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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Effects of Hibarimicins and Hibarimicin-Related Compounds produced by Microbispora on v-Src Kinase Activity and Growth and Differentiation of Human Myeloid Leukemia HL-60 Cells
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Effects of Hibarimicins and Hibarimicin-Related Compounds produced by Microbispora on v-Src Kinase Activity and Growth and Differentiation of Human Myeloid Leukemia HL-60 Cells

机译：微双孢菌产生的hibarimicins和hibarimicin相关化合物对v-Src激酶活性以及人骨髓白血病HL-60细胞生长和分化的影响

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摘要

We studied the effects of hibarimicins and hibarimicin-related compounds produced by Microbispora rosea subsp. hibaria [glycosides (hibarimicins A, B, C,,E,G,H and I)] and aglycon(hibarimicinone)] or compounds produced by its mutants [glycosides (HMP-P4 and -Y6), aglycons (HMP-P1 and -Y1) and shunt products(HMP-M1, M2, M3, and -M4)] on v-Src tyrosine kinase and growth and differentiation of human myeloid leukemia HL-60 cells, Among them, hibarimicin B was a strong and the most selective v-Src kinase inhibitor with differentiation but had to no v-Src kinase inhibitory activity, Hibarimicinone was the most potent v-Src kinase inhibitor, although less selective, and did not induce differentiation of HL-60 cells. Hibarimicin B competitively inhibited ATP binding to the v-Src kinase, but hibarimicinone showed noncompetitive inhibition .These two compounds, however, showed similar mixed types suggest that signaling molecules other than Src might be more important in the differentiation induction of HL-60 cells
机译：我们研究了玫瑰红双孢菌亚种产生的hibarimicins和hibarimicin相关化合物的作用。希贝里亚[糖苷（糖苷（A，B，C ,, E，G，H和I）]和糖苷（hibarimicinone）]或其突变体[糖苷（HMP-P4和-Y6），糖苷（HMP-P1和-Y1）和分流产物（HMP-M1，M2，M3和-M4）对v-Src酪氨酸激酶的作用以及人类髓样白血病HL-60细胞的生长和分化，其中，hibarimicin B最强，最选择性v-Src激酶抑制剂具有分化能力，但没有v-Src激酶抑制活性，Hibarimicinone是最有效的v-Src激酶抑制剂，尽管选择性较低，并且不诱导HL-60细胞分化。 Hibarimicin B竞争性地抑制ATP与v-Src激酶的结合，但是hibarimicinone表现出非竞争性抑制作用。然而，这两种化合物的混合类型相似，表明Src以外的信号分子可能在HL-60细胞的分化诱导中更重要

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