摘要
CYP1B1酶(Cytochrome P4501B1,CYP1B1)是细胞色素P450酶(Cytochrome P450 enzyme,CYPs)的一个亚族,能参与多种内、外源性化合物的氧化/还原反应,在多种恶性肿瘤中高表达。CYP1B1酶逐渐成为抗肿瘤药物设计研发的热门靶点,许多学者以CYP1B1酶为靶标蛋白设计的抑制剂,表现出较好的活性和巨大的应用潜力,尤其是在克服肿瘤耐药性中具有重要意义。目前报道的CYP1B1抑制剂种类繁多,活性最佳的化合物是α-萘黄酮(ANF)。主要介绍了较为常见的几类CYP1B1抑制剂,简述了各类化合物的特点以及酶抑制效果,并对CYP1B1抑制剂的发展前景进行了展望。
Cytochrome P4501B1(CYP1B1)enzyme is a subfamily of Cytochrome P450 enzymes(CYPs),which can participate in the oxidation/reduction reaction of a variety of endogenous and exogenous compounds,and is highly expressed in a variety of malignant tumors.CYP1B1 enzyme has gradually becomed a popular target for the design and development of anti-tumor drugs.Many scholars have designed inhibitors targeting CYP1B1 enzyme,which show good activity and great application potential,especially in overcoming tumor drug resistance.A variety of CYP1B1 inhibitors have been reported,and the most active compound isα-naphthalene flavone(ANF).The review introduced several common classes of CYP1B1 inhibitors,briefly described the characteristics and enzyme inhibition effects of each compound,and look forward to the development prospects of CYP1B1 inhibitors.
作者
王志刚
费荣杰
WANG Zhi-gang;FEI Rong-jie(Nanjing Chemical Reagent Co.,Ltd.,Nanjing 210047,China)
出处
《化学试剂》
CAS
北大核心
2023年第2期69-74,共6页
Chemical Reagents
关键词
CYP1B1酶
抑制剂
靶点
抗肿瘤
α-萘黄酮
CYP1B1 enzyme
inhibitor
a target point
antitumor
alpha-naphthalene flavone
