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

Org Biomol Chem. 2010 Mar 7;8(5):1154-9. doi: 10.1039/b921232a. Epub 2010 Jan 19.

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(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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • HIV / drug effects
  • HIV Infections / drug therapy*
  • Ligands
  • Models, Molecular
  • Nuclear Magnetic Resonance, Biomolecular
  • RNA, Transfer, Amino Acyl / chemistry
  • RNA, Transfer, Amino Acyl / metabolism*
  • RNA, Viral / chemistry
  • RNA, Viral / metabolism*
  • Reverse Transcription / drug effects
  • Triazoles / chemistry*
  • Triazoles / pharmacology*

Substances

  • Ligands
  • RNA, Transfer, Amino Acyl
  • RNA, Viral
  • Triazoles