Jo Ala, Jung Jinjoo, Kim Eunha, Park Seung Bum
Department of Chemistry, Seoul National University, Seoul, 08826, Korea.
Chem Commun (Camb). 2016 Jun 14;52(47):7433-45. doi: 10.1039/c6cc02587k. Epub 2016 May 11.
Phenotypic screening has emerged as a promising approach to discover novel first-in-class therapeutic agents. Rapid advances in phenotypic screening systems facilitate a high-throughput unbiased evaluation of compound libraries. However, limited sets of phenotypic changes are utilized in high-content screening, which require extensive genetic engineering. Therefore, it is critical to develop new chemical probes that can reflect phenotypic changes in any type of cells, especially primary cells, tissues, and organisms. Herein, we introduce our continuous efforts in the development of fluorescent bioprobes and their application to phenotypic screening. In addition, we emphasize the importance of the phenotype-based approach in conjunction with target identification at an early stage of research to accelerate the discovery of therapeutics with new modes of action.
表型筛选已成为发现新型首创治疗药物的一种有前景的方法。表型筛选系统的快速发展有助于对化合物库进行高通量无偏评估。然而，高内涵筛选中使用的表型变化集有限，这需要广泛的基因工程。因此，开发能够反映任何类型细胞，尤其是原代细胞、组织和生物体中表型变化的新型化学探针至关重要。在此，我们介绍我们在荧光生物探针开发及其在表型筛选中的应用方面的持续努力。此外，我们强调基于表型的方法与早期研究中的靶点识别相结合对于加速发现具有新作用模式的治疗药物的重要性。
