کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
9001457 | 1118521 | 2005 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Bis(pivaloyloxymethyl) thymidine 5â²-phosphate is a cell membrane-permeable precursor of thymidine 5â²-phosphate in thymidine kinase deficient CCRF CEM cells
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
AZTMPthymidine kinase deficientNTPPOMTLCTDRDTTPHCLO4DTMPPerchloric acid - اسید پرکلریکThymidine - تیمیدینthymidine 5′-triphosphate - تیمیدین 5'-تری فسفاتthymidine kinase - تیمیدین کینازDDT - دیکرو دیفنیل تری کلرواتانAntitumor - ضد تومورnucleoside triphosphate - نوکلئوزید تری فسفاتProdrugs - پیش داروthin layer chromatography - کروماتوگرافی لایه نازکhigh performance liquid chromatography - کروماتوگرافی مایع با کارایی بالاHPLC - کروماتوگرافی مایعی کارا
موضوعات مرتبط
علوم پزشکی و سلامت
داروسازی، سم شناسی و علوم دارویی
داروشناسی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Bis(pivaloyloxymethyl) thymidine 5â²-phosphate is a cell membrane-permeable precursor of thymidine 5â²-phosphate in thymidine kinase deficient CCRF CEM cells Bis(pivaloyloxymethyl) thymidine 5â²-phosphate is a cell membrane-permeable precursor of thymidine 5â²-phosphate in thymidine kinase deficient CCRF CEM cells](/preview/png/9001457.png)
چکیده انگلیسی
Bis(pivaloyloxymethyl) thymidine 5-phosphate (POM2-dTMP) has been investigated as a membrane-permeable prodrugs of dTMP. The growth inhibitory activity of POM2-TMP has been compared with thymidine (TdR) in wild type CCRF CEM cells (CEM) and a strain that lacks TdR kinase (CEM tkâ). After 72 h incubation at 37 °C, TdR showed significant antiproliferative activity (IC50 = 27 μM) against CEM cells but was weakly effective (IC50 = 730 μM) against the mutant cell line. By comparison, bis(pivaloyloxymethyl) thymidine 5â²-monophosphate (POM2-dTMP) was equally inhibitory (IC50 = 5 μM) to both cell lines. The growth inhibitory effects were reversed by deoxycytidine. Cellular [methyl-3H]dTTP pools increased linearly over 2 h during incubation of CEM or CEM tkâ with 5 μM POM2-[methyl-3H]dTMP. The incorporation of [methyl-3H]TdR into HClO4-insoluble cell residue by CEM tkâ was <0.1% that of CEM and did not increase over 1 h. In contrast, CEM tkâ incorporated radioactivity from POM2-dTMP into acid insoluble residue at a rate 59% that of CEM. These results demonstrate that POM2-dTMP can penetrate into cells and serve as a source of dTMP.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Biochemical Pharmacology - Volume 69, Issue 9, 1 May 2005, Pages 1307-1313
Journal: Biochemical Pharmacology - Volume 69, Issue 9, 1 May 2005, Pages 1307-1313
نویسندگان
Saeed R. Khan, Billie Nowak, William Plunkett, David Farquhar,