期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 29, 期 16, 页码 2016-2024出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2019.06.040
关键词
Cytochromes P450; Selective CYP inhibitor; Drug-drug interaction; Anti-cancer
资金
- Program for Innovative Research Team of the Ministry of Education and Program for Liaoning Innovative Research Team in University
Cytochromes P450 (CYPs) play an important role in the metabolism of endogenic and xenobiotic substances, especially drugs. In addition, many CYPs may serve as targets for disease treatment. However, due to the presence of a common heme, the hydrophobicity of the CYP binding cavity, and the high homology within the binding pocket, most CYP inhibitors lack selectivity, which often leads to drug-drug interactions. Therefore, it is meaningful to develop highly selective CYP inhibitors. In this review, we summarize some of the strategies that have been used to develop highly selective CYP inhibitors, such as the weakening of the heme-binding group interaction, reduction of molecular lipophilicity and introduction of small structural changes within compounds.
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