Roles for the Trypanosoma brucei P2 transporter in DB75 uptake and resistance.

doi:10.1124/mol.106.024653

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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...

Topics

Adenosine
Animals
Benzamidines
Biological Transport
Drug Resistance
Female
Fluorescence
Isotope Labeling
Male
Mice
Mutation
Nucleoside Transport Proteins
Rats
Rats, Sprague-Dawley
Trypanosoma brucei brucei

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Open in PubMed

Identifiers

PMID: 16912218
DOI: 10.1124/mol.106.024653

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