Inhibitory Effect of Lithospermic Acid on the HIV-1 Nucleocapsid Protein.
Fiche publication
Date publication
novembre 2020
Journal
Molecules (Basel, Switzerland)
Auteurs
Membres identifiés du Cancéropôle Est :
Pr MELY Yves
Tous les auteurs :
Mori M, Ciaco S, Mély Y, Karioti A
Lien Pubmed
Résumé
The HIV-1 nucleocapsid protein (NC) is a desirable target in antiretroviral therapy due to its high conservation among HIV-1 strains, and to its multiple and crucial roles in the HIV-1 replication cycle. Natural products represent a valuable source of NC inhibitors, with the catechol group being a privileged scaffold in NC inhibition. By coupling molecular modeling with NMR spectroscopy and fluorescence-based assays, we disclosed lithospermic acid, a catechol derivative extracted from , as a potent and chemically stable non-covalent inhibitor of the NC. Being different from other catechol derivative reported so far, lithospermic acid does not undergo spontaneous oxidation in physiological conditions, thus becoming a profitable starting point for the development of efficient NC inhibitors.
Mots clés
HIV, catechol, fluorescence-based assays, lithospermic acid, molecular modeling, natural products, nucleocapsid protein
Référence
Molecules. 2020 Nov 20;25(22):