| Comparative antiviral activity of integrase inhibitors in human monocyte-derived macrophages and lymphocytes. | |
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MedLine Citation:
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PMID: 21867733 Owner: NLM Status: Publisher |
Abstract/OtherAbstract:
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The activity of raltegravir and 4 other integrase inhibitors (MK-2048, L870,810, IN2, and IN5) was investigated in primary human macrophages, PBMC and C8166-lymphocytic T cells, in order to determine their relative potency and efficacy in different cellular systems of HIV infection. Raltegravir showed better protective efficacy in all cell types; MK-2048, L870,810 and IN5 showed a potent anti-HIV-1 activity in macrophages, while in lymphocytes only MK-2048 and L870,810 showed an inhibitory effect comparable to raltegravir. IN2 was a poorly effective anti-HIV-1 compound in all cellular systems. All effective integrase inhibitors exhibited a potent antiviral activity against both X4 and R5 HIV-1 strains. In general, raltegravir, MK-2048, L870,810 and IN5 showed anti HIV activity similar or slightly higher in macrophages compared to PBMC and C8166 T cells: for MK-2048, the EC(50) was 0.4, 0.9, 11.5nM in macrophages, in PBMCs and T cells, respectively; for L870,810, the EC(50) was 1.5, 14.3, and 10.6nM, respectively; for IN5 the EC(50) was 0.5, 13.7, and 5.7nM, respectively. |
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Authors:
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Fernanda Scopelliti; Michela Pollicita; Francesca Ceccherini-Silberstein; Fabiola Di Santo; Matteo Surdo; Stefano Aquaro; Carlo-Federico Perno |
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Publication Detail:
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Type: JOURNAL ARTICLE Date: 2011-8-16 |
Journal Detail:
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Title: Antiviral research Volume: - ISSN: 1872-9096 ISO Abbreviation: - Publication Date: 2011 Aug |
Date Detail:
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Created Date: 2011-8-26 Completed Date: - Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8109699 Medline TA: Antiviral Res Country: - |
Other Details:
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Languages: ENG Pagination: - Citation Subset: - |
Copyright Information:
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Copyright © 2011. Published by Elsevier B.V. |
Affiliation:
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University of Rome Tor Vergata, Rome, Italy. |
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From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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