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学术实验室对化学生物学工具的发现和开发的贡献。

Contributions of academic laboratories to the discovery and development of chemical biology tools.

机构信息

Department of Pharmaceutical Sciences, University of Pittsburgh Chemical Diversity Center (UP-CDC) , 3501 Terrace Street, Pittsburgh, Pennsylvania 15261, United States.

出版信息

J Med Chem. 2013 Sep 26;56(18):7161-76. doi: 10.1021/jm400132d. Epub 2013 May 31.

Abstract

The academic setting provides an environment that may foster success in the discovery of certain types of small molecule tools while proving less suitable in others. For example, small molecule probes for poorly understood systems, those that exploit a specific resident expertise, and those whose commercial return is not apparent are ideally suited to be pursued in a university setting. In this review, we highlight five projects that emanated from academic research groups and generated valuable tool compounds that have been used to interrogate biological phenomena: reactive oxygen species (ROS) sensors, GPR30 agonists and antagonists, selective CB2 agonists, Hsp70 modulators, and β-amyloid PET imaging agents. By taking advantage of the unique expertise resident in university settings and the ability to pursue novel projects that may have great scientific value but with limited or no immediate commercial value, probes from academic research groups continue to provide useful tools and generate a long-term resource for biomedical researchers.

摘要

学术环境提供了一个可能有助于发现某些类型小分子工具的环境,但在其他方面则不太适合。例如,对于理解不充分的系统、利用特定常驻专业知识的小分子探针,以及那些商业回报不明显的小分子探针,非常适合在大学环境中进行研究。在这篇综述中,我们重点介绍了五个源自学术研究小组的项目,这些项目生成了有价值的工具化合物,用于探究生物现象:活性氧(ROS)传感器、GPR30 激动剂和拮抗剂、选择性 CB2 激动剂、Hsp70 调节剂和β-淀粉样蛋白 PET 成像剂。通过利用大学环境中固有的独特专业知识和追求具有重大科学价值但商业价值有限或没有直接商业价值的新项目的能力,学术研究小组的探针继续提供有用的工具,并为生物医学研究人员提供长期资源。

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