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药物发现的历史概述。

An historical overview of drug discovery.

作者信息

Pina Ana Sofia, Hussain Abid, Roque Ana Cecília A

机构信息

REQUIMTE, Department of Chemistry, Faculdade de Ciências e Tecnologia, Universidade Nova de Lisboa, Caparica, Portugal.

出版信息

Methods Mol Biol. 2009;572:3-12. doi: 10.1007/978-1-60761-244-5_1.

Abstract

Drug Discovery in modern times straddles three main periods. The first notable period can be traced to the nineteenth century where the basis of drug discovery relied on the serendipity of the medicinal chemists. The second period commenced around the early twentieth century when new drug structures were found, which contributed for a new era of antibiotics discovery. Based on these known structures, and with the development of powerful new techniques such as molecular modelling, combinatorial chemistry, and automated high-throughput screening, rapid advances occurred in drug discovery towards the end of the century. The period also was revolutionized by the emergence of recombinant DNA technology, where it became possible to develop potential drugs target candidates. With all the expansion of new technologies and the onset of the "Omics" revolution in the twenty-first century, the third period has kick-started with an increase in biopharmaceutical drugs approved by FDA/EMEA for therapeutic use.

摘要

现代药物发现跨越三个主要阶段。第一个显著阶段可追溯到19世纪,当时药物发现的基础依赖于药物化学家的偶然发现。第二个阶段始于20世纪初,当时发现了新的药物结构,这为抗生素发现的新时代做出了贡献。基于这些已知结构,并随着分子建模、组合化学和自动化高通量筛选等强大新技术的发展,到20世纪末药物发现取得了快速进展。重组DNA技术的出现也使这个时期发生了变革,开发潜在药物靶点候选物成为可能。随着新技术的不断扩展以及21世纪“组学”革命的到来,第三个阶段随着美国食品药品监督管理局(FDA)/欧洲药品管理局(EMEA)批准用于治疗的生物制药药物数量的增加而拉开序幕。

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