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The strand transfer oligonucleotide inhibitors of HIV-integrase
- 1.0327524 - ÚOCHB 2010 RIV GB eng J - Journal Article
Snášel, Jan - Rosenberg, Ivan - Pačes, Ondřej - Pichová, Iva
The strand transfer oligonucleotide inhibitors of HIV-integrase.
Journal of Enzyme Inhibition and Medicinal Chemistry. Roč. 24, č. 1 (2009), s. 241-246. ISSN 1475-6366. E-ISSN 1475-6374
R&D Projects: GA MŠMT 1M0508; GA ČR GA203/05/0827; GA ČR GP203/05/P557; GA AV ČR IAA4055304
Institutional research plan: CEZ:AV0Z40550506
Keywords : HIV-1 integrase * inhibition * phosphonate oligonucleotides
Subject RIV: CE - Biochemistry
Impact factor: 1.496, year: 2009
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.
Permanent Link: http://hdl.handle.net/11104/0174316
Number of the records: 1