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Recent researches for dual Aurora target inhibitors in antitumor field.
European Journal of Medicinal Chemistry ( IF 6.7 ) Pub Date : 2020-06-26 , DOI: 10.1016/j.ejmech.2020.112498
Maoyu Liu 1 , Xueming Ju 2 , Jing Zou 3 , Jianyou Shi 3 , Guiqing Jia 4
Affiliation  

Non-infectious and chronic diseases such as malignant tumors are now one of the main causes of human death. Its occurrence is a multi-factor, multi-step complex process with biological characteristics such as cell differentiation, abnormal proliferation, uncontrolled growth, and metastasis. It has been found that a variety of human malignant tumors are accompanied by over-expression and proliferation of Aurora kinase, which causes abnormalities in the mitotic process and is related to the instability of the genome that causes tumors. Therefore, the use of Aurora kinase inhibitors to target tumors is becoming a research hotspot. However, in cancer, because of the complexity of signal transduction system and the participation of different proteins and enzymes, the anticancer effect of selective single-target drugs is limited. After inhibiting one pathway, signal molecules can be conducted through other pathways, resulting in poor therapeutic effect of single-target drug treatment. Multi-target drugs can solve this problem very well. It can regulate the various links that cause disease at the same time without completely eliminating the relationship between the signal transmission systems, and it is not easy to cause drug resistance. Currently, studies have shown that Aurora dual-target inhibitors generated with the co-inhibition of Aurora and another target (such as CDK, PLK, JAK2, etc.) have better therapeutic effects on tumors. In this paper, we reviewed the studies of dual Aurora inhibitors that have been discovered in recent years.



中文翻译:

抗肿瘤领域中双重Aurora靶标抑制剂的最新研究。

非传染性和慢性疾病,例如恶性肿瘤,现已成为人类死亡的主要原因之一。它的发生是一个多因素,多步骤的复杂过程,具有生物学特征,例如细胞分化,异常增殖,生长失控和转移。已经发现,多种人类恶性肿瘤伴随有Aurora激酶的过表达和增殖,其引起有丝分裂过程的异常,并且与引起肿瘤的基因组的不稳定性有关。因此,使用Aurora激酶抑制剂靶向肿瘤已成为研究热点。然而,在癌症中,由于信号转导系统的复杂性以及不同蛋白质和酶的参与,选择性单靶标药物的抗癌作用受到限制。抑制一个途径后,信号分子可以通过其他途径传导,导致单靶标药物治疗的治疗效果差。多靶点药物可以很好地解决这个问题。它可以在不完全消除信号传输系统之间的关系的情况下,同时调节导致疾病的各种环节,而且不容易引起耐药性。目前,研究表明,与Aurora和另一种靶标(例如CDK,PLK,JAK2等)共同抑制产生的Aurora双靶标抑制剂对肿瘤具有更好的治疗效果。在本文中,我们回顾了近年来发现的双重Aurora抑制剂的研究。多靶点药物可以很好地解决这个问题。它可以在不完全消除信号传输系统之间的关系的情况下,同时调节导致疾病的各种环节,而且不容易引起耐药性。目前,研究表明,与Aurora和另一种靶标(例如CDK,PLK,JAK2等)共同抑制产生的Aurora双靶标抑制剂对肿瘤具有更好的治疗效果。在本文中,我们回顾了近年来发现的双重Aurora抑制剂的研究。多靶点药物可以很好地解决这个问题。它可以在不完全消除信号传输系统之间的关系的情况下,同时调节导致疾病的各种环节,而且不容易引起耐药性。目前,研究表明,与Aurora和另一种靶标(例如CDK,PLK,JAK2等)共同抑制产生的Aurora双靶标抑制剂对肿瘤具有更好的治疗效果。在本文中,我们回顾了近年来发现的双重Aurora抑制剂的研究。研究表明,与Aurora和另一种靶标(例如CDK,PLK,JAK2等)共同抑制产生的Aurora双靶标抑制剂对肿瘤具有更好的治疗效果。在本文中,我们回顾了近年来发现的双重Aurora抑制剂的研究。研究表明,与Aurora和另一种靶标(例如CDK,PLK,JAK2等)共同抑制产生的Aurora双靶标抑制剂对肿瘤具有更好的治疗效果。在本文中,我们回顾了近年来发现的双重Aurora抑制剂的研究。

更新日期:2020-07-18
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