کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5846999 | 1129303 | 2015 | 14 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Fitting Transporter Activities to Cellular Drug Concentrations and Fluxes: Why the Bumblebee Can Fly
ترجمه فارسی عنوان
جابجایی وسایل حمل و نقل به غلظت و جرم سلولی: چرا مارپیچ می تواند پرواز کند
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موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
چکیده انگلیسی
A recent paper in this journal argued that reported expression levels, kcat and Km for drug transporters could be used to estimate the likelihood that drug fluxes through Caco-2 cells could be accounted for solely by protein transporters. It was in fact concluded that if five such transporters contributed 'randomly' they could account for the flux of the most permeable drug tested (verapamil) 35% of the time. However, the values of permeability cited for verapamil were unusually high; this and other drugs have much lower permeabilities. Even for the claimed permeabilities, we found that a single 'random' transporter could account for the flux 42% of the time, and that two transporters can achieve 10 · 10â6 cm·sâ1 90% of the time. Parameter optimisation methods show that even a single transporter can account for Caco-2 drug uptake of the most permeable drug. Overall, the proposal that 'phospholipid bilayer diffusion (of drugs) is negligible' is not disproved by the calculations of 'likely' transporter-based fluxes.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Trends in Pharmacological Sciences - Volume 36, Issue 11, November 2015, Pages 710-723
Journal: Trends in Pharmacological Sciences - Volume 36, Issue 11, November 2015, Pages 710-723
نویسندگان
Pedro Mendes, Stephen G. Oliver, Douglas B. Kell,