Cytochrome P450 Enzymes as Drug Targets in Human Disease

被引:16
作者
Guengerich, F. Peter [1 ,2 ]
机构
[1] Vanderbilt Univ, Sch Med, Dept Biochem, Nashville, TN 37232 USA
[2] Vanderbilt Univ, Sch Med, 638B Robinson Res Bldg, 2200 Pierce Ave, Nashville, TN 37232 USA
基金
美国国家卫生研究院;
关键词
LANOSTEROL 14-ALPHA-DEMETHYLASE CYP51; SYNTHASE CYP11B2 INHIBITORS; CUSHINGS-SYNDROME; DISCOVERY; ANTIFUNGAL; METABOLISM; MECHANISM; SCH-56592; KNOCKOUT; MOLECULE;
D O I
10.1124/dmd.123.001431
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Although the mention of cytochrome P450 (P450) inhibition usually brings to mind unwanted variability in pharmacokinetics, in several cases P450s are good targets for inhibition. These P450s are essential, but in certain disease states, it is desirable to reduce the concentrations of their products. Most of the attention to date has been with human P450s 5A1, 11A1, 11B1, 11B2, 17A1, 19A1, and 51A1. In some of those cases, there are multiple drugs in use, e.g., exemestane, letrozole, and anastrozole with P450 19A1, the steroid aromatase target in breast cancer. There are also several targets that are less developed, e.g., P450s 2A6, 8B1, 4A11, 24A1, 26A1, and 26B1.
引用
收藏
页码:493 / 497
页数:5
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