The Current State of Peptide Drug Discovery: Back to the Future?
The Current State of Peptide Drug Discovery: Back to the Future?
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DOI：
10.1021/acs.jmedchem.7b00318
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发表时间：
2018-02-22
影响因子：
7.3
通讯作者：
Nuss, John M.
中科院分区：
文献类型：
--
作者：
Henninot, Antoine;Collins, James C.;Nuss, John M.
在过去的十年中，肽药物发现经历了兴趣和科学动力的复兴，因为制药行业已经认识到肽治疗剂在解决未满足的医疗需求方面可以发挥的作用，以及这类化合物如何成为小分子和生物治疗剂的优秀补充甚至优选替代品。在这个角度来看，我们给出了一个简洁的描述，在肽药物发现的整体方式的最新进展，突出使技术进步影响几乎每一个方面的这一领域：从铅发现，合成和优化，肽药物输送。重点是描述研究工作，以克服肽类药物的固有弱点，特别是其不良的药代动力学特性，以及如何这些努力一直是至关重要的发现，设计和随后的发展新的治疗方法。
Over the past decade, peptide drug discovery has experienced a revival of interest and scientific momentum, as the pharmaceutical industry has come to appreciate the role that peptide therapeutics can play in addressing unmet medical needs and how this class of compounds can be an excellent complement or even preferable alternative to small molecule and biological therapeutics. In this Perspective, we give a concise description of the recent progress in peptide drug discovery in a holistic manner, highlighting enabling technological advances affecting nearly every aspect of this field: from lead discovery, to synthesis and optimization, to peptide drug delivery. An emphasis is placed on describing research efforts to overcome the inherent weaknesses of peptide drugs, in particular their poor pharmacokinetic properties, and how these efforts have been critical to the discovery, design, and subsequent development of novel therapeutics.