Department of Pharmaceutical Sciences, Center for Biomolecular Sciences, University of Illinois at Chicago, Chicago, Illinois.
Department of Chemistry, University of Illinois at Chicago, Chicago, Illinois.
Transl Res. 2020 Jun;220:114-121. doi: 10.1016/j.trsl.2020.02.001. Epub 2020 Feb 6.
This perspective provides an overview of the evolution of antibiotic discovery from a largely phenotypic-based effort, through an intensive structure-based design focus, to a more holistic approach today. The current focus on antibiotic development incorporates assay and discovery conditions that replicate the host environment as much as feasible. They also incorporate several strategies, including target identification and validation within the whole cell environment, a variety of target deconvolution methods, and continued refinement of structure-based design approaches.
本文从一个主要基于表型的努力的角度，概述了抗生素发现的演变过程，通过密集的基于结构的设计重点，到今天的更全面的方法。目前对抗生素开发的重点包括尽可能复制宿主环境的测定和发现条件。它们还包括几种策略，包括在整个细胞环境中进行目标鉴定和验证、各种目标分解方法，以及继续改进基于结构的设计方法。
