Department of Chemistry and Biochemistry , University of California, San Diego , La Jolla , California 92093 , United States.
Chem Rev. 2019 Jan 23;119(2):1323-1455. doi: 10.1021/acs.chemrev.8b00201. Epub 2018 Sep 7.
Metalloenzymes are central to a wide range of essential biological activities, including nucleic acid modification, protein degradation, and many others. The role of metalloenzymes in these processes also makes them central for the progression of many diseases and, as such, makes metalloenzymes attractive targets for therapeutic intervention. Increasing awareness of the role metalloenzymes play in disease and their importance as a class of targets has amplified interest in the development of new strategies to develop inhibitors and ultimately useful drugs. In this Review, we provide a broad overview of several drug discovery efforts focused on metalloenzymes and attempt to map out the current landscape of high-value metalloenzyme targets.
金属酶在广泛的重要生物活性中起着核心作用，包括核酸修饰、蛋白质降解和许多其他功能。金属酶在这些过程中的作用也使它们成为许多疾病进展的核心，因此，金属酶成为治疗干预的有吸引力的靶点。人们对金属酶在疾病中的作用及其作为一类靶点的重要性的认识不断提高，这也促使人们加大了开发新策略以开发抑制剂并最终开发出有用药物的兴趣。在这篇综述中，我们提供了对几种专注于金属酶的药物发现努力的广泛概述，并试图描绘出高价值金属酶靶点的当前格局。
