PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 13680162-6 2003 The DPD and TS activities were quantified by a radiometric enzymatic assay and a 5-fluoro-2"-deoxyuridine-5"- monophosphate (FdUMP) ligand-binding assay, respectively. Fluorodeoxyuridylate 81-123 dihydropyrimidine dehydrogenase Homo sapiens 4-7 15930305-1 2005 FdUMP[10], a 10mer of 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP), the thymidylate synthase inhibitory metabolite of 5-fluorouracil (FU), is most closely correlated with the DNA topoisomerase I (Top1) inhibitor camptothecin in the National Cancer Institute COMPARE analysis, but not with FU. Fluorodeoxyuridylate 0-5 topoisomerase (DNA) I Mus musculus 180-199 15930305-1 2005 FdUMP[10], a 10mer of 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP), the thymidylate synthase inhibitory metabolite of 5-fluorouracil (FU), is most closely correlated with the DNA topoisomerase I (Top1) inhibitor camptothecin in the National Cancer Institute COMPARE analysis, but not with FU. Fluorodeoxyuridylate 22-63 thymidylate synthase Mus musculus 77-97 15930305-1 2005 FdUMP[10], a 10mer of 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP), the thymidylate synthase inhibitory metabolite of 5-fluorouracil (FU), is most closely correlated with the DNA topoisomerase I (Top1) inhibitor camptothecin in the National Cancer Institute COMPARE analysis, but not with FU. Fluorodeoxyuridylate 22-63 topoisomerase (DNA) I Mus musculus 180-199 14770427-2 2004 5-FU is a prodrug, and orotate phosphoribosyltransferase (OPRT) is the principal enzyme that converts 5-FU directly into an active antitumor metabolite, 5-fluoro-2"-deoxyuridine 5"-monophosphate. Fluorodeoxyuridylate 153-194 uridine monophosphate synthetase Homo sapiens 23-56 14770427-2 2004 5-FU is a prodrug, and orotate phosphoribosyltransferase (OPRT) is the principal enzyme that converts 5-FU directly into an active antitumor metabolite, 5-fluoro-2"-deoxyuridine 5"-monophosphate. Fluorodeoxyuridylate 153-194 uridine monophosphate synthetase Homo sapiens 58-62 14713770-2 2004 It is a prodrug and orotate phosphoribosyltransferase (OPRT) is the principal enzyme that directly converts 5-FU to the active anticancer metabolite 5-fluoro-2"-deoxyuridine 5"-monophosphate. Fluorodeoxyuridylate 149-190 uridine monophosphate synthetase Homo sapiens 20-53 14713770-2 2004 It is a prodrug and orotate phosphoribosyltransferase (OPRT) is the principal enzyme that directly converts 5-FU to the active anticancer metabolite 5-fluoro-2"-deoxyuridine 5"-monophosphate. Fluorodeoxyuridylate 149-190 uridine monophosphate synthetase Homo sapiens 55-59 16505899-1 2006 Thymidylate synthase purified from 5-fluoro-dUrd-resistant mouse leukemia L1210 cells (TSr) was less sensitive to slow-binding inhibition by 5-fluoro-dUMP than the enzyme from the parental cells (TSp), both enzyme forms differing also in sensitivity to several other dump analogues, apparent molecular weights of monomer and dimer, and temperature dependence of the catalyzed reaction. Fluorodeoxyuridylate 141-154 thymidylate synthase Mus musculus 0-20 13680162-6 2003 The DPD and TS activities were quantified by a radiometric enzymatic assay and a 5-fluoro-2"-deoxyuridine-5"- monophosphate (FdUMP) ligand-binding assay, respectively. Fluorodeoxyuridylate 81-123 thymidylate synthetase Homo sapiens 12-14 12167486-1 2002 Folate based inhibitors of thymidylate synthase (TS) might facilitate binding of 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) to TS similar to the natural reduced folate 5,10-methylenetetrahydrofolate (CH(2)-H(4)-folate). Fluorodeoxyuridylate 81-122 thymidylate synthetase Homo sapiens 27-47 12929570-6 2003 After infusion of 5-FU (40 mg/kg body), the serum 5-FU concentration and 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP)-bound TS levels in the jejunum were significantly higher in the PN group than the FED group (156.8 +/- 51.9 vs 100.5 +/- 51.9 ng/ml, p < 0.001 and 38.55 +/- 7.61 vs 22.89 +/- 4.46 pmol/g of tissue, p < 0.01, respectively). Fluorodeoxyuridylate 73-114 thymidylate synthetase Rattus norvegicus 129-131 12684419-7 2003 EXPERIMENTAL DESIGN: The levels of TS and DPD activities in nonfixed fresh-frozen RCC and normal kidney were determined biochemically by the 5-fluoro-2"-deoxyuridine 5"-monophosphate binding assay and the 5-FU degradation assay, respectively. Fluorodeoxyuridylate 141-182 thymidylate synthetase Homo sapiens 35-37 12820419-3 2003 This product can form 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP) through the action of thymidine kinase, and FdUMP in turn can inhibit thymidylate synthase (TS), leading to reduced thymidylate formation and subsequent inhibition of DNA synthesis. Fluorodeoxyuridylate 22-63 thymidylate synthetase Homo sapiens 142-162 12820419-3 2003 This product can form 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP) through the action of thymidine kinase, and FdUMP in turn can inhibit thymidylate synthase (TS), leading to reduced thymidylate formation and subsequent inhibition of DNA synthesis. Fluorodeoxyuridylate 22-63 thymidylate synthetase Homo sapiens 164-166 12553027-5 2002 Thymidine phosphorylase (TP), the enzyme that converts 5"-DFUR into 5-FU and 5-FU into 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP), was estimated by ELISA. Fluorodeoxyuridylate 87-128 thymidine phosphorylase Homo sapiens 0-23 12553027-5 2002 Thymidine phosphorylase (TP), the enzyme that converts 5"-DFUR into 5-FU and 5-FU into 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP), was estimated by ELISA. Fluorodeoxyuridylate 87-128 thymidine phosphorylase Homo sapiens 25-27 12553027-5 2002 Thymidine phosphorylase (TP), the enzyme that converts 5"-DFUR into 5-FU and 5-FU into 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP), was estimated by ELISA. Fluorodeoxyuridylate 130-135 thymidine phosphorylase Homo sapiens 0-23 12553027-5 2002 Thymidine phosphorylase (TP), the enzyme that converts 5"-DFUR into 5-FU and 5-FU into 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP), was estimated by ELISA. Fluorodeoxyuridylate 130-135 thymidine phosphorylase Homo sapiens 25-27 12883718-2 2003 Thymidylate synthase (TS) is inhibited to form an inactive ternary complex by 5-fluoro-dUMP and is considered to be a target enzyme of 5-FU treatment. Fluorodeoxyuridylate 78-91 thymidylate synthetase Homo sapiens 0-20 12883718-2 2003 Thymidylate synthase (TS) is inhibited to form an inactive ternary complex by 5-fluoro-dUMP and is considered to be a target enzyme of 5-FU treatment. Fluorodeoxyuridylate 78-91 thymidylate synthetase Homo sapiens 22-24 12167486-1 2002 Folate based inhibitors of thymidylate synthase (TS) might facilitate binding of 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) to TS similar to the natural reduced folate 5,10-methylenetetrahydrofolate (CH(2)-H(4)-folate). Fluorodeoxyuridylate 124-129 thymidylate synthetase Homo sapiens 27-47 12084461-2 2002 TS is an important target for chemotherapy; it is inhibited by folate and nucleotide analogs, such as by 5-fluoro-dUMP (FdUMP), the active metabolite of 5-fluorouracil (5FU). Fluorodeoxyuridylate 105-118 thymidylate synthetase Homo sapiens 0-2 11836594-5 2002 The levels of TS and DPD activities in non-fixed fresh frozen bladder cancer specimens were determined biochemically by the 5-fluoro-2"-deoxyuridine 5"-monophosphate binding assay and the 5-fluorouracil degradation assay, respectively. Fluorodeoxyuridylate 124-165 thymidylate synthetase Homo sapiens 14-16 11750847-15 2002 Incubation of Caki-1 cells with TRAIL enhanced the intracellular accumulation of 5-FU and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 90-131 TNF superfamily member 10 Homo sapiens 32-37 11750847-15 2002 Incubation of Caki-1 cells with TRAIL enhanced the intracellular accumulation of 5-FU and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 133-138 TNF superfamily member 10 Homo sapiens 32-37 10741735-8 2000 A significant correlation was found between TP enzyme activity and 5-fluoro-2"-deoxyuridine-5"-monophosphate binding activity. Fluorodeoxyuridylate 67-108 thymidine phosphorylase Homo sapiens 44-46 11101356-7 2000 Thymidylate synthase inhibition was studied with two forms of the enzyme differing in sensitivities toward 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP), isolated from parental and FdUrd-resistant L1210 cell lines. Fluorodeoxyuridylate 107-148 thymidylate synthase Mus musculus 0-20 11212266-3 2001 In the cell, 5-FU is metabolized to 5-fluoro-2"-deoxyuridine 5"-monophosphate, a tight binding covalent inhibitor of thymidylate synthase. Fluorodeoxyuridylate 36-77 thymidylate synthetase Homo sapiens 117-137 10509749-8 1999 FdUrd is a prodrug of the tight-binding TS inhibitor, 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP). Fluorodeoxyuridylate 54-95 thymidylate synthetase Homo sapiens 40-42 10535743-5 1999 The levels of functional TS in C18 cells were analyzed by the binding of the mechanism-based inhibitor 5-fluoro-2"-deoxyuridylate (FdUMP) under conditions that allowed for the detection of 10 fmol of TS. Fluorodeoxyuridylate 131-136 thymidylate synthetase Homo sapiens 25-27 10697629-2 1999 5-FU is metabolically converted to 5-fluorouracil-2"-deoxyuridine-5"-monophosphate-(FdUMP) which is believed to inhibit DNA synthesis in neoplastic cells by forming a tightly bound ternary complex with thymidylate synthase (TS). Fluorodeoxyuridylate 84-89 thymidylate synthetase Homo sapiens 202-222 10697629-2 1999 5-FU is metabolically converted to 5-fluorouracil-2"-deoxyuridine-5"-monophosphate-(FdUMP) which is believed to inhibit DNA synthesis in neoplastic cells by forming a tightly bound ternary complex with thymidylate synthase (TS). Fluorodeoxyuridylate 84-89 thymidylate synthetase Homo sapiens 224-226 10509749-8 1999 FdUrd is a prodrug of the tight-binding TS inhibitor, 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP). Fluorodeoxyuridylate 97-102 thymidylate synthetase Homo sapiens 40-42 10441376-1 1999 A naturally occurring mutant of human thymidylate synthase (hTS) that contains a Tyr to His mutation at residue 33 was found to confer 4-fold resistance to 5-fluoro-2"-deoxyuridine (FdUrd), a prodrug of 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 203-244 thymidylate synthetase Homo sapiens 38-58 10441376-1 1999 A naturally occurring mutant of human thymidylate synthase (hTS) that contains a Tyr to His mutation at residue 33 was found to confer 4-fold resistance to 5-fluoro-2"-deoxyuridine (FdUrd), a prodrug of 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 203-244 APC down-regulated 1 Homo sapiens 60-63 10441376-1 1999 A naturally occurring mutant of human thymidylate synthase (hTS) that contains a Tyr to His mutation at residue 33 was found to confer 4-fold resistance to 5-fluoro-2"-deoxyuridine (FdUrd), a prodrug of 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 246-251 APC down-regulated 1 Homo sapiens 60-63 10441376-1 1999 A naturally occurring mutant of human thymidylate synthase (hTS) that contains a Tyr to His mutation at residue 33 was found to confer 4-fold resistance to 5-fluoro-2"-deoxyuridine (FdUrd), a prodrug of 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 246-251 thymidylate synthetase Homo sapiens 38-58 10652619-2 1999 We investigated the polymorphism on the repeat length of the TS gene and its relation to the number of 5-fluoro-dUMP (FdUMP) binding sites in human gastrointestinal cancers. Fluorodeoxyuridylate 103-116 thymidylate synthetase Homo sapiens 61-63 9186496-1 1997 Fluorinated pyrimidines, such as 5-fluorouracil (FUra) and 5-fluoro-2"-deoxyuridine (FdUrd), are cytotoxic to cells as a consequence of generation of 5-fluoro-2"-deoxyuridylate (FdUMP), which is a mechanism-based inhibitor of the enzyme thymidylate synthase (TS). Fluorodeoxyuridylate 178-183 thymidylate synthetase Homo sapiens 237-257 10212232-4 1999 The fluoropyrimidines 5-fluorouracil and 5-fluoro-2"-deoxyuridine are cytotoxic as a consequence of inhibition of TS by the metabolite 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 135-176 thymidylate synthetase Homo sapiens 114-116 10212232-4 1999 The fluoropyrimidines 5-fluorouracil and 5-fluoro-2"-deoxyuridine are cytotoxic as a consequence of inhibition of TS by the metabolite 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 178-183 thymidylate synthetase Homo sapiens 114-116 9565579-9 1998 We postulate that the D49G or G52S mutation leads to the structural perturbation of the highly conserved Arg50 loop, decreasing the binding of thymidylate synthase to the inhibitors, Thymitaq and fluorodeoxyuridylate. Fluorodeoxyuridylate 196-216 thymidylate synthetase Homo sapiens 143-163 9701498-0 1998 Acyclic analogues of 5-fluoro-dUMP and 5-fluoro-2"-deoxyuridine: synthesis and inhibition of thymidylate synthase and tumour cell growth. Fluorodeoxyuridylate 21-34 thymidylate synthase Mus musculus 93-113 9535167-4 1997 Included among these structures are complexes of TS bound to substrate dUMP; cofactor CH2THF; the nucleotide analogs 5-fluoro-dUMP, 5-nitro-dUMP and dGMP; and the promising antifolates BW1843, ZD1694, and AG337. Fluorodeoxyuridylate 117-130 thymidylate synthetase Homo sapiens 49-51 9186496-1 1997 Fluorinated pyrimidines, such as 5-fluorouracil (FUra) and 5-fluoro-2"-deoxyuridine (FdUrd), are cytotoxic to cells as a consequence of generation of 5-fluoro-2"-deoxyuridylate (FdUMP), which is a mechanism-based inhibitor of the enzyme thymidylate synthase (TS). Fluorodeoxyuridylate 178-183 thymidylate synthetase Homo sapiens 259-261 9148948-2 1997 In the latter case, the location of TS was established through the use of [6-3H]5-fluorodeoxyuridine, which forms a tight ternary complex of TS with 5-fluorodeoxyuridylate (FdUMP) and 5, 10-methylenetetrahydrofolylpolyglutamate within the cell. Fluorodeoxyuridylate 173-178 thymidylate synthetase Rattus norvegicus 36-38 9148948-2 1997 In the latter case, the location of TS was established through the use of [6-3H]5-fluorodeoxyuridine, which forms a tight ternary complex of TS with 5-fluorodeoxyuridylate (FdUMP) and 5, 10-methylenetetrahydrofolylpolyglutamate within the cell. Fluorodeoxyuridylate 173-178 thymidylate synthetase Rattus norvegicus 141-143 8632414-1 1996 To develop novel lipophilic thymidylate synthase (TS) inhibitors, the X-ray structure of Escherichia coli TS in ternary complex with FdUMP and the inhibitor 10-propargyl-5,8-dideazafolic acid (CB3717) was used as a basis for structure-based design. Fluorodeoxyuridylate 133-138 thymidylate synthetase Homo sapiens 28-48 9155534-3 1997 IFN-alpha may elevate the levels of the active 5-FU metabolite 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) in the cell, possibly leading to increased inhibition of the target enzyme thymidylate synthase (TS), which might enhance DNA damage. Fluorodeoxyuridylate 63-104 interferon alpha 1 Homo sapiens 0-9 9155534-3 1997 IFN-alpha may elevate the levels of the active 5-FU metabolite 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) in the cell, possibly leading to increased inhibition of the target enzyme thymidylate synthase (TS), which might enhance DNA damage. Fluorodeoxyuridylate 63-104 thymidylate synthetase Homo sapiens 188-208 9155534-3 1997 IFN-alpha may elevate the levels of the active 5-FU metabolite 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) in the cell, possibly leading to increased inhibition of the target enzyme thymidylate synthase (TS), which might enhance DNA damage. Fluorodeoxyuridylate 106-111 interferon alpha 1 Homo sapiens 0-9 9155534-3 1997 IFN-alpha may elevate the levels of the active 5-FU metabolite 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) in the cell, possibly leading to increased inhibition of the target enzyme thymidylate synthase (TS), which might enhance DNA damage. Fluorodeoxyuridylate 106-111 thymidylate synthetase Homo sapiens 188-208 8790719-0 1996 Molecular mechanism of thymidylate synthase-catalyzed reaction and interaction of the enzyme with 2- and/or 4-substituted analogues of dUMP and 5-fluoro-dUMP. Fluorodeoxyuridylate 144-157 thymidylate synthetase Homo sapiens 23-43 7627962-6 1995 One of the compounds, the novel pyrimidine analogue 5-ethoxy-2"-deoxyuridine (EOdU), was found to be a substrate for the transferase reaction of TP, to have little or no direct cytotoxicity, to selectively increase the cellular levels of 5-fluoro-dUMP, to enhance the inhibitory effect of FUra on thymidylate synthase activity, and to potentiate the cytotoxicity of FUra and IFN in human colon carcinoma cells. Fluorodeoxyuridylate 238-251 thymidine phosphorylase Homo sapiens 145-147 8823494-1 1996 Interferon (IFN) augments the anabolism of 5-fluorouracil (5FU) to its active metabolite, fluorodeoxyuridylate (FdUMP), which inhibits thymidylate synthase (TS). Fluorodeoxyuridylate 90-110 interferon alpha 1 Homo sapiens 0-10 8823494-1 1996 Interferon (IFN) augments the anabolism of 5-fluorouracil (5FU) to its active metabolite, fluorodeoxyuridylate (FdUMP), which inhibits thymidylate synthase (TS). Fluorodeoxyuridylate 90-110 interferon alpha 1 Homo sapiens 12-15 8823494-1 1996 Interferon (IFN) augments the anabolism of 5-fluorouracil (5FU) to its active metabolite, fluorodeoxyuridylate (FdUMP), which inhibits thymidylate synthase (TS). Fluorodeoxyuridylate 90-110 thymidylate synthetase Homo sapiens 135-155 8790719-2 1996 With two dUMP analogues, 5-fluoro-dUMP (FdUMP) and 5-(trifluoromethyl)-dUMP (CF3dUMP), strong thymidylate synthase inhibitors and active forms of drugs, the inhibition mechanism is based on the reaction mechanism. Fluorodeoxyuridylate 25-38 thymidylate synthetase Homo sapiens 94-114 7641209-1 1995 Thymidylate synthase (TS) is a target enzyme of 5-fluorouracil and is inhibited by 5-fluoro-dUMP (FdUMP) to form an inactive ternary complex. Fluorodeoxyuridylate 83-96 thymidylate synthetase Homo sapiens 0-20 7641209-1 1995 Thymidylate synthase (TS) is a target enzyme of 5-fluorouracil and is inhibited by 5-fluoro-dUMP (FdUMP) to form an inactive ternary complex. Fluorodeoxyuridylate 83-96 thymidylate synthetase Homo sapiens 22-24 8461049-0 1993 Effect of folate diastereoisomers on the binding of 5-fluoro-2"-deoxyuridine-5"-monophosphate to thymidylate synthase. Fluorodeoxyuridylate 52-93 thymidylate synthetase Homo sapiens 97-117 8407987-4 1993 Analysis of the in vitro translation product of FUra-substituted TS mRNA by Western immunoblotting, isoelectric focusing, 5-fluoro-2"-deoxyuridine 5"-monophosphate binding, and TS catalytic activity experiments shows no difference compared to control TS mRNA. Fluorodeoxyuridylate 122-163 thymidylate synthase Oryctolagus cuniculus 65-67 8355668-1 1993 A major mechanism underlying the cytotoxicity of fluoropyrimidine analogs such as 5-fluorouracil and 5-fluoro-2"-deoxyuridine (FdUrd) occurs via the formation of 5-fluoro-2"-deoxyuridylate (FdUMP), a tight-binding inhibitor of thymidylate synthase (TS). Fluorodeoxyuridylate 190-195 thymidylate synthetase Homo sapiens 227-247 7763285-4 1995 Using both the radioenzymatic 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) binding and catalytic assays for measurement of thymidylate synthase (TS) enzyme activity, there was significantly increased TS activity in resistant H630-R1 (13- and 23-fold), H630-R10 (37- and 40-fold), and H630-R (24- and 34-fold) lines, for binding and catalytic assays, respectively, compared with the parent H630 line. Fluorodeoxyuridylate 30-71 thymidylate synthetase Homo sapiens 205-207 8500219-2 1993 The reduced folate 5,10-methylenetetrahydrofolate (CH2FH4) and its precursor tetrahydrofolate (FH4) are essential cofactors for the formation of a tight ternary complex of thymidylate synthase (TS) and 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) derived from FUra. Fluorodeoxyuridylate 202-243 thymidylate synthetase Rattus norvegicus 172-192 8500219-2 1993 The reduced folate 5,10-methylenetetrahydrofolate (CH2FH4) and its precursor tetrahydrofolate (FH4) are essential cofactors for the formation of a tight ternary complex of thymidylate synthase (TS) and 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) derived from FUra. Fluorodeoxyuridylate 245-250 thymidylate synthetase Rattus norvegicus 172-192 1532673-6 1992 The resistant cells showed significantly increased levels of thymidylate synthase, the target enzyme of the fluoropyrimidines" active metabolite, 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP). Fluorodeoxyuridylate 146-187 thymidylate synthetase Homo sapiens 61-81 1532344-3 1992 This acyclonucleoside analogue is an inhibitor of thymidylate synthase (TS) as determined by inhibition of [6-3H]-2"-deoxyuridine incorporation into DNA, inhibition of 3H release from [5-3H]-2"-deoxyuridine, and decrease in both the free and total TS 5"-fluoro-2"-deoxyuridine 5"-monophosphate binding sites. Fluorodeoxyuridylate 251-293 thymidylate synthetase Homo sapiens 50-70 1557655-1 1992 The inhibition of thymidylate synthase (TS) by the fluorouracil (5-FU) metabolite 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) is considered to be one of the main mechanisms of action of 5-FU. Fluorodeoxyuridylate 82-123 thymidylate synthetase Homo sapiens 18-38 1532673-6 1992 The resistant cells showed significantly increased levels of thymidylate synthase, the target enzyme of the fluoropyrimidines" active metabolite, 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP). Fluorodeoxyuridylate 189-194 thymidylate synthetase Homo sapiens 61-81 1557655-1 1992 The inhibition of thymidylate synthase (TS) by the fluorouracil (5-FU) metabolite 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) is considered to be one of the main mechanisms of action of 5-FU. Fluorodeoxyuridylate 82-123 thymidylate synthetase Homo sapiens 40-42 1992915-2 1991 FdUMP, a metabolite of 5-fluorouracil(5-FU), is known to have an inhibitory activity of thymidylate synthase (TS). Fluorodeoxyuridylate 0-5 thymidylate synthetase Homo sapiens 88-108 1557655-1 1992 The inhibition of thymidylate synthase (TS) by the fluorouracil (5-FU) metabolite 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) is considered to be one of the main mechanisms of action of 5-FU. Fluorodeoxyuridylate 125-130 thymidylate synthetase Homo sapiens 18-38 1557655-1 1992 The inhibition of thymidylate synthase (TS) by the fluorouracil (5-FU) metabolite 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) is considered to be one of the main mechanisms of action of 5-FU. Fluorodeoxyuridylate 125-130 thymidylate synthetase Homo sapiens 40-42 1596583-2 1992 In various tumor cell lines and clinical tumor biopsies, TS mRNA levels correlated with TS levels as determined by [3H]-fluorodeoxyuridylate binding. Fluorodeoxyuridylate 120-140 thymidylate synthetase Homo sapiens 57-59 1596583-2 1992 In various tumor cell lines and clinical tumor biopsies, TS mRNA levels correlated with TS levels as determined by [3H]-fluorodeoxyuridylate binding. Fluorodeoxyuridylate 120-140 thymidylate synthetase Homo sapiens 88-90 1924359-6 1991 The inclusion of dUMP, 5-fluoro-dUMP, or 5,10-methylene-tetrahydrofolate in in vitro translation reactions completely relieved the inhibition of TS mRNA translation by TS protein. Fluorodeoxyuridylate 23-36 thymidylate synthetase Homo sapiens 145-147 1924359-6 1991 The inclusion of dUMP, 5-fluoro-dUMP, or 5,10-methylene-tetrahydrofolate in in vitro translation reactions completely relieved the inhibition of TS mRNA translation by TS protein. Fluorodeoxyuridylate 23-36 thymidylate synthetase Homo sapiens 168-170 1992915-2 1991 FdUMP, a metabolite of 5-fluorouracil(5-FU), is known to have an inhibitory activity of thymidylate synthase (TS). Fluorodeoxyuridylate 0-5 thymidylate synthetase Homo sapiens 110-112 2244925-6 1990 In the presence of FdUMP or dUMP, all the studied compounds except 7-hydroxymethotrexate exhibited a large negative enthalpy variation when binding to thymidylate synthase (from -44 to -91 kJ/mol). Fluorodeoxyuridylate 19-24 thymidylate synthetase Homo sapiens 151-171 1827310-0 1991 Thymidylate synthase from untreated human colorectal cancer and colonic mucosa: enzyme activity and inhibition by 5-fluoro-2"-deoxy-uridine-5"-monophosphate. Fluorodeoxyuridylate 114-156 thymidylate synthetase Homo sapiens 0-20 34132895-11 2021 In tumours, there was an association between OAT2 expression and FdUMP concentration. Fluorodeoxyuridylate 65-70 solute carrier family 22 member 7 Homo sapiens 45-49 1697502-6 1990 Thymidylate synthase (TS) activity was measured by both the 5-fluoro-2"-deoxyuridine-5"-monophosphate binding and catalytic assays, using cytosolic extracts. Fluorodeoxyuridylate 60-101 thymidylate synthetase Homo sapiens 0-20 2142214-4 1990 Methotrexate (MTX) pretreatment may also enhance binding of the fluoropyrimidine inhibitor, 5-fluodeoxyuridylate (FdUMP), to the target enzyme, thymidylate synthase (TS), indirectly by increasing dihydrofolate polyglutamates or directly, as MTX polyglutamates, by enhancing the formation of ternary complexes with FdUMP and TS. Fluorodeoxyuridylate 114-119 thymidylate synthetase Homo sapiens 144-164 2142214-4 1990 Methotrexate (MTX) pretreatment may also enhance binding of the fluoropyrimidine inhibitor, 5-fluodeoxyuridylate (FdUMP), to the target enzyme, thymidylate synthase (TS), indirectly by increasing dihydrofolate polyglutamates or directly, as MTX polyglutamates, by enhancing the formation of ternary complexes with FdUMP and TS. Fluorodeoxyuridylate 314-319 thymidylate synthetase Homo sapiens 144-164 2521810-2 1989 Available evidence suggests that the mechanism of this synergism is a kinetic stabilization of complex formed between thymidylate synthase and fluorodeoxyuridylate that also involves a mole of the cofactor for the thymidylate synthase reaction, 5,10-methylenetetrahydrofolate. Fluorodeoxyuridylate 143-163 thymidylate synthetase Homo sapiens 118-138 2729562-2 1989 FAB-MS methods were developed to optimize sensitivity using adenosine 5"-monophosphate as a model compound and then applied to reference standards of two clinically important nucleotides: tricyclic nucleoside-5"-monophosphate (TCNMP) and 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP). Fluorodeoxyuridylate 238-279 FA complementation group B Homo sapiens 0-3 2729562-2 1989 FAB-MS methods were developed to optimize sensitivity using adenosine 5"-monophosphate as a model compound and then applied to reference standards of two clinically important nucleotides: tricyclic nucleoside-5"-monophosphate (TCNMP) and 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP). Fluorodeoxyuridylate 281-286 FA complementation group B Homo sapiens 0-3 2521810-2 1989 Available evidence suggests that the mechanism of this synergism is a kinetic stabilization of complex formed between thymidylate synthase and fluorodeoxyuridylate that also involves a mole of the cofactor for the thymidylate synthase reaction, 5,10-methylenetetrahydrofolate. Fluorodeoxyuridylate 143-163 thymidylate synthetase Homo sapiens 214-234 2977717-7 1988 Each of these agents modifies the response of tumor cells with the result that the fluorodeoxyuridylate-induced inhibition of thymidylate synthase is maintained. Fluorodeoxyuridylate 83-103 thymidylate synthetase Homo sapiens 126-146 3049954-4 1988 However, its conversion to 5-fluoro-2"deoxy-5" monophosphate (FdUMP) leading to inhibition of thymidylate synthase (TS) and subsequently of DNA synthesis, is considered to be its main mechanism of action. Fluorodeoxyuridylate 62-67 thymidylate synthetase Homo sapiens 94-114 3126806-1 1987 Thymidylate synthase (TS), 5-fluorodeoxyuridylate (FdUMP), and 5,10-methylenetetrahydrofolate (CH2-H4folate) form a covalent complex in which a Cys thiol of TS is attached to the 6-position of FdUMP and the one-carbon unit of the cofactor is attached to the 5-position. Fluorodeoxyuridylate 51-56 thymidylate synthetase Homo sapiens 0-20 2963229-4 1987 The most probable mechanism of the interaction between folinic acid and the fluoropyrimidines is stabilization of thymidylate synthase (TS) in inactive complexes with 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) and folate cofactor. Fluorodeoxyuridylate 167-208 thymidylate synthetase Homo sapiens 114-134 3814166-0 1987 Studies on the interaction with thymidylate synthase of analogues of 2"-deoxyuridine-5"-phosphate and 5-fluoro-2"-deoxyuridine-5"-phosphate with modified phosphate groups. Fluorodeoxyuridylate 102-139 thymidylate synthetase Homo sapiens 32-52 2963229-4 1987 The most probable mechanism of the interaction between folinic acid and the fluoropyrimidines is stabilization of thymidylate synthase (TS) in inactive complexes with 5-fluoro-2"-deoxyuridine-5"-monophosphate (FdUMP) and folate cofactor. Fluorodeoxyuridylate 210-215 thymidylate synthetase Homo sapiens 114-134 3745210-1 1986 The formation of covalent binary complexes of thymidylate synthase and its nucleotide substrate dUMP, product dTMP, and inhibitor, 5-fluorodeoxyuridylate (FdUMP) was investigated using the trichloroacetic acid precipitation method. Fluorodeoxyuridylate 155-160 thymidylate synthetase Homo sapiens 46-66 2938731-8 1986 We propose that the elevated TS levels result in sequestration of the reduced-folate pool (as N5,10-methylene tetrahydrofolic acid) into the TS ternary complex with 5-fluoro-2"-deoxyuridine 5"-monophosphate. Fluorodeoxyuridylate 165-206 thymidylate synthase Mus musculus 29-31 2938731-8 1986 We propose that the elevated TS levels result in sequestration of the reduced-folate pool (as N5,10-methylene tetrahydrofolic acid) into the TS ternary complex with 5-fluoro-2"-deoxyuridine 5"-monophosphate. Fluorodeoxyuridylate 165-206 thymidylate synthase Mus musculus 141-143 31520592-5 2019 Furthermore, the tetrahydrofolate- and time-dependent, covalent binding by thymidylate synthase of each 5-fluoro-dUMP and N4-hydroxy-dCMP was shown to be accompanied by the enzyme inactivation, as well as spectrophotometrically confirmed dihydrofolate production, the latter demonstrated to depend on the reaction time, thymidylate synthase activity and temperature of the incubation mixture, further documenting its catalytic character. Fluorodeoxyuridylate 104-117 thymidylate synthase Mus musculus 75-95 3877729-4 1985 In contrast, AE1 cells were highly resistant to almost all other cytotoxic nucleosides including the thymidine analogs, 5-bromodeoxyuridine and 5-fluoro-2"-deoxyuridine 5"-monophosphate. Fluorodeoxyuridylate 144-185 solute carrier family 4 member 1 (Diego blood group) Homo sapiens 13-16 3928628-5 1985 Exposure of the double-labeled thymidylate synthetase-FdUMP-[2-14C,7,9,3",5"-3H]5,10-CH2H4folate complex to the Bratton-Marshall reaction resulted in 16% cleavage of the C-9, N-10 bond with release solely of p-aminobenzoylglutamate, whereas all of the carbon-14-labeled pterin residue remained covalently bound to the protein. Fluorodeoxyuridylate 54-59 complement C9 Homo sapiens 170-173 139127-0 1977 A calorimetric study of the binding of 2"-deoxyuridine-5"-phosphate and 5-fluoro-2"-deoxyuridine-5"-phosphate to thymidylate synthetase. Fluorodeoxyuridylate 72-109 thymidylate synthetase Homo sapiens 113-135 31520592-3 2019 Electrophoretic analysis showed mouse recombinant TS protein to form, in the presence of tetrahydrofolate, a covalently bound, electrophoretically separable 5-fluoro-dUMP-thymidylate synthase complex, similar to that produced in the presence of N5,10-methylenetetrahydrofolate. Fluorodeoxyuridylate 157-170 thymidylate synthase Mus musculus 171-191 6241433-1 1984 A radiochemical assay for thymidylate synthase (EC 2.1.1.45, dTMP synthase), which permits the accurate determination of total, free, and 5-fluoro-2"-deoxyuridylate (FdUMP)-bound enzyme in cells exposed to the 5-fluoropyrimidine anticancer agents, is described. Fluorodeoxyuridylate 166-171 thymidylate synthetase Homo sapiens 26-46 31520592-5 2019 Furthermore, the tetrahydrofolate- and time-dependent, covalent binding by thymidylate synthase of each 5-fluoro-dUMP and N4-hydroxy-dCMP was shown to be accompanied by the enzyme inactivation, as well as spectrophotometrically confirmed dihydrofolate production, the latter demonstrated to depend on the reaction time, thymidylate synthase activity and temperature of the incubation mixture, further documenting its catalytic character. Fluorodeoxyuridylate 104-117 thymidylate synthase Mus musculus 320-340 31520592-4 2019 Further studies of the mouse enzyme binding with 5-fluoro-dUMP/N4-hydroxy-dCMP by TCA precipitation of the complex on filter paper showed it to be tetrahydrofolate-promoted, as well as to depend on both time in the range of minutes and the enzyme molecular activity, indicating thymidylate synthase-catalyzed reaction to be responsible for it. Fluorodeoxyuridylate 49-62 thymidylate synthase Mus musculus 278-298 30486276-8 2018 MTHF and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP) had combined inhibition and significantly downregulated the expression of thymidylate synthase (TS). Fluorodeoxyuridylate 9-50 thymidylate synthetase Homo sapiens 133-153 30486276-8 2018 MTHF and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP) had combined inhibition and significantly downregulated the expression of thymidylate synthase (TS). Fluorodeoxyuridylate 52-57 thymidylate synthetase Homo sapiens 133-153 21561529-0 2011 Calpain regulates thymidylate synthase-5-fluoro-dUMP complex levels associated with response to 5-fluorouracil in gastric cancer cells. Fluorodeoxyuridylate 39-52 thymidylate synthetase Homo sapiens 18-38 21561529-1 2011 Thymidylate synthase (TS) plays a major role in the response to 5-fluorouracil (5-FU) by binding directly to the 5-FU metabolite, 5-fluoro-dUMP (FdUMP). Fluorodeoxyuridylate 130-143 thymidylate synthetase Homo sapiens 0-20 21561529-1 2011 Thymidylate synthase (TS) plays a major role in the response to 5-fluorouracil (5-FU) by binding directly to the 5-FU metabolite, 5-fluoro-dUMP (FdUMP). Fluorodeoxyuridylate 145-150 thymidylate synthetase Homo sapiens 0-20 17237272-1 2007 Multidrug-resistance-associated protein, MRP8/ABCC11 (ABCC11), is an efflux pump for nucleotide analogues and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 110-151 ATP binding cassette subfamily C member 3 Homo sapiens 0-39 17237272-1 2007 Multidrug-resistance-associated protein, MRP8/ABCC11 (ABCC11), is an efflux pump for nucleotide analogues and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 110-151 ATP binding cassette subfamily C member 11 Homo sapiens 41-45 17237272-1 2007 Multidrug-resistance-associated protein, MRP8/ABCC11 (ABCC11), is an efflux pump for nucleotide analogues and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 110-151 ATP binding cassette subfamily C member 11 Homo sapiens 46-52 17237272-1 2007 Multidrug-resistance-associated protein, MRP8/ABCC11 (ABCC11), is an efflux pump for nucleotide analogues and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 110-151 ATP binding cassette subfamily C member 11 Homo sapiens 54-60 17237272-1 2007 Multidrug-resistance-associated protein, MRP8/ABCC11 (ABCC11), is an efflux pump for nucleotide analogues and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 153-158 ATP binding cassette subfamily C member 3 Homo sapiens 0-39 17237272-1 2007 Multidrug-resistance-associated protein, MRP8/ABCC11 (ABCC11), is an efflux pump for nucleotide analogues and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 153-158 ATP binding cassette subfamily C member 11 Homo sapiens 41-45 17237272-1 2007 Multidrug-resistance-associated protein, MRP8/ABCC11 (ABCC11), is an efflux pump for nucleotide analogues and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 153-158 ATP binding cassette subfamily C member 11 Homo sapiens 46-52 17237272-1 2007 Multidrug-resistance-associated protein, MRP8/ABCC11 (ABCC11), is an efflux pump for nucleotide analogues and 5-fluoro-2"-deoxyuridine 5"-monophosphate (FdUMP). Fluorodeoxyuridylate 153-158 ATP binding cassette subfamily C member 11 Homo sapiens 54-60 26916840-0 2016 Phosphorylation of thymidylate synthase affects slow-binding inhibition by 5-fluoro-dUMP and N(4)-hydroxy-dCMP. Fluorodeoxyuridylate 75-88 thymidylate synthase Mus musculus 19-39 23641929-0 2013 Localization of putative binding sites for cyclic guanosine monophosphate and the anti-cancer drug 5-fluoro-2"-deoxyuridine-5"-monophosphate on ABCC11 in silico models. Fluorodeoxyuridylate 99-140 ATP binding cassette subfamily C member 11 Homo sapiens 144-150