title: Tether influence on the binding properties of tRNALys3 ligands designed by a fragment-based approach.
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.
authors.affiliation: Chimie Thérapeutique, Université Paris Descartes, CNRS UMR 8638, 4 avenue de l'Observatoire, 75006, Paris, France.
authors.forename: Roba
authors.initials: R
authors.lastname: Moumné
authors.forename: Valéry
authors.initials: V
authors.lastname: Larue
authors.forename: Bili
authors.initials: B
authors.lastname: Seijo
authors.forename: Thomas
authors.initials: T
authors.lastname: Lecourt
authors.forename: Laurent
authors.initials: L
authors.lastname: Micouin
authors.forename: Carine
authors.initials: C
authors.lastname: Tisné
mesh_terms: D001665:Binding Sites; D006678:HIV / Q000187:drug effects; D015658:HIV Infections / Q000188:drug therapy*; D008024:Ligands; D008958:Models, Molecular; D019906:Nuclear Magnetic Resonance, Biomolecular; D012346:RNA, Transfer, Amino Acyl / Q000737:chemistry / Q000378:metabolism*; D012367:RNA, Viral / Q000737:chemistry / Q000378:metabolism*; D048348:Reverse Transcription / Q000187:drug effects; D014230:Triazoles / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D008024:Ligands; D012346:RNA, Transfer, Amino Acyl; D012367:RNA, Viral; D014230:Triazoles