ATP 柠檬酸裂解酶抑制剂在癌症及相关疾病治疗中的最新进展。
Recent advance of ATP citrate lyase inhibitors for the treatment of cancer and related diseases.
机构信息
Hubei Key Laboratory of Natural Products Research and Development, Key Laboratory of Functional Yeast, China National Light Industry, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China.
Hubei Key Laboratory of Natural Products Research and Development, Key Laboratory of Functional Yeast, China National Light Industry, College of Biological and Pharmaceutical Sciences, China Three Gorges University, Yichang 443002, China; CAS Key Laboratory of Synthetic Biology, CAS Center for Excellence in Molecular Plant Sciences, Institute of Plant Physiology and Ecology, Chinese Academy of Sciences, Shanghai 200032, China.
出版信息
Bioorg Chem. 2024 Jan;142:106933. doi: 10.1016/j.bioorg.2023.106933. Epub 2023 Oct 21.
ATP citrate lyase (ACLY), a strategic metabolic enzyme that catalyzes the glycolytic to lipidic metabolism, has gained increasing attention as an attractive therapeutic target for hyperlipidemia, cancers and other human diseases. Despite of continual research efforts, targeting ACLY has been very challenging. In this field, most reported ACLY inhibitors are "substrate-like" analogues, which occupied with the same active pockets. Besides, some ACLY inhibitors have been disclosed through biochemical screening or high throughput virtual screening. In this review, we briefly summarized the cancer-related functions and the recent advance of ACLY inhibitors with a particular focus on the SAR studies and their modes of action. We hope to provide a timely and updated overview of ACLY and the discovery of new ACLY inhibitors.
三磷酸腺苷柠檬酸裂解酶（ACLY）是一种具有战略意义的代谢酶，能够催化糖酵解向脂质代谢的转化，作为治疗高脂血症、癌症和其他人类疾病的有吸引力的治疗靶点，已受到越来越多的关注。尽管进行了持续的研究，但靶向 ACLY 一直具有很大的挑战性。在该领域中，大多数报道的 ACLY 抑制剂是“类似底物”的类似物，占据相同的活性口袋。此外，一些 ACLY 抑制剂是通过生化筛选或高通量虚拟筛选发现的。在这篇综述中，我们简要总结了 ACLY 与癌症相关的功能及其抑制剂的最新进展，特别关注了 SAR 研究及其作用模式。我们希望为 ACLY 及其新型 ACLY 抑制剂的发现提供一个及时和更新的概述。
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