Interaction of monobenzamidine-linked trypanocides with the Trypanosoma brucei P2 aminopurine transporter.
Single benzamidine group-carrying compounds were shown to interact with the Trypanosoma brucei P2 aminopurine transporter. Replacement of the amidine with a guanidine group decreased affinity. Trypanocidal activity was evident, but compounds were equally toxic against trypanosomes lacking the P2 transporter, which indicates additional uptake routes for monobenzamidine-derived compounds.
Stewart
Mhairi L
ML
University of Glasgow, Institute of Biomedical and Life Sciences, Division of Infection & Immunity, Glasgow G12 8QQ, United Kingdom.
Boussard
Cyrille
C
Brun
Reto
R
Gilbert
Ian H
IH
Barrett
Michael P
MP
D000818:Animals; D001550:Benzamidines / Q000737:chemistry*; D001692:Biological Transport / Q000187:drug effects; D033703:Nucleoside Transport Proteins / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000378:metabolism* / Q000494:pharmacology; D014346:Trypanosoma brucei brucei / Q000737:chemistry*
D001550:Benzamidines; D033703:Nucleoside Transport Proteins; C486446:P2 transporter, Trypanosoma brucei; D014344:Trypanocidal Agents; C032157:benzamidine