研究动态
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乳腺癌治疗中激酶的小分子抑制剂:最新进展、机遇与挑战。

Small-molecule inhibitors of kinases in breast cancer therapy: recent advances, opportunities, and challenges.

发表日期:2023
作者: Isha Bansal, Amit Kumar Pandey, Munindra Ruwali
来源: Frontiers in Pharmacology

摘要:

乳腺癌是全球妇女最常见的恶性肿瘤,尽管在癌症的检测、治疗和管理方面取得了显著进展,但仍然是导致女性恶性肿瘤相关死亡的主要原因。近年来,对乳腺癌的基础生物学的了解和新的诊断和治疗策略的创立在研究中得到了重新关注。在乳腺癌的发生和传播过程中,一群名为激酶的酶非常重要。小分子激酶抑制剂已成为乳腺癌治疗中一种有希望的药物类别,因为它们具有针对与癌症生长和进展相关的激酶的特异性靶向能力。阻断这些激酶及其激活的信号通路的靶向治疗措施已完全改变了乳腺癌的治疗方式。许多这些靶向治疗措施已经通过临床试验获得了乳腺癌治疗的批准,并显示出很高的疗效。CDK4/6 抑制剂,如帕博西尼、阿贝马西尼和里博西尼,EGFR 抑制剂,如吉非替尼和厄洛替尼,以及HER2靶向小分子激酶,如奈拉替尼和图卡替尼,是一些已经显示出治疗乳腺癌潜力的例子。然而,乳腺癌靶向药物的开发仍然存在困难,例如确定哪些患者亚群会从这些治疗中获益以及应对药物耐药问题。尽管存在这些困难,针对乳腺癌的激酶靶向治疗仍然具有很大的潜力。随着基因组学和蛋白质组学技术的进步,通过识别新的靶点和生物标志物,定制药物的开发将继续推动。版权所有 © 2023 Bansal, Pandey and Ruwali.
Breast cancer is the most common malignancy in women worldwide and despite significant advancements in detection, treatment, and management of cancer, it is still the leading cause of malignancy related deaths in women. Understanding the fundamental biology of breast cancer and creating fresh diagnostic and therapeutic strategies have gained renewed focus in recent studies. In the onset and spread of breast cancer, a group of enzymes known as kinases are extremely important. Small-molecule kinase inhibitors have become a promising class of medications for the treatment of breast cancer owing to their capacity to specifically target kinases involved in the growth and progression of cancer. The creation of targeted treatments that block these kinases and the signalling pathways that they activate has completely changed how breast cancer is treated. Many of these targeted treatments have been approved for the treatment of breast cancer as clinical trials have demonstrated their great efficacy. CDK4/6 inhibitors, like palbociclib, abemaciclib, and ribociclib, EGFR inhibitors such as gefitinib and erlotinib and HER2-targeting small-molecule kinases like neratinib and tucatinib are some examples that have shown potential in treating breast cancer. Yet, there are still difficulties in the development of targeted medicines for breast cancer, such as figuring out which patient subgroups may benefit from these therapies and dealing with drug resistance problems. Notwithstanding these difficulties, kinase-targeted treatments for breast cancer still have a lot of potential. The development of tailored medicines will continue to be fuelled by the identification of novel targets and biomarkers for breast cancer as a result of advancements in genomic and proteomic technology.Copyright © 2023 Bansal, Pandey and Ruwali.