Roles for Structural Biology in the Discovery of Drugs and Agrochemicals Targeting Sterol 14α-Demethylases
Antifungal drugs and antifungal agrochemicals have significant limitations. These include several unintended consequences of their use including the growing importance of intrinsic and acquired resistance. These problems underpin an increasingly urgent need to improve the existing classes of antifun...
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Online Access: | https://www.mdpi.com/2309-608X/7/2/67 |
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doaj-3d852f5be8e64d26ad70e183677d9ce92021-01-21T00:00:54ZengMDPI AGJournal of Fungi2309-608X2021-01-017676710.3390/jof7020067Roles for Structural Biology in the Discovery of Drugs and Agrochemicals Targeting Sterol 14α-DemethylasesBrian C. Monk0Mikhail V. Keniya1Department of Oral Sciences, Sir John Walsh Research Institute, University of Otago, Dunedin 9016, New ZealandDepartment of Oral Sciences, Sir John Walsh Research Institute, University of Otago, Dunedin 9016, New ZealandAntifungal drugs and antifungal agrochemicals have significant limitations. These include several unintended consequences of their use including the growing importance of intrinsic and acquired resistance. These problems underpin an increasingly urgent need to improve the existing classes of antifungals and to discover novel antifungals. Structural insights into drug targets and their complexes with both substrates and inhibitory ligands increase opportunity for the discovery of more effective antifungals. Implementation of this promise, which requires multiple skill sets, is beginning to yield candidates from discovery programs that could more quickly find their place in the clinic. This review will describe how structural biology is providing information for the improvement and discovery of inhibitors targeting the essential fungal enzyme sterol 14α-demethylase.https://www.mdpi.com/2309-608X/7/2/67antifungal drug discoveryCYP51sterol 14α-demethylaseazole drugsazole agrochemicalsstructure-directed drug design |
collection |
DOAJ |
language |
English |
format |
Article |
sources |
DOAJ |
author |
Brian C. Monk Mikhail V. Keniya |
spellingShingle |
Brian C. Monk Mikhail V. Keniya Roles for Structural Biology in the Discovery of Drugs and Agrochemicals Targeting Sterol 14α-Demethylases Journal of Fungi antifungal drug discovery CYP51 sterol 14α-demethylase azole drugs azole agrochemicals structure-directed drug design |
author_facet |
Brian C. Monk Mikhail V. Keniya |
author_sort |
Brian C. Monk |
title |
Roles for Structural Biology in the Discovery of Drugs and Agrochemicals Targeting Sterol 14α-Demethylases |
title_short |
Roles for Structural Biology in the Discovery of Drugs and Agrochemicals Targeting Sterol 14α-Demethylases |
title_full |
Roles for Structural Biology in the Discovery of Drugs and Agrochemicals Targeting Sterol 14α-Demethylases |
title_fullStr |
Roles for Structural Biology in the Discovery of Drugs and Agrochemicals Targeting Sterol 14α-Demethylases |
title_full_unstemmed |
Roles for Structural Biology in the Discovery of Drugs and Agrochemicals Targeting Sterol 14α-Demethylases |
title_sort |
roles for structural biology in the discovery of drugs and agrochemicals targeting sterol 14α-demethylases |
publisher |
MDPI AG |
series |
Journal of Fungi |
issn |
2309-608X |
publishDate |
2021-01-01 |
description |
Antifungal drugs and antifungal agrochemicals have significant limitations. These include several unintended consequences of their use including the growing importance of intrinsic and acquired resistance. These problems underpin an increasingly urgent need to improve the existing classes of antifungals and to discover novel antifungals. Structural insights into drug targets and their complexes with both substrates and inhibitory ligands increase opportunity for the discovery of more effective antifungals. Implementation of this promise, which requires multiple skill sets, is beginning to yield candidates from discovery programs that could more quickly find their place in the clinic. This review will describe how structural biology is providing information for the improvement and discovery of inhibitors targeting the essential fungal enzyme sterol 14α-demethylase. |
topic |
antifungal drug discovery CYP51 sterol 14α-demethylase azole drugs azole agrochemicals structure-directed drug design |
url |
https://www.mdpi.com/2309-608X/7/2/67 |
work_keys_str_mv |
AT briancmonk rolesforstructuralbiologyinthediscoveryofdrugsandagrochemicalstargetingsterol14ademethylases AT mikhailvkeniya rolesforstructuralbiologyinthediscoveryofdrugsandagrochemicalstargetingsterol14ademethylases |
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