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Вид документа : Статья из журнала

РЖ ВИНИТИ 76 (BI30) 97.02-04Н2.96

Автор(ы) : Lambe Catherine U., Averett Devron R., Paff Melanie T., Reardon John E., Wilson Joan G., Krenitsky Thomas A.
Заглавие : 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies
Источник статьи : Cancer Res. - 1995. - Vol. 55, N 15. - С. 3352-3356
Аннотация: 2-Amino-6-methoxypurine arabinoside (506U) is a water-soluble prodrug converted to ara-G by adenosine deaminase. 506U is not a substrate for deoxycytidine kinase, adenosine kinase, or purine nucleoside phosphorylase and is phosphorylated by mitochondrial deoxyguanosine kinase at a rate 4% that of ara-G phosphorylation. Mitochondrial DNA polymerase was the least sensitive to ara-GTP inhibition of the five human DNA polymerases tested. [{3}H]506U was anabolized to ara-G 5'-phosphates in CEM cells but not to phosphorylated metabolites of 506U. 506U was selective for transformed T over B cells and also inhibited growth in two of three monocytic lines tested. 506U given i.v. to cynomolgus monkeys was rapidly converted to ara-G; the ara-G had a half-life of approximately 2 h. 506U had in vivo dose-dependent efficacy against human T-cell tumors in immunodeficient mice. A Phase 1 trial of 506U against refractory hematological malignancies is now in progress at two study sites. Библ. 27
ГРНТИ : 76.29.49
Предметные рубрики: ПРОТИВООПУХОЛЕВЫЕ СРЕДСТВА
2-АМИНО-6-МЕТОКСИПУРИНА АРАБИНОЗИД
ARA G
506 U
ХИМИОТЕРАПИЯ
ФАЗА 1
ГЕМОБЛАСТОЗЫ
Т-КЛЕТОЧНЫЕ
ОБЕЗЬЯНЫ
ЧЕЛОВЕК
Дата ввода:

Вид документа : Статья из журнала

РЖ ВИНИТИ 76 (BI28) 97.01-04Н3.108

Автор(ы) : Lambe Catherine U., Averett Devron R., Paff Melanie T., Reardon John E., Wilson Joan G., Krenitsky Thomas A.
Заглавие : 2-Amino-6-methoxypurine arabinoside: An agent for T-cell malignancies
Источник статьи : Cancer Res. - 1995. - Vol. 55, N 15. - С. 3352-3356
Аннотация: 2-Amino-6-methoxypurine arabinoside (506U) is a water-soluble prodrug converted to ara-G by adenosine deaminase. 506U is not a substrate for deoxycytidine kinase, adenosine kinase, or purine nucleoside phosphorylase and is phosphorylated by mitochondrial deoxyguanosine kinase at a rate 4% that of ara-G phosphorylation. Mitochondrial DNA polymerase was the least sensitive to ara-GTP inhibition of the five human DNA polymerases tested. [{3}H]506U was anabolized to ara-G 5'-phosphates in CEM cells but not to phosphorylated metabolites of 506U. 506U was selective for transformed T over B cells and also inhibited growth in two of three monocytic lines tested. 506U given i.v. to cynomolgus monkeys was rapidly converted to ara-G; the ara-G had a half-life of approximately 2 h. 506U had in vivo dose-dependent efficacy against human T-cell tumors in immunodeficient mice. A Phase 1 trial of 506U against refractory hematological malignancies is now in progress at two study sites. Библ. 27
ГРНТИ : 76.29.49
Предметные рубрики: ПРОТИВООПУХОЛЕВЫЕ СРЕДСТВА
2-АМИНО-6-МЕТОКСИПУРИНА АРАБИНОЗИД
ARA G
506 U
ХИМИОТЕРАПИЯ
ФАЗА 1
ГЕМОБЛАСТОЗЫ
Т-КЛЕТОЧНЫЕ
ОБЕЗЬЯНЫ
ЧЕЛОВЕК
Дата ввода:

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