HIV infection is pandemic in humans and is responsible for millions of deaths every year. The discovery of new cellular targets that can be used to prevent the infection process represents a new opportunity for developing more effective antiviral drugs. In this work, dendritic cell-specific ICAM-3 grabbing non-integrin (DC-SIGN), a lectin expressed at the surface of immature dendritic cells and involved in the initial stages of HIV infection, is described as a promising therapeutic target. The project is being developed within the European research Network CARMUSYS (http://www.carmusys.iiq.csic.es). Herein we show the synthesis of a small library of derivatives of a dimannoside mimic recently reported by our laboratory.1 The mimic was functionalized with two identical amide groups. Further, multivalent presentations of the prepared DC-SIGN ligands were obtained via click chemistry using dendrimeric scaffolds. The activities of the prepared molecules towards DC-SIGN were determined using surface plasmon resonance (SPR) technique. Multivalency showed significant improvement of the DC-SIGN inhibition in comparison with the corresponding monovalent ligands.

Synthesis of mono and multivalent pseudosacharide based DC-SIGN ligands : research update / N. Varga, A. Bernardi. ((Intervento presentato al convegno CARMUSYS regular meeting and workshop : human applications and clinical trials design tenutosi a Toledo nel 2011.

Synthesis of mono and multivalent pseudosacharide based DC-SIGN ligands : research update

N. Varga
Primo
;
A. Bernardi
Ultimo
2011

Abstract

HIV infection is pandemic in humans and is responsible for millions of deaths every year. The discovery of new cellular targets that can be used to prevent the infection process represents a new opportunity for developing more effective antiviral drugs. In this work, dendritic cell-specific ICAM-3 grabbing non-integrin (DC-SIGN), a lectin expressed at the surface of immature dendritic cells and involved in the initial stages of HIV infection, is described as a promising therapeutic target. The project is being developed within the European research Network CARMUSYS (http://www.carmusys.iiq.csic.es). Herein we show the synthesis of a small library of derivatives of a dimannoside mimic recently reported by our laboratory.1 The mimic was functionalized with two identical amide groups. Further, multivalent presentations of the prepared DC-SIGN ligands were obtained via click chemistry using dendrimeric scaffolds. The activities of the prepared molecules towards DC-SIGN were determined using surface plasmon resonance (SPR) technique. Multivalency showed significant improvement of the DC-SIGN inhibition in comparison with the corresponding monovalent ligands.
27-giu-2011
DC-SIGN ; infection ; HIV ; pseudosacharide ; sugar ; synthesis
Settore CHIM/06 - Chimica Organica
Carbohydrate Multivalent System
Synthesis of mono and multivalent pseudosacharide based DC-SIGN ligands : research update / N. Varga, A. Bernardi. ((Intervento presentato al convegno CARMUSYS regular meeting and workshop : human applications and clinical trials design tenutosi a Toledo nel 2011.
Conference Object
File in questo prodotto:
Non ci sono file associati a questo prodotto.
Pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2434/164174
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus ND
  • ???jsp.display-item.citation.isi??? ND
social impact