Chun Young-Jin, Kim Sanghee
College of Pharmacy, Chungang University, 221 Huksuk, Dongjak, Seoul 156-756, Korea.
Med Res Rev. 2003 Nov;23(6):657-68. doi: 10.1002/med.10050.
Human cytochrome P450 (CYP)1B1 is a major enzyme for carcinogenic estrogen metabolism and involved in the metabolic activation of procarcinogens of the polycyclic aromatic hydrocarbons (PAHs). CYP1B1 is known to be expressed at a high frequency in various human cancers, but not in normal tissues. It also plays an important role in the metabolism of various anti-cancer drugs. These findings suggest inhibition of CYP1B1 as a new oncological therapeutic strategy. Several natural and synthetic compounds have been studied in an effort to find the isoform-specific inhibitors of the CYP1 subfamily. A survey of the inhibitors of CYP1B1 and other related inhibitors of the CYP1 subfamily is provided in this review.
人类细胞色素P450（CYP）1B1是致癌性雌激素代谢的主要酶，参与多环芳烃（PAHs）前致癌物的代谢活化。已知CYP1B1在各种人类癌症中高频率表达，但在正常组织中不表达。它在各种抗癌药物的代谢中也起着重要作用。这些发现表明抑制CYP1B1作为一种新的肿瘤治疗策略。为了找到CYP1亚家族的同工型特异性抑制剂，人们研究了几种天然和合成化合物。本综述提供了对CYP1B1抑制剂及CYP1亚家族其他相关抑制剂的调查。
