Suppr超能文献

油酸是蘑菇大秃马勃中抑制Bcr-Abl激酶自磷酸化活性的活性成分。

Oleic acid is the active component in the mushroom Daedalea gibbosa inhibiting Bcr-Abl kinase autophosphorylation activity.

作者信息

Khamaisie Hazem, Sussan Sherbel, Tal Michael, Najajreh Yousef, Ruthardt Martin, Mahajna Jamal

机构信息

Cancer Drug Discovery Program, Migal, Kiryat Shmona, 11016, Israel.

出版信息

Anticancer Res. 2011 Jan;31(1):177-83.

Abstract

The hallmark of chronic myeloid leukemia (CML) is the abnormal activity of p210(Bcr-Abl) kinase. Selective kinase inhibitors such as imatinib or nilotinib have been established successfully for the treatment of CML. Despite high rates of clinical response, CML patients can develop resistance to these kinase inhibitors mainly due to point mutations within the Abl kinase domain of the fusion protein. Previously, we reported that a crude extract of the mushroom Daedalea gibbosa inhibited kinase activity of Bcr-Abl kinase. Here we report on the identification of the active component of Daedalea gibbosa, oleic acid, which inhibited Bcr-Abl kinase autophosphorylation in Ba/F3 cells and exhibited anti-CML activity in a BCR/ABL-positive mouse model.

摘要

慢性髓性白血病(CML)的标志是p210(Bcr-Abl)激酶的异常活性。选择性激酶抑制剂如伊马替尼或尼罗替尼已成功用于治疗CML。尽管临床缓解率很高,但CML患者可能会对这些激酶抑制剂产生耐药性,主要原因是融合蛋白的Abl激酶结构域内的点突变。此前,我们报道过蘑菇大秃马勃的粗提物可抑制Bcr-Abl激酶的活性。在此我们报告大秃马勃活性成分油酸的鉴定,该成分可抑制Ba/F3细胞中Bcr-Abl激酶的自磷酸化,并在BCR/ABL阳性小鼠模型中表现出抗CML活性。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验