Article
Roles for the Trypanosoma brucei P2 transporter in DB75 uptake and resistance.
Molecular pharmacology - 1 Nov 2006
Lanteri Charlotte A, Stewart Mhairi L, Brock Janice M, Alibu Vincent P, Meshnick Steven R, Tidwell Richard R, Barrett Michael P
Abstract excerpt
A novel trypanocide, 2,5-bis(4-amidinophenyl)furan (DB75), in its prodrug amidoxime-derivative form, 2,5-bis(4-amidinophenyl)furan-bis-O-methylamidoxime (DB289), is in trials as the first orally administered drug for human African trypanosomiasis. DB75 is a diamidine. Resistance to some diamidines correlates to loss of uptake via the P2 aminopurine transporter. We show here that uptake of DB75 into Trypanosoma...
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