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本文引用的文献

1
Cancer Drug Development Using Drosophila as an in vivo Tool: From Bedside to Bench and Back.利用果蝇作为体内工具进行癌症药物开发:从床边到实验台再回到床边。
Trends Pharmacol Sci. 2016 Sep;37(9):789-806. doi: 10.1016/j.tips.2016.05.010. Epub 2016 Jun 10.
2
GEMMs as preclinical models for testing pancreatic cancer therapies.基因工程小鼠模型作为测试胰腺癌治疗方法的临床前模型。
Dis Model Mech. 2015 Oct 1;8(10):1185-200. doi: 10.1242/dmm.021055.
3
Yeast as a system for modeling mitochondrial disease mechanisms and discovering therapies.酵母作为一种用于模拟线粒体疾病机制和发现治疗方法的系统。
Dis Model Mech. 2015 Jun;8(6):509-26. doi: 10.1242/dmm.020438.
4
The zebrafish as a tool to identify novel therapies for human cardiovascular disease.斑马鱼作为一种用于识别人类心血管疾病新疗法的工具。
Dis Model Mech. 2014 Jul;7(7):763-7. doi: 10.1242/dmm.016170.
5
Hooking the big one: the potential of zebrafish xenotransplantation to reform cancer drug screening in the genomic era.钓大鱼:斑马鱼异种移植在基因组时代改革癌症药物筛选的潜力。
Dis Model Mech. 2014 Jul;7(7):745-54. doi: 10.1242/dmm.015784.
6
Zebrafish models in translational research: tipping the scales toward advancements in human health.斑马鱼模型在转化研究中的应用:助力人类健康取得进展
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7
Finding function in novel targets: C. elegans as a model organism.在新靶点中寻找功能:以秀丽隐杆线虫作为模式生物
Nat Rev Drug Discov. 2006 May;5(5):387-98. doi: 10.1038/nrd2031.
8
Yeast as a model system for anticancer drug discovery.酵母作为抗癌药物发现的模型系统。
Nat Rev Cancer. 2004 Jun;4(6):481-92. doi: 10.1038/nrc1372.

使用模型系统进行药物筛选:一些基础要点。

Drug screening using model systems: some basics.

作者信息

Cagan Ross

机构信息

Icahn School of Medicine at Mount Sinai, Annenberg 25-40, Campus Box 1020, 1468 Madison Avenue, New York, NY 10029, USA

出版信息

Dis Model Mech. 2016 Nov 1;9(11):1241-1244. doi: 10.1242/dmm.028159.

DOI:10.1242/dmm.028159
PMID:27821602
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5117237/
Abstract

An increasing number of laboratories that focus on model systems are considering drug screening. Executing a drug screen is complicated enough. But the path for moving initial hits towards the clinic requires a different knowledge base and even a different mindset. In this Editorial I discuss the importance of doing some homework before you start screening. 'Lead hits', 'patentable chemical space' and 'druggability' are all concepts worth exploring when deciding which screening path to take. I discuss some of the lessons I learned that may be useful as you navigate the screening matrix.

摘要

越来越多专注于模型系统的实验室正在考虑进行药物筛选。执行一次药物筛选已经够复杂的了。但是将最初筛选出的活性物质推进到临床阶段需要不同的知识基础,甚至是不同的思维方式。在这篇社论中,我讨论了在开始筛选之前做好一些准备工作的重要性。在决定采取哪种筛选途径时,“先导活性物质”“可专利的化学空间”和“成药性”都是值得探索的概念。我将讨论一些我学到的经验教训,这些经验教训在您梳理筛选矩阵时可能会有所帮助。