摘要
HER2阳性乳腺癌的特点是转移患者存活率低。耐药性和疾病复发的发展是与目前可用的HER2阳性乳腺癌治疗相关的主要问题。有两种主要的针对HER2阳性乳腺癌的治疗方法,单克隆抗体和酪氨酸激酶抑制剂,这两种疗法都有其优点和局限性。为了解决与现有疗法相关的限制,使用抗体和TKI作为组合疗法证明是更有效的。可以对酪氨酸激酶抑制剂进行各种化学修饰以开发具有增加的对HER2激酶选择性的新配体。许多酪氨酸激酶抑制剂处于治疗HER2阳性乳腺癌的临床试验的不同阶段。在当前的综述文章中,已经报道了各种HER2酪氨酸激酶抑制剂的最新进展。各种结构不同的支架与HER2受体结合并显示有效的抗癌活性。对支架的结构和药效要求进行了详细讨论,以发现治疗HER2阳性乳腺癌的有效候选药物
关键词: 乳腺癌,HER1 / HER2,酪氨酸激酶抑制剂,耐药性,单克隆抗体,曲妥珠单抗。
图形摘要
Current Cancer Drug Targets
Title:Recent Updates on the Therapeutic Potential of HER2 Tyrosine Kinase Inhibitors for the Treatment of Breast Cancer
Volume: 18 Issue: 4
关键词: 乳腺癌,HER1 / HER2,酪氨酸激酶抑制剂,耐药性,单克隆抗体,曲妥珠单抗。
摘要: HER2 positive breast cancer is characterized by the low survival rate in the metastatic patients. Development of resistance and disease-relapse are the major problems associated with the currently available therapies for HER2 positive breast cancer. There are two major targeted therapies for HER2 positive breast cancer viz. monoclonal antibodies and tyrosine-kinase inhibitors, and both of these therapies have their advantages and limitations. To address the limitations associated with the existing therapies, use of antibodies and TKIs as combination therapy proved to be more effective. Various chemical modifications can be performed on tyrosine-kinase inhibitors to develop novel ligands with increased selectivity for HER2 kinase. A number of tyrosine-kinase inhibitors are in various phases of clinical trials for the treatment of HER2 positive breast cancer. In the current review article, recent developments on various HER2 tyrosine-kinase inhibitors have been reported. Various structurally different scaffolds bind to the HER2 receptor and exhibit potent anti-cancer activities. The structural and pharmacophoric requirements of the scaffolds are discussed in detail so as to discover effective drug candidates for the treatment of HER2 positive breast cancer.
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Cite this article as:
Recent Updates on the Therapeutic Potential of HER2 Tyrosine Kinase Inhibitors for the Treatment of Breast Cancer, Current Cancer Drug Targets 2018; 18 (4) . https://dx.doi.org/10.2174/1568009617666170623122213
DOI https://dx.doi.org/10.2174/1568009617666170623122213 |
Print ISSN 1568-0096 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5576 |
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