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DNA Triplex-Based Complexes Display Anti-HIV-1-Cell Fusion Activity.

ABSTRACT: DNA triplexes with hydrophobic modifications were designed and evaluated for their activity as inhibitors of the cell fusion of human immunodeficiency virus type 1 (HIV-1). Triplex inhibitors displayed low micromolar activities in the cell-cell fusion assay and nanomolar activities in the anti-HIV-1 pseudovirus test. Helix structure and the presence of sufficient numbers of hydrophobic regions were essential for the antifusion activity. Results from native polyacrylamide gel electrophoresis and a fluorescent resonance energy transfer-based inhibitory assay indicated that these triplexes may interact with the primary pocket at the glycoprotein 41 (gp41) N-heptad repeat, thereby inhibiting formation of the HIV-1 gp41 6-helical bundle. Triplex-based complexes may represent a novel category of HIV-1 inhibitors in anti-HIV-1 drug discovery.

SUBMITTER: Xu L

PROVIDER: S-EPMC4507350 | biostudies-literature | 2015 Aug

REPOSITORIES: biostudies-literature

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DNA Triplex-Based Complexes Display Anti-HIV-1-Cell Fusion Activity.

Xu Liang L Zhang Tao T Xu Xiaoyu X Chong Huihui H Lai Wenqing W Jiang Xifeng X Wang Chao C He Yuxian Y Liu Keliang K

Nucleic acid therapeutics 20150801 4

DNA triplexes with hydrophobic modifications were designed and evaluated for their activity as inhibitors of the cell fusion of human immunodeficiency virus type 1 (HIV-1). Triplex inhibitors displayed low micromolar activities in the cell-cell fusion assay and nanomolar activities in the anti-HIV-1 pseudovirus test. Helix structure and the presence of sufficient numbers of hydrophobic regions were essential for the antifusion activity. Results from native polyacrylamide gel electrophoresis and ...[more]

PMID: 26192705

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