Zobrazeno 1 - 10
of 44
pro vyhledávání: '"R G Moran"'
Publikováno v:
JNCI Journal of the National Cancer Institute. 85:1154-1159
Background Cancer chemotherapy with folate antimetabolites has been traditionally targeted at the enzyme dihydrofolate reductase and is based on the requirement of dividing tumor cells for a supply of thymidylate and purines. However, a new compound,
Publikováno v:
Advances in Enzyme Regulation. 31:13-27
Heterocyclic para-aminobenzoate modifications of 2-desamino-2-methyl-5,8-dideazafolic acid and a series of its N10-substituted analogs have produced a number of interesting compounds that have enabled a deeper understanding of the biochemical events
Autor:
S A, Titus, R G, Moran
Publikováno v:
The Journal of biological chemistry. 275(47)
The transduction of a human placental cDNA retroviral library into glyB cells, a Chinese hamster ovary K1 subline that is deficient in the transport of folates into mitochondria, resulted in the complementation of glycine auxotrophy of these cells. A
Publikováno v:
Cancer research. 59(24)
Folates and folate antimetabolites are metabolically trapped in mammalian cells as polyglutamates, a process catalyzed by folylpoly-gamma-glutamate synthetase (FPGS). Using 5'-rapid amplification of cDNA ends, RNase protection assays, transfection of
Autor:
R G, Moran
Publikováno v:
Seminars in oncology. 26(2 Suppl 6)
Folylpoly-gamma-glutamate synthetase (FPGS) catalyzes the addition of several equivalents of glutamic acid to the gamma-carboxyl group in the side chain of folate cofactors and analogs. Folylpoly-gamma-glutamate synthetase has three functions in fola
Autor:
A, Tse, R G, Moran
Publikováno v:
The Journal of biological chemistry. 273(40)
Mouse L1210 cell variants were selected for resistance to 5, 10-dideazatetrahydrofolate, a potent inhibitor of the first folate-dependent enzyme in de novo purine synthesis, glycinamide ribonucleotide formyltransferase. The drug-resistant phenotype s
Publikováno v:
Cancer research. 56(10)
Recent clinical trials with lometrexol [(6R)-5,10-dideazatetrahydrofolate] have revealed a level of toxicity in humans that was not predicted on the basis of previous in vivo preclinical studies. Because standard laboratory animal diets contain high
Publikováno v:
Cancer research. 55(24)
The cytotoxicity, and probably the selectivity, of folate antimetabolites depend upon the expression of the enzyme folylpoly-gamma-glutamate synthetase in tumor cells. Evidence for the existence of multiple forms of this enzyme and the need to define
Autor:
L L, Habeck, L G, Mendelsohn, C, Shih, E C, Taylor, P D, Colman, L S, Gossett, T A, Leitner, R M, Schultz, S L, Andis, R G, Moran
Publikováno v:
Molecular pharmacology. 48(2)
The metabolism of 5,10-dideazatetrahydrofolate (DDATHF [lometrexol]) to polyglutamate derivatives by folylpoly-gamma-glutamate synthetase (FPGS) plays a central role in the activity of this compound as an antineoplastic agent. The availability of a s
Publikováno v:
Molecular pharmacology. 45(2)
Previous attempts to design inhibitors of mammalian folylpolyglutamate synthetase (FPGS) have resulted in three classes of active compounds, all of which have charged moieties in the side chain, but structural alteration of the rest of the folate mol