真菌细胞色素P451：其功能、结构、相关耐药性及抑制剂

The Fungal CYP51s: Their Functions, Structures, Related Drug Resistance, and Inhibitors.

作者信息

Zhang Jingxiang, Li Liping, Lv Quanzhen, Yan Lan, Wang Yan, Jiang Yuanying

机构信息

Center for New Drug Research, School of Pharmacy, Second Military Medical University, Shanghai, China.

Shanghai Tenth People's Hospital, Tongji University School of Medicine, Shanghai, China.

出版信息

Front Microbiol. 2019 Apr 24;10:691. doi: 10.3389/fmicb.2019.00691. eCollection 2019.

CYP51 (Erg11) belongs to the cytochrome P450 monooxygenase (CYP) superfamily and mediates a crucial step of the synthesis of ergosterol, which is a fungal-specific sterol. It is also the target of azole drugs in clinical practice. In recent years, researches on fungal CYP51 have stepped into a new stage attributing to the discovery of crystal structures of the homologs in and . This review summarizes the functions, structures of fungal CYP51 proteins, and the inhibitors targeting these homologs. In particular, several drug-resistant mechanisms associated with the fungal CYP51s are introduced. The sequences and crystal structures of CYP51 proteins in different fungal species are also compared. These will provide new insights for the advancement of research on antifungal agents.