摘要
CYP4Z1活性和抑制实验是围绕能够转化成易于监测产物的探针底物来进行的,探针底物类型主要包括饱和脂肪酸类(月桂酸和肉豆蔻酸)、不饱和脂肪酸类(花生四烯酸和二十碳二烯酸)以及荧光素衍生物等。其中,利用荧光素衍生物来进行的生物发光测定法,具有灵敏度高、方法简捷、测定快速的优点。近年来发现的CYP4Z1抑制剂主要有HET0016、1-苯并咪唑、ABT类似物以及计算机模拟设计药物Compound 9等,借助计算机模拟设计药物的手段来开发CYP4Z1抑制剂的方法更具高选择性和高特异性。对近年来发现的CYP4Z1的探针底物和抑制剂进行了总结和综述,以期为乳腺癌和其他特定类型癌症的治疗提供相关基础。
CYP4Z1 activity and inhibition experiments were performed around probe substrates that can be converted into easily monitored products. The types of probe substrates mainly include saturated fatty acids(lauric acid and myristic acid), unsaturated fatty acids(arachidonic acid and eicosadienoic acid) and fluorescein derivatives. Among them, the bioluminescence assay using fluorescein derivatives has the advantages of high sensitivity, simple method,and rapid determination.CYP4Z1 inhibitors discovered in recent years mainly include HET0016, 1-benzimidazole,ABT analogs, and computer simulation design drugs Compound 9, etc. The method of developing CYP4Z1 inhibitors by means of computer simulation design drugs is more highly selective and high specificity. In this paper, the probe substrates and inhibitors of CYP4Z1 discovered in recent years were summarized, which could provide a relevant basis for the treatment of breast cancer and other specific types of cancer.
作者
张雪
顾凌悦
ZHANG Xue;GULing-yue(School of Pharmaceutical Science and Technology,Tianjin University,Tianjin 300072,China)
出处
《当代化工》
CAS
2022年第2期431-435,440,共6页
Contemporary Chemical Industry
基金
天津市自然科学基金(项目编号:17JCZDJC32000)。
