Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

Weisberg E; Manley PW; Breitenstein W; Bruggen J; Cowan Jacob SW; Ray A; Huntly B; Fabbro D; Fendrich G; Hall Meyers E; Kung AL; Mestan J; Daley GQ; Callahan L; Catley L; Cavazza C; Mohammed A; Neuberg D; Wright RD; Gilliland DG; Griffin JD

首页> 外文期刊>Cancer Cell >Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

【24h】

Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

机译：AMN107的表征，AMN107是天然和突变Bcr-Abl的选择性抑制剂。

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

The Bcr-Abl tyrosine kinase oncogene causes chronic myelogenous leukemia (CML) and Philadelphia chromosome-positive (Ph+) acute lymphoblastic leukemia (ALL). We describe a novel selective inhibitor of Bcr-Abl, AMN107 (IC50 <30 nM), which is significantly more potent than imatinib, and active against a number of imatinib-resistant Bcr-Abl mutants. Crystallographic analysis of Abl-AMN107 complexes provides a structural explanation for the differential activity of AMN107 and imatinib against imatinib-resistant Bcr-Abl. Consistent with its in vitro and pharmacokinetic profile, AMN107 prolonged survival of mice injected with Bcr-Abl-transformed hematopoietic cell lines or primary marrow cells, and prolonged survival in imatinib-resistant CML mouse models. AMN107 is a promising new inhibitor for the therapy of CML and Ph+ ALL.

机译：Bcr-Abl酪氨酸激酶致癌基因可导致慢性粒细胞性白血病（CML）和费城染色体阳性（Ph +）急性淋巴细胞白血病（ALL）。我们描述了一种新型的Bcr-Abl选择性抑制剂AMN107（IC50 <30 nM），其显着比伊马替尼更有效，并且对许多对伊马替尼耐药的Bcr-Abl突变体具有活性。 Abl-AMN107复合物的晶体学分析为AMN107和伊马替尼针对伊马替尼耐药的Bcr-Abl的差异活性提供了结构解释。与其体外和药代动力学特征一致，AMN107延长了注射Bcr-Abl转化的造血细胞系或原代骨髓细胞的小鼠的存活，并延长了对伊马替尼耐药的CML小鼠的存活。 AMN107是一种有前途的新型抑制剂，可用于治疗CML和Ph + ALL。

著录项

来源
《Cancer Cell》 |2005年第2期|共13页
作者
Weisberg E; Manley PW; Breitenstein W; Bruggen J; Cowan Jacob SW; Ray A; Huntly B; Fabbro D; Fendrich G; Hall Meyers E; Kung AL; Mestan J; Daley GQ; Callahan L; Catley L; Cavazza C; Mohammed A; Neuberg D; Wright RD; Gilliland DG; Griffin JD;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类肿瘤学;
关键词
IMATINIB; BCR Gene; mutant; survival aspects; Laboratory mice;

机译：IMATINIB;BCR基因;突变;存活情况;实验室小鼠;

相似文献

外文文献
中文文献
专利

1. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl. [J] . Weisberg E, Manley PW, Breitenstein W, Cancer Cell . 2005,第2期

机译：AMN107的表征，AMN107是天然和突变Bcr-Abl的选择性抑制剂。
2. Nilotinib (formerly AMN107), a highly selective BCR-ABL tyrosine kinase inhibitor, is active in patients with imatinib-resistant or -intolerant accelerated-phase chronic myelogenous leukemia. [J] . le-Coutre P, Ottmann OG, Giles F, Blood: The Journal of the American Society of Hematology . 2008,第4期

机译：尼罗替尼（以前的AMN107）是一种高度选择性的BCR-ABL酪氨酸激酶抑制剂，对伊马替尼耐药或不耐受的加速期慢性粒细胞白血病患者有效。
3. AMN107 (nilotinib): a novel and selective inhibitor of BCR-ABL [J] . E Weisberg, P Manley, J Mestan, British Journal of Cancer . 2006,第12期

机译：AMN107（尼洛替尼）：一种新型的选择性BCR-ABL抑制剂
4. Selective tyrosine kinase inhibitor, STI571, inhibitsgrowth of p53 mutant anaplastic thyroid cancer cellsby inducing S-G2 transition arrest [C] . Alexei P. Podtcheko, Satoshi Tsuda, Akira Ohtsuru International Consortium for Medical Care of Hibakusha and Radiation Life Science . 2003

机译：选择性酪氨酸激酶抑制剂，STI571，P53突变体的抑制性诱导S-G2过渡逮捕的抑制性甲状腺癌细胞
5. Development and characterization of wheat mutants resistant to acetyl co-enzyme A carboxylase inhibitors. [D] . Ostlie, Michael H. 2012

机译：抗乙酰辅酶A羧化酶抑制剂的小麦突变体的开发和鉴定。
6. Discovery and characterization of a novel highly potent and selective type II native and drug-resistant V299L mutant BCR-ABL inhibitor (CHMFL-ABL-039) for Chronic Myeloid Leukemia (CML) [O] . Jiaxin Wu, Aoli Wang, Xixiang Li, 2019

机译：发现和表征一种新型的强效和选择性II型天然和耐药V299L突变型BCR-ABL抑制剂（CHMFL-ABL-039）用于治疗慢性粒细胞白血病（CML）
7. Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl [O] . Weisberg Ellen, Manley Paul W., Breitenstein Werner, 2005

机译：AMN107的表征，AMN107是天然和突变Bcr-Abl的选择性抑制剂

Characterization of AMN107, a selective inhibitor of native and mutant Bcr-Abl.

摘要

著录项

相似文献

相关主题

期刊订阅