In humans, more than three hundred diverse enzymes that require zinc as an essential cofactor have been identified. These zinc enzymes have demonstrated different and important physiological functions and some of them have been considered as valuable therapeutic targets for drug discovery. Indeed, many drugs targeting a few zinc enzymes have been marketed to treat a variety of diseases. This review discusses drug discovery and drug development based on a dozen of zinc enzymes, including their biological functions and pathogenic roles, their best in class inhibitors (and clinical trial data when available), coordination and binding modes of representative inhibitors, and their implications for further drug design. The opportunities and challenges in developing zinc enzyme inhibitors for the treatment of human disorders are highlighted, too.

在人类中，已鉴定出 300 多种需要锌作为必需辅助因子的酶。这些锌酶已表现出不同且重要的生理功能，其中一些已被认​​为是药物发现的有价值的治疗靶点。事实上，许多针对一些锌酶的药物已经上市用于治疗多种疾病。本综述讨论了基于十几种锌酶的药物发现和药物开发，包括它们的生物学功能和致病作用、同类最佳抑制剂（以及可用的临床试验数据）、代表性抑制剂的协调和结合模式，以及它们对进一步的药物设计。还强调了开发用于治疗人类疾病的锌酶抑制剂的机遇和挑战。