The mechanism of resistance to sterol 14? demethylation inhibitors in a mutant (Erg 40) ofUstilago maydis

Butters, J. A.; Zhou, Meng; Hollomon, D. W.

doi:10.1002/(sici)1526-4998(200003)56:3<257::aid-ps131>3.0.co;2-b

Cited by 9 publications

(2 citation statements)

References 25 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…They have outstanding broadspectrum inhibitory effects. Unfortunately, owing to continuous and intensive applications of DMIs, serious resistance has emerged among some phytopathogenic fungi, for instance, Ustilago maydis, 7 Phakopsora pachyrhizi, 8 Blumeriella jaapii, 9 Fusarium fujikuroi, 10 Ustilaginoidea virens, 11 and Pencillium digitatum. 12,13 Thus, in recent years, the design, synthesis, and evaluation of novel CYP51 inhibitors have become an active realm of researches.…”

Section: Introductionmentioning

confidence: 99%

“…They have outstanding broad-spectrum inhibitory effects. Unfortunately, owing to continuous and intensive applications of DMIs, serious resistance has emerged among some phytopathogenic fungi, for instance, Ustilago maydis, Phakopsora pachyrhizi, Blumeriella jaapii, Fusarium fujikuroi, Ustilaginoidea virens, and Pencillium digitatum. , Thus, in recent years, the design, synthesis, and evaluation of novel CYP51 inhibitors have become an active realm of researches. CYP51 inhibitors with new structures and outstanding performances are constantly discovered. − Literature surveys show that this is the first time that pyrido[4,3- d ]pyrimidine analogs as potential CYP51 inhibitors have been reported.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Novel Pyrido[4,3-d]pyrimidine Derivatives as Potential Sterol 14α-Demethylase Inhibitors: Design, Synthesis, Inhibitory Activity, and Molecular Modeling

Yan,

Xie,

Jiang

et al. 2024

J. Agric. Food Chem.

View full text Add to dashboard Cite

pyrimidine analogs were designed, synthesized, and characterized. The crystal structures for compounds 2c and 4f were measured by means of X-ray diffraction of single crystals. The bioassay results showed that most target compounds exhibited good fungicidal activities against Pyricularia oryzae, Rhizoctonia cerealis, Sclerotinia sclerotiorum, Botrytis cinerea, and Penicillium italicum at 16 μg/mL. Compounds 2l, 2m, 4f, and 4g possessed better fungicidal activities than the commercial fungicide epoxiconazole against B. cinerea. Their half maximal effective concentration (EC 50 ) values were 0.191, 0.487, 0.369, 0.586, and 0.670 μg/mL, respectively. Furthermore, the inhibitory activities of the bioactive compounds were determined against sterol 14α-demethylase (CYP51). The results displayed that they had prominent activities. Compounds 2l, 2m, 4f, and 4g also showed better inhibitory activities than epoxiconazole against CYP51. Their half maximal inhibitory concentration (IC 50 ) values were 0.219, 0.602, 0.422, 0.726, and 0.802 μg/mL, respectively. The results of molecular dynamics (MD) simulations exhibited that compounds 2l and 4f possessed a stronger affinity to CYP51 than epoxiconazole.

show abstract

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Novel Pyrido[4,3-d]pyrimidine Derivatives as Potential Sterol 14α-Demethylase Inhibitors: Design, Synthesis, Inhibitory Activity, and Molecular Modeling

Yan,

Xie,

Jiang

et al. 2024

J. Agric. Food Chem.

View full text Add to dashboard Cite

show abstract

Triazole Resistance in Aspergillus Species: An Emerging Problem

Garcia-Rubio

Cuenca‐Estrella

Mellado

2017

Drugs

137

134

View full text Add to dashboard Cite

Aspergillus species are ubiquitous fungal saprophytes found in diverse ecological niches worldwide. Among them, Aspergillus fumigatus is the most prevalent and is largely responsible for the increased incidence of invasive aspergillosis with high mortality rates in some immunocompromised hosts. Azoles are the first-line drugs in treating diseases caused by Aspergillus spp. However, increasing reports in A. fumigatus azole resistance, both in the clinical setting and in the environment, are threatening the effectiveness of clinical and agricultural azole drugs. The azole target is the 14-α sterol demethylase encoded by cyp51A gene and the main mechanisms of resistance involve the integration of tandem repeats in its promoter and/or single point mutations in this gene. In A. fumigatus, azole resistance can emerge in two different scenarios: a medical route in which azole resistance is generated during long periods of azole treatment in the clinical setting and a route of resistance derived from environmental origin due to extended use of demethylation inhibitors in agriculture. The understanding of A. fumigatus azole resistance development and its evolution is needed in order to prevent or minimize its impact. In this article, we review the current situation of azole resistance epidemiology and the predominant molecular mechanisms described based on the resistance acquisition routes. In addition, the clinical implications of A. fumigatus azole resistance and future research are discussed.

show abstract

Advances in understanding molecular mechanisms of fungicide resistance and molecular detection of resistant genotypes in phytopathogenic fungi

2005

View full text Add to dashboard Cite

The mechanism of resistance to sterol 14? demethylation inhibitors in a mutant (Erg 40) ofUstilago maydis

Cited by 9 publications

References 25 publications

Novel Pyrido[4,3-d]pyrimidine Derivatives as Potential Sterol 14α-Demethylase Inhibitors: Design, Synthesis, Inhibitory Activity, and Molecular Modeling

Novel Pyrido[4,3-d]pyrimidine Derivatives as Potential Sterol 14α-Demethylase Inhibitors: Design, Synthesis, Inhibitory Activity, and Molecular Modeling

Triazole Resistance in Aspergillus Species: An Emerging Problem

Advances in understanding molecular mechanisms of fungicide resistance and molecular detection of resistant genotypes in phytopathogenic fungi

Contact Info

Product

Resources

About