کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
5915781 1163328 2010 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Short technical reportA fluorescence-based assay for the uptake of CPD0801 (DB829) by African trypanosomes
موضوعات مرتبط
علوم زیستی و بیوفناوری بیوشیمی، ژنتیک و زیست شناسی مولکولی زیست شناسی مولکولی
پیش نمایش صفحه اول مقاله
Short technical reportA fluorescence-based assay for the uptake of CPD0801 (DB829) by African trypanosomes
چکیده انگلیسی

Drug therapies currently used for second stage Human African Trypanosomiasis (HAT) exhibit problems with toxicity, difficulty of administration, and resistance linked to the loss of transporter function. Key to the development of new drugs for HAT is a better understanding of the transport properties of candidate compounds. Standard methods for studying transport utilize radio-labelled permeant or HPLC-MS, however the natural fluorescence of many trypanocidal compounds can be exploited.Here we present a fluorescence-based assay for measuring uptake, by trypanosomes, of CPD0801, a drug candidate for second stage HAT. Sample fluorescence is measured in a 96-well format using a benchtop fluorimeter. Our method is directly applicable to the study of other diamidines with similar fluorescent properties and readily adapted for use with other cell types or fluorescent molecules as we demonstrate for the veterinary trypanocide ethidium.

. A fluorescence based method for quantifying the uptake of CPD0801 (DB829), a drug candidate against second stage HAT, by African trypanosomes.42Research highlights▶ CPD0801, a novel diamidine, has potent trypanocidal activity. ▶ Like other diamidines it is carried into trypanosomes principally via the P2 aminopurine transporter. ▶ Here we report a simple fluorescence based method to quantitate uptake.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Molecular and Biochemical Parasitology - Volume 174, Issue 2, December 2010, Pages 145-149
نویسندگان
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