History of the development of antifungal azoles: A review on structures, SAR, and mechanism of action

M Shafiei, L Peyton, M Hashemzadeh, A Foroumadi - Bioorganic chemistry, 2020 - Elsevier
With the increasing risk of invasive and life threating fungal infections, there is now a great
concern regarding the lower discovery rate of antifungal drugs in comparison to …

The fungal CYP51s: their functions, structures, related drug resistance, and inhibitors

J Zhang, L Li, Q Lv, L Yan, Y Wang… - Frontiers in microbiology, 2019 - frontiersin.org
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 …

Exploring the diverse landscape of biaryl-containing peptides generated by cytochrome P450 macrocyclases

H Nam, JS An, J Lee, Y Yun, H Lee… - Journal of the …, 2023 - ACS Publications
Cytochrome P450 enzymes (P450s) catalyze diverse oxidative cross-coupling reactions
between aromatic substrates in the natural product biosynthesis. Specifically, P450s install …

Structural analyses of Candida albicans sterol 14α-demethylase complexed with azole drugs address the molecular basis of azole-mediated inhibition of fungal sterol …

TY Hargrove, L Friggeri, Z Wawrzak, A Qi… - Journal of Biological …, 2017 - ASBMB
With some advances in modern medicine (such as cancer chemotherapy, broad exposure to
antibiotics, and immunosuppression), the incidence of opportunistic fungal pathogens such …

Architecture of a single membrane spanning cytochrome P450 suggests constraints that orient the catalytic domain relative to a bilayer

BC Monk, TM Tomasiak, MV Keniya… - Proceedings of the …, 2014 - National Acad Sciences
Bitopic integral membrane proteins with a single transmembrane helix play diverse roles in
catalysis, cell signaling, and morphogenesis. Complete monospanning protein structures …

Fungal cytochrome P450 sterol 14α-demethylase (CYP51) and azole resistance in plant and human pathogens

R Becher, SGR Wirsel - Applied microbiology and biotechnology, 2012 - Springer
Azoles have been applied widely to combat pathogenic fungi in medicine and agriculture
and, consequently, loss of efficacy has occurred in populations of some species. Often, but …

Structural insights into binding of the antifungal drug fluconazole to Saccharomyces cerevisiae lanosterol 14α-demethylase

AA Sagatova, MV Keniya, RK Wilson… - Antimicrobial agents …, 2015 - Am Soc Microbiol
Infections by fungal pathogens such as Candida albicans and Aspergillus fumigatus and
their resistance to triazole drugs are major concerns. Fungal lanosterol 14α-demethylase …

Crystal structures of full-length lanosterol 14α-demethylases of prominent fungal pathogens Candida albicans and Candida glabrata provide tools for antifungal …

MV Keniya, M Sabherwal, RK Wilson… - Antimicrobial agents …, 2018 - Am Soc Microbiol
Targeting lanosterol 14α-demethylase (LDM) with azole drugs provides prophylaxis and
treatments for superficial and disseminated fungal infections, but cure rates are not optimal …

Structure-functional characterization of cytochrome P450 sterol 14α-demethylase (CYP51B) from Aspergillus fumigatus and molecular basis for the development of …

TY Hargrove, Z Wawrzak, DC Lamb… - Journal of Biological …, 2015 - ASBMB
Aspergillus fumigatus is the opportunistic fungal pathogen that predominantly affects the
immunocompromised population and causes 600,000 deaths/year. The cytochrome P450 …

Highlighting membrane protein structure and function: A celebration of the Protein Data Bank

F Li, PF Egea, AJ Vecchio, I Asial, M Gupta… - Journal of Biological …, 2021 - ASBMB
Biological membranes define the boundaries of cells and compartmentalize the chemical
and physical processes required for life. Many biological processes are carried out by …