A possible improvement for structure-based drug design illustrated by the discovery of a Tat HIV-1 inhibitor |
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| Authors: | Montembault Mickaël Vo-Thanh Giang Deyine Abdallah Fargeas Valérie Villiéras Monique Adjou Ané Dubreuil Didier Esquieu Didier Grégoire Catherine Opi Sandrine Péloponèse Jean-Marie Campbell Grant Watkins Jennifer de Mareuil Jean Aubertin Anne-Marie Bailly Christian Loret Erwann Lebreton Jacques |
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| Affiliation: | Laboratoire de Synthèse Organique, CNRS UMR 6513, Faculté des Sciences, 2 rue de la Houssinière, BP 92208, 44322 Nantes Cedex 3, France. |
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| Abstract: | The HIV-1 Tat protein is a promising target for AIDS therapy, due to its extra-cellular roles against the immune system. From the 2D-NMR structure of Tat, we have designed molecules, called TDS, able to bind to Tat and inhibit HIV-1 replication in vitro. This new family of antivirals is composed of a triphenylene aromatic ring substituted with at least one carbon chain bearing a succinimide group. These ligands are prepared from triphenylene or 2,6,10-trimethylphenylene in 3-6 steps depending on the target molecule. |
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