Effect of polyglutamylation of 5,10-methylenetetrahydrofolate on the binding of 5-fluoro-2'-deoxyuridylate to thymidylate synthase purified from a human colon adenocarcinoma xenografT
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Cited by (72)
Drug resistance in colorectal cancer: General aspects
2020, Drug Resistance in Colorectal Cancer: Molecular Mechanisms and Therapeutic StrategiesFolylpoly-γ-glutamate synthetase: A key determinant of folate homeostasis and antifolate resistance in cancer
2016, Drug Resistance UpdatesCitation Excerpt :Porcine TS displayed preference toward the tetraglutamate form of FA with a 175-fold decrease in the Km (Matthews et al., 1987). Several other studies characterized the various affinity/dissociation constants of TS for different folate-polyglutamates, all showing an increased affinity toward long chain polyglutamates, accompanied by increased stability of TS's ternary complexes with dUMP and 5,10-MTHF (Danenberg and Lockshin, 1982; Dolnick and Cheng, 1978; Radparvar et al., 1989). Furthermore, steady-state kinetic characterization of human MTHFD1L activity performed using the (6R,S)-THF-Glu1, (6R,S)-THFGlu3 and (6R,S)-THF-PteGlu5 substrates, revealed that the Km of MTHFD1L dropped from >0.5 mM for the monoglutamate form to 15 μM and 3.6 μM toward the tri- and pentaglutamates, respectively (Walkup and Appling, 2005).
A review of the evolution of systemic chemotherapy in the management of colorectal cancer
2015, Clinical Colorectal CancerCitation Excerpt :The potentiation of 5-FU activity was shown to be mediated by the formation of a stable ternary complex consisting of FdUMP, MTHF, and thymidylate synthase.10,13,24 Polyglutamate derivatives of MTHF were shown to substantially increase the efficiency of binding of FdUMP to thymidylate synthase compared with monoglutamate derivatives, in a human colon adenocarcinoma xenograft25 and human Michigan Cancer Foundation-7 breast cancer cells.26 In a pivotal in vitro study of the biomodulation of 5-FU activity by the reduced folate leucovorin (5-formyl tetrahydrofolate [THF]), Ullman et al19 reported that 20 μM leucovorin enhanced 5-FU cytotoxicity approximately fivefold in cultured leukemia cells.
Epigenetics and chemoresistance in colorectal cancer: An opportunity for treatment tailoring and novel therapeutic strategies
2011, Drug Resistance UpdatesCitation Excerpt :The stability of this complex is highly dependent on the different size and composition of cellular folate cofactor pools (Yin et al., 1983) while the formation of an unstable binary complex results in poor enzyme inhibition (Lockshin and Danenberg, 1981). The low availability of cofactor and its polyglutamates in tumors thus leads to intrinsic resistance to 5-FU (Houghton et al., 1981; Radparvar et al., 1989; Aschele et al., 1992). This has provided the rational basis for the use of combination treatment regimens of folinic acid and 5-FU for colorectal cancer (Mini et al., 1990).
Folylpolyglutamate synthase and γ-glutamyl hydrolase regulate leucovorin-enhanced 5-fluorouracil anticancer activity
2008, Biochemical and Biophysical Research CommunicationsCitation Excerpt :First, downregulating GGH might increase the accumulation or retention of CH2THF and consequently enhance the sensitivity of cells to FdUrd. Second, downregulating GGH might extend the length of the glutamate chains in CH2THF; as CH2THF with longer polyglutamate chains has been reported to more efficiently form and stabilize ternary complexes with TS and FdUMP [13], this might also enhance the sensitivity to FdUrd. Kidd et al. reported high expression levels of FPGS and GGH mRNAs in colorectal tumors compared with normal tissue, with great variability between patients [14].
Expression and clinical significance of methylenetetrahydrofolate reductase in patients with colorectal cancer
2006, Clinical Colorectal Cancer