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Anti-Tat and anti-HIV activities of trimers of n-alkylglycines

AuthorsMárquez, Nieves; Sancho, Rocío; Macho, Antonio; Moure Fernández, Alejandra ; Masip, Isabel ; Messeguer Peypoch, Ángel ; Muñoz, Eduardo
KeywordsCombinatorial libraries
Issue Date28-Feb-2006
CitationBiochemical Pharmacology 71(5): 596-604 (2006)
AbstractTranscription of human immunodeficiency virus (HIV-1) is activated by viral Tat protein which regulates HIV–LTR transcription and elongation. In the present report, the evaluation of the anti-Tat activity of a combinatorial library composed of 5120 N-trialkylglycines is reported. The antiviral activity was studied through luciferase-based assays targeting the HIV-1 promoter activation induced by the HIV-1 Tat protein. We identified five peptoids with specific anti-HIV-1 Tat activity; none of these peptoids affected the binding of HIV-1 Tat protein to the viral TAR RNA. Using a recombinant-virus assay in which luciferase activity correlates with the rate of HIV-1 transcription we have detected that one of the five selected peptoids, NC37-37-15C, is a potent inhibitor of HIV-1–LTR transcription in both primary T lymphocytes and transformed cell lines. The inhibitory effect of NC37-37-15C, which is additive with azidothymidine (AZT), correlates with its ability to inhibit CTD phosphorylation and shows a suitable profile for development of novel anti-HIV-1 drugs. Likewise, the structural simplicity of N-alkylglycine oligomers makes these peptidomimetics amenable to structural manipulation, thus facilitating the optimisation of lead molecules for drug-like properties.
Description9 pages, 7 figures.
Publisher version (URL)http://dx.doi.org/10.1016/j.bcp.2005.11.024
Appears in Collections:(IQAC) Artículos
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