title: Synthesis of polyamine derivatives for the preparation of affinity chromatography columns for the search of new Trypanosoma cruzi targets.
abstract: The most potent trypanocidal compound of a series of symmetrically substituted 1,4-bis(3-aminopropylpiperazines) which displayed an IC50 value of 5 microM on Trypanosoma cruzi trypomastigotes, was inactive on trypanothione reductase. Two derivatives 6 and 12 of this compound, one symmetrical and one dissymmetrical, were synthesized via a reductive amination reaction, to prepare affinity chromatography columns, which allowed us to isolate three parasitic proteins. Among these, the major ligand 6- and 12-binding protein having an apparent molecular weight of 52 kDa has been identified as the thiol-disulfide oxido-reductase Tc52, previously characterized in Trypanosoma cruzi.
authors.affiliation: Institut de Biologie et Institut Pasteur de Lille - UMR CNRS 8525 - Faculté de Pharmacie - Université de Lille II, France.
authors.forename: E
authors.initials: E
authors.lastname: Davioud-Charvet
authors.forename: A
authors.initials: A
authors.lastname: Berecibar
authors.forename: S
authors.initials: S
authors.lastname: Girault
authors.forename: V
authors.initials: V
authors.lastname: Landry
authors.forename: H
authors.initials: H
authors.lastname: Drobecq
authors.forename: C
authors.initials: C
authors.lastname: Sergheraert
mesh_terms: D000818:Animals; D015153:Blotting, Western; D002846:Chromatography, Affinity; D020128:Inhibitory Concentration 50; D008956:Models, Chemical; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology*; D011073:Polyamines / Q000138:chemical synthesis*; D014344:Trypanocidal Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects
chemical_list: D010879:Piperazines; D011073:Polyamines; D014344:Trypanocidal Agents