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Title

Anti-HIV-1 activity of a tripodal receptor that recognizes mannose oligomers

AuthorsRivero-Buceta, Eva ; Carrero, Paula ; Casanova, Elena ; Doyagüez, Elisa G.; Madrona, Andrés; Quesada, Ernesto; Peréz-Pérez, María-Jesús ; Mateos, Raquel ; Bravo, Laura ; Mathys, Leen; Noppen, Sam; Kiselev, Evgency; Marchand, Christophe; Pommier, Yves; Liekens, Sandra; Balzarini, Jan; Camarasa Rius, María José ; San-Félix, Ana
KeywordsPolyphenols
AIDS
Antiviral agents
Integrase
HIV
Issue Date2015
PublisherElsevier
CitationEuropean Journal of Medicinal Chemistry 106: 132-143 (2015)
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.
Publisher version (URL)http://dx.doi.org/10.1016/j.ejmech.2015.10.027
URIhttp://hdl.handle.net/10261/132520
DOI10.1016/j.ejmech.2015.10.027
Identifiersdoi: 10.1016/j.ejmech.2015.10.027
issn: 0223-5234
e-issn: 1768-3254
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(CENQUIOR) Artículos
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