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Por favor, use este identificador para citar o enlazar a este item: http://hdl.handle.net/10261/12333
Título

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

AutorMárquez, Nieves; Sancho, Rocío; Macho, Antonio; Moure Fernández, Alejandra; Masip, Isabel; Messeguer Peypoch, Ángel; Muñoz, Eduardo
Palabras claveCombinatorial libraries
Peptoids
CDK
HIV-1
LTR
Tat
Fecha de publicación28-feb-2006
EditorElsevier
CitaciónBiochemical Pharmacology 71(5): 596-604 (2006)
ResumenTranscription 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.
Descripción9 pages, 7 figures.
Versión del editorhttp://dx.doi.org/10.1016/j.bcp.2005.11.024
URIhttp://hdl.handle.net/10261/12333
DOI10.1016/j.bcp.2005.11.024
ISSN0006-2952
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