Tether influence on the binding properties of tRNALys3 ligands designed by a fragment-based approach.

Roba Moumné (1, 2) , Valéry Larue (3) , Bili Seijo , Thomas Lecourt (4) , Laurent Micouin (4) , Carine Tisné (3)

1 SSFMB - Synthèse, Structure et Fonction de Molécules Bioactives
2 UPMC - Université Pierre et Marie Curie - Paris 6
3 LCRB - UMR 8015 - Laboratoire de cristallographie et RMN biologiques
4 SSMIP - Synthèse et structure de molécules d'interet pharmacologique

A small library of 1,5-triazole derivatives linking a diaminocyclopentadiol and aromatic ketones has been prepared and screened using NMR and fluorescent techniques against tRNA(Lys)(3), the HIV reverse transcription primer. The comparison of their binding properties to those of their 1,4-triazole isomers, previously discovered in a fragment-based approach, outlines the influence of the linker on affinity and binding selectivity in such an approach.

Domaines: Chimie organique

Roba Moumné, Valéry Larue, Bili Seijo, Thomas Lecourt, Laurent Micouin, et al.. Tether influence on the binding properties of tRNALys3 ligands designed by a fragment-based approach.. Organic & Biomolecular Chemistry, 2010, 8 (5), pp.1154-9. ⟨10.1039/b921232a⟩. ⟨hal-00596199⟩