Article
Carbonylhydrazide-based molecular tongs inhibit wild-type and mutated HIV-1 protease dimerization.
Journal of medicinal chemistry - 9 Aug 2012
Dufau Laure, Marques Ressurreição Ana Sofia, Fanelli Roberto, Kihal Nadjib, Vidu Anamaria, Milcent Thierry, Soulier Jean-Louis, Rodrigo Jordi, Desvergne Audrey, Leblanc Karine, Bernadat Guillaume, Crousse Benoit, Reboud-Ravaux Michèle, Ongeri Sandrine
Abstract excerpt
We have designed and synthesized new molecular tongs based on a rigid naphthalene scaffold and evaluated their antidimer activity on HIV-1 protease (PR). We inserted carbonylhydrazide and oligohydrazide (azatide) fragments into their peptidomimetic arms to reduce hydrophobicity and increase metab...
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