The background, discovery and clinical development of BCR-ABL inhibitors

LambertG.K.; Duhme-KlairA.-K.; MorganT.; RamjeeM.K.

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The background, discovery and clinical development of BCR-ABL inhibitors

机译：BCR-ABL抑制剂的背景，发现和临床开发

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The story of the inhibition of BCR-ABL as a treatment for chronic myelogenous leukaemia serves to illustrate key aspects of the kinase drug discovery and development process. Firstly, elucidation of the disease mechanism enabled identification of the molecular target(s) which catalysed pharmaceutical research and resulted in Gleevec? (Novartis) as the first FDA approved BCR-ABL inhibitor. However, clinical success was soon tempered by the emergence of drug resistance through various mechanisms. Using rational drug design, several hypotheses were devised to overcome resistance issues leading to the development of second generation inhibitors, providing clinicians and patients with greater therapeutic choice.

机译：BCR-ABL作为慢性髓性白血病治疗的抑制的故事是为了说明激酶药物发现和发育过程的关键方面。首先，阐明疾病机制的鉴定鉴定了催化药学研究的分子靶标并导致Gleevec？（Novartis）作为第一个FDA批准的BCR-ABL抑制剂。然而，临床成功很快通过各种机制出现耐药性的抗药性。使用理性药物设计，设计了几个假设，以克服导致第二代抑制剂发展的抵抗问题，为临床医生和患者提供更大的治疗选择。

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《Drug discovery today》 |2013年第20期|共8页
作者
LambertG.K.; Duhme-KlairA.-K.; MorganT.; RamjeeM.K.;
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Department of Chemistry University of York Heslington York YO10 5DD United Kingdom;

Department of Chemistry University of York Heslington York YO10 5DD United Kingdom;

Cyclofluidic Limited BioPark Welwyn Garden City AL7 3AX United Kingdom;

Cyclofluidic Limited BioPark Welwyn Garden City AL7 3AX United Kingdom;

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正文语种 eng
中图分类药学;
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1. The background, discovery and clinical development of BCR-ABL inhibitors [J] . LambertG.K., Duhme-KlairA.-K., MorganT., Drug discovery today . 2013,第19a20期

机译：BCR-ABL抑制剂的背景，发现和临床开发
2. Advances in the structural biology, design and clinical development of Bcr-Abl kinase inhibitors for the treatment of chronic myeloid leukaemia [J] . Manley PW, Cowan-Jacob SW, Mestan J Biochimica et biophysica acta: BBA: International journal of biochemistry, biophysics and molecular biololgy. Proteins and Proteomics . 2005,第1a2期

机译：Bcr-Abl激酶抑制剂在治疗慢性粒细胞白血病中的结构生物学，设计及临床研究进展
3. The discovery and pre-clinical development of the first clinical stage EZH2-inhibitor, EPZ-6438 (E7438) [J] . Kuntz K., Keilhack H., Pollock R., European journal of cancer: official journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR) . 2014,第Suppla6期

机译：临床第一阶段EZH2抑制剂EPZ-6438（E7438）的发现和临床前开发
4. Development of Companion Diagnostics to Investigate the Action of a Dual MNK/ BCR-ABL Inhibitor [C] . Esther Ong, Jeffrey Hill, Kassoum Nacro, Molecular Medicine TRI-CON. . 2014

机译：伴随伴随探讨双MNK / BCR-ABL抑制剂的作用的疗效
5. Discovery, evolution, and clinical use of poly(adenosine-diphosphate-ribose)polymerase-1,2 (PARP-1,2) inhibitors. [D] . Jang, KyungMin. 2012

机译：聚（腺苷二磷酸核糖）聚合酶-1，2（PARP-1，2）抑制剂的发现，发展和临床应用。
6. Past present and future of Bcr-Abl inhibitors: from chemical development to clinical efficacy [O] . Federico Rossari, Filippo Minutolo, Enrico Orciuolo 2018

机译：Bcr-Abl抑制剂的过去现在和未来：从化学研发到临床疗效
7. Latest perspectives of orally bioavailable 2,4-diarylaminopyrimidine analogues (DAAPalogues) as anaplastic lymphoma kinase inhibitors: discovery and clinical developments [O] . Muhammad Latif, Zaman Ashraf, Sulman Basit, 2018

机译：口服生物可利用的2,4-二芳基吡啶吡啶氨酸类似物（Daapalogues）作为血糖性淋巴瘤激酶抑制剂的最新视角：发现和临床发展

The background, discovery and clinical development of BCR-ABL inhibitors

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