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利用FDA批准药物进行计算机辅助药物重新设计以预测耐药性T315I突变型和野生型BCR-ABL1的新型抑制剂:一项虚拟筛选和分子动力学研究。

In silico drug repurposing of FDA-approved drugs to predict new inhibitors for drug resistant T315I mutant and wild-type BCR-ABL1: A virtual screening and molecular dynamics study.

作者信息

Sohraby Farzin, Bagheri Milad, Aliyar Masoud, Aryapour Hassan

机构信息

Department of Biology, Faculty of Science, Golestan University, Gorgan, Iran.

Department of Biology, Faculty of Science, Golestan University, Gorgan, Iran.

出版信息

J Mol Graph Model. 2017 Jun;74:234-240. doi: 10.1016/j.jmgm.2017.04.005. Epub 2017 Apr 13.

DOI:10.1016/j.jmgm.2017.04.005
PMID:28458002
Abstract

The BCR-ABL fusion gene is one of the major causes of 95% of Chronic Myeloid Leukemia (CML). While, BCR-ABL protein is currently being used as a major target to treat CML. Although, current FDA-approved drugs such as; Imatinib and Nilotinib have stupendously improved the patients 5-year's survival rates, the drug resistance has dramatically reduced their effects. So, more accurate and effective alternative treatments are crucially needed. To address this issue, we screened the FDA-approved drugs by virtual screening and binding free energy calculations to identify new inhibitors for the wild-type and T315I gatekeeper mutant ABL1. It was invigorating to identify that chlorohexidine, paromomycin and deferoxamine could inhibit the wild-type ABL1, while chlorohexidine and ritonavir could inhibit the T315I mutant ABL1. The applications of these newly identified drugs are not just an effortless hypothesis in drug discovery. These drugs can be evaluated in phase 2 clinical trials after a simple kinase selectivity assay.

摘要

BCR-ABL融合基因是95%的慢性髓性白血病(CML)的主要病因之一。同时,BCR-ABL蛋白目前被用作治疗CML的主要靶点。尽管目前美国食品药品监督管理局(FDA)批准的药物,如伊马替尼和尼罗替尼,极大地提高了患者的5年生存率,但耐药性已显著降低了它们的疗效。因此,迫切需要更准确有效的替代治疗方法。为了解决这个问题,我们通过虚拟筛选和结合自由能计算对FDA批准的药物进行筛选,以鉴定针对野生型和T315I守门突变型ABL1的新型抑制剂。令人振奋的是,我们发现洗必泰、巴龙霉素和去铁胺可以抑制野生型ABL1,而洗必泰和利托那韦可以抑制T315I突变型ABL1。这些新鉴定药物的应用并非药物发现中的简单假设。经过简单的激酶选择性测定后,这些药物可在2期临床试验中进行评估。

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