Tether influence on the binding properties of tRNALys3 ligands designed by a fragment-based approach.
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.
Moumné
Roba
R
Chimie Thérapeutique, Université Paris Descartes, CNRS UMR 8638, 4 avenue de l'Observatoire, 75006, Paris, France.
Larue
Valéry
V
Seijo
Bili
B
Lecourt
Thomas
T
Micouin
Laurent
L
Tisné
Carine
C
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*
D008024:Ligands; D012346:RNA, Transfer, Amino Acyl; D012367:RNA, Viral; D014230:Triazoles