Usmani Khawja A, Tang Jun
North Carolina State University, Raleigh, North Carolina, USA.
Curr Protoc Toxicol. 2004 Jun;Chapter 4:Unit4.13. doi: 10.1002/0471140856.tx0413s20.
This unit describes methods for measuring CYP3A4 activity using testosterone as a specific substrate, and for measuring CYP3A4 inhibition using ketoconazole as a selective inhibitor of testosterone oxidation. CYP3A4 is one of the most important and most abundant drug-metabolizing CYP isoforms in human liver microsomes (∼40% of total CYP), and it has the broadest substrate specificity. It is important to determine whether CYP3A4 is involved in its metabolism.
本单元介绍了以睾酮作为特异性底物来测量CYP3A4活性，以及以酮康唑作为睾酮氧化的选择性抑制剂来测量CYP3A4抑制作用的方法。CYP3A4是人类肝微粒体中最重要且含量最丰富的药物代谢CYP同工型之一（约占总CYP的40%），并且具有最广泛的底物特异性。确定CYP3A4是否参与其代谢很重要。
