Branched oligonucleotide‐intercalator conjugate forming a parallel stranded structure inhibits HIV‐1 integrase

FEBS Letters

Romanova, Elena²  Mouscadet, Jean-François¹  Volkov, Evgenii²  Leh, Hervé¹  Brodin, Priscille¹  Pinskaya, Marina²  Gottikh, Marina²  Auclair, Christian¹ 

[1]CNRS-UMR 8532, Institut Gustave Roussy, 39 rue C. Desmoulins, 94805 Villejuif cedex, France

[2]Belozersky Institute of Physico-Chemical Biology, Lomonosov Moscow State University, 119899 Moscow, Russia

关键词: Integration;    HIV-1;    Parallel stranded DNA;    Oxazolopyridocarbazole;    Branched oligonucleotide;    HIV;    human immunodeficiency virus;    LTR;    long terminal repeat;    TFO;    triplex forming oligonucleotide;    IN;    integrase;    OPC;    oxazolopyridocarbazole;    CD;    circular dichroism;   

DOI  :  10.1016/S0014-5793(99)01350-2

学科分类：生物化学/生物物理

来源: John Wiley & Sons Ltd.

【 摘 要 】

Integration of a DNA copy of the HIV-1 genome into chromosomal DNA of infected cells is a key step of viral replication. Integration is carried out by integrase, a viral protein which binds to both ends of viral DNA and catalyses reactions of the 3′-end processing and strand transfer. A 3′-3′ branched oligonucleotide functionalised by the intercalator oxazolopyridocarbazole at each 5′-end was found to inhibit integration in vitro. We show that both a specific (G,A) sequence and the OPC intercalating agent contribute to the capability of the branched oligonucleotide to form a parallel stranded structure responsible for the inhibition.

【 授权许可】

Unknown