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dc.contributor.authorRivero-Buceta, Eva-
dc.contributor.authorCarrero, Paula-
dc.contributor.authorCasanova, Elena-
dc.contributor.authorDoyagüez, Elisa G.-
dc.contributor.authorMadrona, Andrés-
dc.contributor.authorQuesada, Ernesto-
dc.contributor.authorPeréz-Pérez, María-Jesús-
dc.contributor.authorMateos, Raquel-
dc.contributor.authorBravo, Laura-
dc.contributor.authorMathys, Leen-
dc.contributor.authorNoppen, Sam-
dc.contributor.authorKiselev, Evgency-
dc.contributor.authorMarchand, Christophe-
dc.contributor.authorPommier, Yves-
dc.contributor.authorLiekens, Sandra-
dc.contributor.authorBalzarini, Jan-
dc.contributor.authorCamarasa Rius, María José-
dc.contributor.authorSan-Félix, Ana-
dc.identifierdoi: 10.1016/j.ejmech.2015.10.027-
dc.identifierissn: 0223-5234-
dc.identifiere-issn: 1768-3254-
dc.identifier.citationEuropean Journal of Medicinal Chemistry 106: 132-143 (2015)-
dc.description.abstractThe glycoprotein gp120 of the HIV-1 viral envelope has a high content in mannose residues, particularly ¿-1,2-mannose oligomers. Compounds that interact with these high-mannose type glycans may disturb the interaction between gp120 and its (co)receptors and are considered potential anti-HIV agents. Previously, we demonstrated that a tripodal receptor (1), with a central scaffold of 1,3,5-triethylbenzene substituted with three 2,3,4-trihydroxybenzoyl groups, selectively recognizes ¿-1,2-mannose polysaccharides. Here we present additional studies to determine the anti-HIV-1 activity and the mechanism of antiviral activity of this compound. Our studies indicate that 1 shows anti-HIV-1 activity in the low micromolar range and has pronounced gp120 binding and HIV-1 integrase inhibitory capacity. However, gp120 binding rather than integrase inhibition seems to be the primary mechanism of antiviral activity of 1.-
dc.description.sponsorshipThe Spanish MICINN/MINECO (Project: SAF 201239760-C02-01, co-financed by the FEDER programme); Plan Nacional de Cooperación Público-Privada. Subprograma INNPACTO (IPT-2012-0213-060000, co-financed by the FEDER programme) and the Comunidad de Madrid (BIPEDD2-CM-S2010/BMD-2457) are acknowledged for fi nancial support. The Spanish ICINN/MINECCO is also acknowledged for a grant to E. Rivero-Buceta. We thank Leentje Persoons, Frieda De Meyer, Leen Ingels, Stijn Delmotte, Katrien Geerts, and Inge Vliegen for excellent technical assistance. Financial support of KU Leuven (GOA 10/14; PF 10/18) and the FWO (G-0528.12N) was provided for the antiviral experiments. The integrase studies were supported by the Center for Cancer Research, the Intramural Program of the National Cancer Institute,NIH (Z01-BC 007333).-
dc.subjectAntiviral agents-
dc.titleAnti-HIV-1 activity of a tripodal receptor that recognizes mannose oligomers-
dc.description.versionPeer Reviewed-
dc.contributor.funderMinisterio de Economía y Competitividad (España)-
dc.contributor.funderComunidad de Madrid-
dc.contributor.funderUniversity of Leuven-
dc.contributor.funderCancer Research Institute-
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