| Literature DB >> 30504222 |
Rasmus D Wollenberg1, Manuel H Taft2, Sven Giese2, Claudia Thiel3, Zoltán Balázs1, Henriette Giese1, Dietmar J Manstein4,3, Teis E Sondergaard5.
Abstract
The cyanoacrylate compound phenamacril (also known as JS399-19) is a recently identified fungicide that exerts its antifungal effect on susceptible Fusarium species by inhibiting the ATPase activity of their myosin class I motor domains. Although much is known about the antifungal spectrum of phenamacril, the exact mechanism behind the phenamacril-mediated inhibition remains to be resolved. Here, we describe the characterization of the effect of phenamacril on purified myosin motor constructs from the model plant pathogen and phenamacril-susceptible species Fusarium graminearum, phenamacril-resistant Fusarium species, and the mycetozoan model organism Dictyostelium discoideum Our results show that phenamacril potently (IC50 ∼360 nm), reversibly, and noncompetitively inhibits ATP turnover, actin binding during ATP turnover, and motor activity of F. graminearum myosin-1. Phenamacril also inhibits the ATPase activity of Fusarium avenaceum myosin-1 but has little or no inhibitory effect on the motor activity of Fusarium solani myosin-1, human myosin-1c, and D. discoideum myosin isoforms 1B, 1E, and 2. Our findings indicate that phenamacril is a species-specific, noncompetitive inhibitor of class I myosin in susceptible Fusarium sp.Entities:
Keywords: ATPase; allosteric regulation; cytoskeleton; fungi; fungicide; inhibition mechanism; inhibitor; motor protein; myosin; phenamacril
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Year: 2018 PMID: 30504222 PMCID: PMC6349130 DOI: 10.1074/jbc.RA118.005408
Source DB: PubMed Journal: J Biol Chem ISSN: 0021-9258 Impact factor: 5.157