tailieunhanh - Báo cáo khoa học: Insight into the mechanisms of aminoglycoside derivatives interaction with HIV-1 entry steps and viral gene transcription

Cytosine methylation at the 5-carbon position is the only known stable base modification found in the mammalian genome. The organization and modification of chromatin is a key factor in programming gene expression patterns. Recent findings suggest that DNA methylation at the junction of transcription initiation and elongation plays a critical role in suppression of transcription. | FEBS Journal REVIEW ARTICLE Insight into the mechanisms of aminoglycoside derivatives interaction with HIV-1 entry steps and viral gene transcription Aviva Lapidot1 Alexander Berchanski1 and Gadi Borkow2 1 Department of Organic Chemistry The Weizmann Institute of Science Rehovot Israel 2 Cupron Inc. Beth Shemesh Israel Keywords arginine-aminoglycoside conjugates CD4 CXCL12 CXCR4 CCR5 gp120 gp41 HIV-1 entry inhibitors molecular modeling and docking poly-arginine-aminoglycoside conjugates Rev-RRE Tat-TAR Correspondence A. Lapidot Department of Organic Chemistry The Weizmann Institute of Science Rehovot 76100 Israel Fax 972 8 9344142 Tel 972 8 9343413 E-mail Received 3 July 2008 revised 13 August 2008 accepted 27 August 2008 doi In recent years based on peptide models of HIV-1 RNA binding NMR structures of Tat-responsive element-ligand complexes and aminoglyco-side-RNA interactions and HIV-1 Tat structure we have designed and synthesized aminoglycoside-arginine conjugates AACs and aminoglycoside poly-arginine conjugates APACs to serve as Tat mimetics. These novel molecules inhibit HIV-1 infectivity with 50 effective concentration values in the low micromolar range the most potent compounds being the hexa-arginine-neomycin B and nona-D-arginine-neomycin conjugates. Importantly these compounds in addition to acting as Tat antagonists inhibit HIV-1 infectivity by blocking several steps in HIV-1 cell entry. The AACs and APACs inhibit HIV-1 cell entry by interacting with gp120 at the CD4-binding site by interacting with CXCR4 at the binding site of the CXCR4 mAb 12G5 and apparently by interacting with transient structures of the ectodomain of gp41. In the current review we discuss the mechanisms of anti-HIV-1 activities of these AACs APACs and other aminoglycoside derivatives in detail. Targeting several key processes in the viral life cycle by the same compound not only may increase its antiviral efficacy but

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