotation	We have designed and synthesized oligonucleotides (ONs) of various lengths that mimic the processed HIV-1 U5 terminus of the proviral long terminal repeat (LTR) and are ended by 2‘-deoxyadenosine containing a 3‘-O-phosphonomethyl group for inhibition of HIV-1 integrase. The duplex stability of phosphonomethyl ONs was increased by covalent linkage of the modified strand with its complementary strand by a triethylene glycol loop (TEG). Modified ONs containing up to 10 bases inhibited in vitro the strand transfer reaction catalyzed by HIV-1 integrase at nanomolar concentrations.
Workplace	Institute of Organic Chemistry and Biochemistry
Contact	asep@uochb.cas.cz ; Kateřina Šperková, Tel.: 232 002 584 ; Viktorie Chládková, Tel.: 232 002 434
Year of Publishing	2010

Number of the records: 1