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Title: Role of cations in the interaction of pradimicins with HIV-1 envelope gp120
Authors: Hoorelbeke, Bart ×
Kim, Youngju
Oki, Toshikazu
Igarashi, Yasuhiro
Balzarini, Jan #
Issue Date: Aug-2013
Publisher: Bentham Science Publishers
Series Title: Current Topics in Medicinal Chemistry vol:13 issue:16 pages:1907-15
Abstract: Pradimicins (PRM) are a unique class of nonpeptidic carbohydrate-binding agents that inhibit HIV infection by efficiently binding to the HIV-1 envelope gp120 glycans in the obligatory presence of Ca(2+). Surface plasmon resonance (SPR) data revealed that addition of EDTA dose-dependently results in lower binding signals of PRM-A to immobilized gp120. Pradimicin derivatives that lack the free carboxylic acid group on the C-18 position failed to bind gp120 and were devoid of significant antiviral activity. Ca(2+) was much more efficient for PRM-A binding to gp120 than Cd(2+), Ba(2+) or Sr(2+). Instead, calcium could not be replaced by any other mono- (i.e. K(+)), di- (i.e. Cu(2+), Mg(2+), Mn(2+), Fe(2+), Zn(2+)) or trivalent (i.e. Al,(3+), Fe(3+)) cation without complete loss of gp120 binding. However, Zn(2+), Mg(2+) and Mn(2+) added to a Ca(2+)- pradimicin mixture, prevented pradimicin from efficient binding to gp120 glycans. These data suggest that these bivalent cations may bind to pradimicins but lead to pradimicin-cation complexes that are unable to further coordinate with the glycans of gp120. Thus, in order to afford antiviral activity, only a few cations can (i) bind to pradimicin to form a dimeric complex and (ii) subsequently coordinate the pradimicin/cation interaction with gp120 glycans.
URI: 
ISSN: 1568-0266
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
× corresponding author
# (joint) last author

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