Metal-dependent enzymes (i.e., metalloenzymes) make up a large fraction of all enzymes and are critically important in a wide range of biological processes, including DNA modification, protein homeostasis, antibiotic resistance, and many others. Consequently, metalloenzymes represent a vast and largely untapped space for drug development. The discovery of effective therapeutics that target metalloenzymes lies squarely at the interface of bioinorganic and medicinal chemistry and requires expertise, methods, and strategies from both fields to mount an effective campaign. In this Account, our research program that brings together the principles and methods of bioinorganic and medicinal chemistry are described, in an effort to bridge the gap between these fields and address an important class of medicinal targets.

中文翻译：

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针对基于金属酶的基于片段的药物发现的生物无机方法。

金属依赖性酶（即金属酶）占所有酶的很大一部分，并且在包括DNA修饰，蛋白质稳态，抗生素抗性等许多生物过程中至关重要。因此，金属酶代表了巨大且尚未开发的药物开发空间。针对金属酶的有效疗法的发现正好位于生物无机化学和药物化学的交界处，并且需要来自两个领域的专业知识，方法和策略来开展有效的运动。在此报告中，我们描述了将生物无机化学和药物化学的原理和方法结合在一起的研究计划，以弥合这些领域之间的差距并解决重要的医学目标类别。