Wynik wyszukiwania w bazie Polska Bibliografia Lekarska GBL

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Tytuł oryginału: Synthesis and biological activity of Nŕ-[4-[N-(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]-N-propargylamino]phenylacetyl]-L-gluatimic acid.
Autorzy: Kusakiewicz-Dawid Anna, Bugaj Marta, Dzik Jolanta M., Gołos Barbara, Wińska Patrycja, Pawełczak Krzysztof, Rzeszotarska Barbara, Rode Wojciech
Źródło: Acta Bioch. Pol. 2002: 49 (1) s.197-203, il., tab., bibliogr. [17] poz. - 8 Międzynarodowe Sympozjum pt. Aspekty molekularne chemioterapii Gdańsk 09. 2001
Sygnatura GBL: 303,116

Hasła klasyfikacyjne GBL:
  • farmacja
  • gastroenterologia
  • onkologia

    Typ dokumentu:
  • praca związana ze zjazdem
  • praca doświadczalna

    Wskaźnik treści:
  • zwierzęta
  • szczury

    Streszczenie angielskie: 2-Deamino-2-methyl-N10-propargyl-5,8-dideazafolic acid (ICI 198583) is a potent inhibitor of thymidylate synthase. Its analgue, Nŕ-[4-[N-[(3,4-dihydro-2-methyl-4-oxo-6-quinazoliny)methyl]-N-propargylamino]phenylacetyl]-L]glutamic acid, containing p-aminohenylacetic acd residue substituting p-aminobenzoic acid residue, was synthesized. The new analogue exhibited a moderately potent thyidylate synthase inhibition, of linear mixed type vs. the cofactor, N1,10-methylenetetrahydrofolate. The Ki value of 0.34 ćM, determined with a purified recombinant rat hepatoma enzyme, was about 30-fold higher than that reported for inhibition of thymidylate synthase from mouse leukemia L1210 cells by ICI 198583 (Hughes et al., 1990, J. Med. Chem. 33, 3060). Growth of mouse leukemia L5178Y cells was inhibited by the analogue (IC50 = 1.25 mM) 180-fold weaker than by ICI 198583 (IC50 = 6.9 ćM).

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    Tytuł oryginału: The effect of Arg209 to Lys mutation in mouse thymidylate synthase.
    Autorzy: Cieśla Joanna, Gołos Barbara, Wałajtys-Rode Elżbieta, Jagielska Elżbieta, Płucienniczak Andrzej, Rode Wojciech
    Źródło: Acta Bioch. Pol. 2002: 49 (3) s.651-658, il., tab., bibliogr. s. 657-658
    Sygnatura GBL: 303,116

    Hasła klasyfikacyjne GBL:
  • genetyka
  • onkologia
  • hematologia
  • mikrobiologia

    Typ dokumentu:
  • praca doświadczalna
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • zwierzęta
  • myszy

    Streszczenie angielskie: Mouse thymidylate synthase R209K (a mutation corresponding to R218K in Lactobacillus casei), overexpressed in thymidylate synthase-deficient Escherichia coli strain, was poorly soluble and with only feeble enzyme activity. The mutated protein, incubated with FdUMP and N5,10 -methylenetetrahydrofolate, did not form a complex stable under conditions of SDS/polyacrylamide gel electrophoresis. The reaction catalyzed by the R209K enzyme (studied in a crude extract), compared to that catalyzed by purified wild-type recombinant mouse thymidylate synthase, showed the Km value for dUMP 571-fold higher and Vmax value over 50-fold (assuming that the mutated enzyme constituted 20 p.c. of total crude extract protein) lower. Thus the ratios kcat, R209K/kcat, 'wild' and (kcat, R209K/Km, R209K**dUMP)/(kcat, 'wild'/Km, 'wild'**dUMP) were 0.019 and 0.000032, respectively, documenting that mouse thymidylate synthase R209, similar to the corresponding L. casei R218, is essential for both dUMP binding and enzyme reaction.

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    Tytuł oryginału: Sulfamide antifolates inhibiting thymidylate synthase: synthesis, enzyme inhibition and cytotoxicity.
    Autorzy: Pawełczak Krzysztof, Makowski Maciej, Kempny Michał, Dzik Jolanta M., Gołos Barbara, Rode Wojciech, Rzeszotarska Barbara
    Źródło: Acta Bioch. Pol. 2002: 49 (2) s.407-420, il., tab., bibliogr. s. 418-420 - 1046 Międzynarodowe Sympozjum nt. biologii i chemii pochodnych pterydyny i folionówMiędzynarodowe Sympozjum nt. molekularnych aspektów chemioterapiiMiędzynarodowy Kongres nt. leczenia przeciwnowotworowego Orange BeachGdańskParyż 199319931996
    Sygnatura GBL: 303,116

    Hasła klasyfikacyjne GBL:
  • gastroenterologia
  • onkologia

    Typ dokumentu:
  • tytuł obcojęzyczny
  • praca związana ze zjazdem
  • praca doświadczalna

    Wskaźnik treści:
  • zwierzęta
  • myszy
  • in vitro

    Streszczenie angielskie: Synthesis and biological evaluation are described of seven new analogues (309) of two potent thymidylate synthase inhibitors, 10-propargyl-5,8-dideazafolate (1) and its 2-methyll-2-deamino congener ICI 198583 (2). While the new compounds 3 and 4 were analogues of 1 and 2, respectively, containing a p-aminobenzenesulfonyl residue in place of the p-aminobenzoic acid residue, the remaining 5 new compounds were analogues of 4 with the L-glutamic acid residue replaced by glycine (5), L-valine (6), L-alanine (7), L-phenylglycine (8) or L-norvaline (9). The new analogues were tested as inhibitors of thymidylate synthases isolated from tumour (Ehrilich carcinoma), parasite (Hymenolepis diminuta) and normal tissue (regenerating ratliver) and found to ve weaker inhibitors than the parent 10-propargyl-5,8-dideazafolic acid. Selected new analogues, tested as inihbitors of growth of mouse leukemia L 5178Y cells, were less potent than the parent 10-propargyl-5,8-dideazafolic acid. Substitution of the glutamyl residue in compound 4 with L-norvaline (9) resulted in only a 5-fold stronger thymidylate synthase inhibitor, but a 40-fold weaker cell growth inhibitor.

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