Title of article
A possible improvement for structure-based drug design illustrated by the discovery of a Tat HIV-1 inhibitor
Author/Authors
Mickaël Montembault، نويسنده , , Giang Vo-Thanh، نويسنده , , Abdallah Deyine، نويسنده , , Valérie Fargeas، نويسنده , , Monique Villiéras، نويسنده , , Ané Adjou، نويسنده , , Didier Dubreuil، نويسنده , , Didier Esquieu، نويسنده , , Catherine Grégoire، نويسنده , , Sandrine Opi، نويسنده , , Jean-Marie Péloponèse، نويسنده , , D. Grant Campbell، نويسنده , , Jennifer Watkins، نويسنده , , Jean de Mareuil، نويسنده , , Anne-Marie Aubertin، نويسنده , , Christian Bailly، نويسنده , , Erwann Loret، نويسنده , , Jacques Lebreton، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
4
From page
1543
To page
1546
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
Keywords
HIV , Tat protein.* Corresponding authors. E-mail: erwann.loret@pharmacie.univ-mrs. , inhibitor
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
794230
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