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

Roba Moumné; Valéry Larue; Bili Seijo; Thomas Lecourt; Laurent Micouin; Carine Tisné

doi:10.1039/B921232A

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Tether influence on the binding properties of tRNA^Lys₃ligands designed by a fragment-based approach†

Roba Moumné,^a Valéry Larue,^b Bili Seijo,^b Thomas Lecourt,^a Laurent Micouin*^a and Carine Tisné*^b

Author affiliations

* Corresponding authors

^a Chimie Thérapeutique, Université Paris Descartes, CNRS UMR 8638, 4 avenue de l'Observatoire, Paris, (France)
E-mail: laurent.micouin@parisdescartes.fr
Fax: +33 143-29-1403

^b Cristallographie et RMN biologiques, Université Paris Descartes, CNRS UMR 8015, 4 avenue de l'Observatoire, Paris, (France)
E-mail: carine.tisne@parisdescartes.fr
Fax: +33 153-73-9925

Abstract

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^Lys₃, 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.

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Supplementary files

Experimental procedures and NMR data obtained for all compounds PDF (5346K)

Article information

DOI: https://doi.org/10.1039/B921232A
Article type: Paper
Submitted: 12 Oct 2009
Accepted: 09 Dec 2009
First published: 19 Jan 2010

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Org. Biomol. Chem., 2010,8, 1154-1159

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Tether influence on the binding properties of tRNA^Lys₃ ligands designed by a fragment-based approach

R. Moumné, V. Larue, B. Seijo, T. Lecourt, L. Micouin and C. Tisné, Org. Biomol. Chem., 2010, 8, 1154 DOI: 10.1039/B921232A

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Organic & Biomolecular Chemistry