Fluorodeoxyuridylate

09/01/1984 - "Those gastrointestinal tumors with higher FdUMP:dUMP ratios showed significantly greater TS inhibition. "
08/24/2001 - "Thus, FA-FdUMP[N] may prove useful for the treatment of 5-FU-resistant malignancies."
10/01/2017 - "Analysis of orthotopic tumors from mice treated systemically with tumor-targeted FdUMP-CPSNPs confirmed the in vivo up take of these particles by PDAC tumor cells and release of active drug cargos intracellularly. "
09/01/2002 - "The TS and DPD activity in tumor tissue was measured before and after UFT administration by the FdUMP binding assay and a catalytic assay in 38 patients, respectively. "
01/01/2001 - "Further, elevated expression of DPD in the tumor tissue results in a lack of FdUMP. "

10/15/1988 - "Among the 30 of the 37 colorectal tumors that showed suboptimal (less than 85%) inhibition of TS, 16 (53%) showed FdUMP levels less than 75 pmol/g, 8 (27%) showed relatively high dUMP levels (over 35 nmol/g), and 16 (53%) showed poor efficiency of inhibition of TS, with the major overlap between these mechanisms of resistance being high dUMP and poor binding in 6 (20%). "
10/15/1988 - "Colorectal tumors showed significantly greater FdUMP levels than other gastrointestinal malignancies, associated with somewhat lower free TS values. "
09/01/1995 - "We investigated the changes in the number of FdUMP binding sites in human colorectal carcinoma tissues after treatment with 5-fluorouracil derivatives and also examined the mechanisms underlying these changes. "
02/22/2022 - "Recently, we hypothesized that 5-FU-resistant colorectal cancer (CRC) cells have increased levels of TS protein relative to 5-FU-sensitive CRC cells and use a fraction of their TS to trap FdUMP, which results in resistance to 5-FU. "
05/01/1988 - "Hemolysates were found to catalyze efficient dephosphorylation of FdUMP to yield nearly stoichiometric amounts of the corresponding deoxyribonucleoside 5-fluoro-2'-deoxyuridine (FdUrd), an antineoplastic drug showing selective cytotoxicity toward liver metastases from colorectal carcinomas. "

02/10/1977 - "Hence, the formation of FdUMP from FUra in Novikoff hepatoma cells apparently proceeds primarily via the intermediate formation of ribonucleotides. "
02/10/1977 - "N1-S1/FdUrd Novikoff hepatoma cells, which lack thymidine kinase activity, are resistant to 5-fluorouracil (FUra) as well as 5-fluorodeoxyuridine (FdUrd), suggesting that the pathway, FUra leads to FdUrd leads to FdUMP, is utilized for the conversion of FUra to FdUMP. "
02/10/1977 - "However, the inhibition of thymidylate synthetase activity, the presumed target of FdUMP, by 1 X 10(-4) M FUra in intact N1-S1 Novikoff hepatoma cells, which have significant levels of thymidine kinase activity, is completely eliminated by 5 X 10(-4) M hydroxyurea, which is a potent inhibitor of ribonucleotide reductase. "

02/01/1995 - "In UFTL group, concentration of FdUMP was higher in the tumor tissue of moderately differentiated adenocarcinoma than that of well differentiated adenocarcinoma. "
05/01/2009 - "In the present study, we compared the ability of 5-FU and FdUMP to induce apoptosis and to influence the cell cycle progression in human colon SW620 adenocarcinoma cells in regards to their genotoxic and clastogenic activities. "
03/01/1999 - "TS expression was assessed by both Fluorodeoxyuridine-monophosphate (FdUMP) binding assay and cPCR in 9 human adenocarcinoma cell lines and 50 human adenocarcinoma tissues obtained by surgical resection. "
09/01/1989 - "These results suggest that 5-FU sensitivity of cervical adenocarcinoma cell line (OMC-4) is lower than that of cervical squamous carcinoma cell line (OMC-1) and it may owe much not to the TS inhibition rate but to the intracellular FdUMP."
04/01/1982 - "This study was designed to examine the endogenous concentrations of 5,10-methylenetetrahydrofolate (CH2FH4) in human colorectal adenocarcinoma xenografts, and to determine the ability of other folate derivatives to increase the formation of the ternary covalent complex between CH2FH4, [6-3H]-5-fluorodeoxyuridylate (FdUMP) and thymidylate synthetase (TS, EC 2.1.1.45). "

02/14/1992 - "IFN alpha treatment of HT-29 colon carcinoma cells induced a greater than two-fold increase in the intracellular levels of the active metabolite of FUra, FdUMP. "
12/15/1991 - "Quantitation of TS by Western blot analysis and biochemical FdUMP binding assay in 5-fluorouracil-resistant colon carcinoma cell lines (NCI H630R10, NCI H630R1) and a sensitive colon carcinoma cell line (NCI H630) revealed a 36- and 6-fold increase in TS in the resistant cell line as measured by the biochemical assay compared to a 39- and 10.6-fold increase as measured by densitometric analysis of the Western blot. "
08/01/2001 - "The levels of TS and DPD activities in nonfixed, fresh, frozen, bladder carcinoma and normal bladder specimens were determined biochemically by the FdUMP binding assay and the 5-FU degradation assay, respectively. "
03/15/1994 - "We have reported previously an IFN alpha-mediated elevation in cellular FdUMP levels accompanied by the stimulation of thymidine phosphorylase (TP) activity in extracts from HT-29 human colon carcinoma cells treated with IFN alpha. "
03/15/1981 - "Similarly, the smaller amount of FdUMP dephosphorylation found in all carcinomas compared with autologous normal mucosal preparations might result in prolonged thymidylate synthetase inhibition. "