Vanoxonin, a new inhibitor of thymidylate synthetase.
نویسندگان
چکیده
Vanoxonin, a new inhibitor of thymidylate synthetase, was found in cultured broths of the strain MG245-CF2 classified as Saccharopolyspora hirsuta. Vanoxonin, C18H25N3O9, was obtained as colorless powder. Vanoxonin forms a vanadium complex which exhibits a strong inhibition against thymidylate synthetase. The concentration for 50% inhibition of the enzyme (IC50) was 0.7 micrograms/ml.
منابع مشابه
Enzyme studies with new analogues of folic acid and homofolic acid.
Many new analogues of dihydrofolate and dihydrohomofolate have been synthesized and tested as substrates of dihydrofolate reductase. Since all of the dihydroderivatives were efficiently reduced by the action of dihydrofolate reductase from L1210 mouse leukemia cells, the tetrahydroderivatives thus formed could be tested directly for cofactor and inhibitor activity with thymidylate synthetase. A...
متن کاملThe role of thymidylate synthetase inhibitors in bromodeoxyuridine-induced neoplasia in Drosophila.
When 5-bromodeoxyuridine (BUdR) or 5-iododeoxyuridine is administered to Drosophila larvae together with 5-fluorouracil, many of the adult flies show growth lesions in the form of extra bristles and other supernumerary wing structures. The hypothesis that the growth lesions are the result of thymidine analog incorporation in DNA and that the effects of this incorporation are increased by feedin...
متن کاملConditions allowing synthesis of thymidylate synthetase at the nonpermissive temperature in a temperature-sensitive thy mutant normally blocked in its translation.
Escherichia coli thyAl is a temperature-sensitive mutant altered in the structural gene for thymidylate synthetase. A previous study from this laboratory has shown that thyAl belongs to a new class of temperature-sensitive mutants (Group IV) and is blocked in the synthesis of thymidylate synthetase at the level of the polyribosome complex. The block has been postulated to result from a conforma...
متن کاملOverproduction of a bifunctional thymidylate synthetase-dihydrofolate reductase and DNA amplification in methotrexate-resistant Leishmania tropica.
Leishmania tropica promastigotes that are highly resistant to methotrexate, a dihydrofolate reductase inhibitor, have been developed. Organisms resistant to 1 mM methotrexate have a 40-fold increase in dihydrofolate reductase which is associated with thymidylate synthetase, and they contain amplified regions of DNA that may be directly visualized on stained gels of restriction digests. The ampl...
متن کاملElevation of dihydrofolate reductase, thymidylate synthetase, and thymidine kinase in cultured mammalian cells after exposure to folate antagonists.
Roswell Park Memorial Institute 4265 human lymphoblasts were grown with three dihydrofolate reductase inhibitors: a 2,4-diaminopteridine, methotrexate; a 2,4-diaminoquinazoline, chlorasquin; and, a 2,4-diaminotriazine, triazinate. In the absence of inhibitor, dihydrofolate reductase activity increased to a peak at mid-log growth and then declined during the later growth stages. When cells were ...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- The Journal of antibiotics
دوره 36 6 شماره
صفحات -
تاریخ انتشار 1983