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

Frontiers in Microbiology

Jingxiang Zhang¹  Lan Yan¹  Yan Wang¹  Quanzhen Lv¹  Yuanying Jiang²  Liping Li² 

[1] Center for New Drug Research, School of Pharmacy, Second Military Medical University, Shanghai, China;Department of Pharmacology, Tongji University School of Medicine, Shanghai, China;Shanghai Tenth People’s Hospital, Tongji University School of Medicine, Shanghai, China;

关键词: CYP51;    antifungal;    crystal structure;    azoles;    resistance;   

DOI  :  10.3389/fmicb.2019.00691

来源: DOAJ

【 摘 要 】

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 Candida albicans, Cryptococcus neoformans and Aspergillus fumigatus. 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.

【 授权许可】

Unknown