• Bulletin of the Korean Chemical Society
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• v.34 no.4
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• pp.1023-1024
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• 2013

• Bulletin of the Korean Chemical Society
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• v.33 no.11
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• pp.3772-3776
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• 2012

Mitogen-activated protein kinase phosphatase 4 (MKP4) has proved to be a promising target for the development of therapeutics for the treatment of diabetes and the other metabolic diseases. Here, we report an example for a successful application of the structure-based virtual screening to identify three novel inhibitors of MKP4. These inhibitors have desirable physicochemical properties as a drug candidate and reveal a moderate potency with $IC_{50}$ values ranging from 4.9 to $32.3{\mu}M$. Therefore, they deserve consideration for further development by structure-activity relationship studies to optimize the inhibitory and antidiabetic activities. Structural features relevant to the stabilization of the newly identified inhibitors in the active site of MKP4 are discussed in detail.

• Research in Plant Disease
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• v.16 no.3
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• pp.279-284
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• 2010

Clubroot caused by Plasmodiophora brassicae is a widespread disease that causes serious problems in many brassica growing areas. To establish more simple and reliable clubroot screening method of Chinese cabbage to P. brassicae using soil-drenching inoculation, the development of clubroot on Chinese cabbage according to several conditions such as soil type, inoculum concentration of P. brassicae GN-1 (race 9), plant growth stage and incubation period was studied. In a commercial horticulture nursery media soil (CNS), disease severity of the seedling according to inoculum concentration increased in a dose-dependent manner, but did not in mixture of CNS and upland soil (1:1, v/v). To facilitate and acquire precise result of resistance screening of Chinese cabbage to clubroot, 10-day-old seedlings should be inoculated by drenching the spore suspension of P. brassicae to give inoculum density of $4.0{\times}10^8$ spores/pot. To develop the disease, the inoculated seedlings were incubated in a growth chamber at $20^{\circ}C$ for 3 days, and then cultivated in a greenhouse ($25{\pm}5^{\circ}C$) for five weeks. Under the optimum conditions, 25 clubroot-resistant (CR) and 3 clubroot-susceptible (CS) cultivars were tested for resistance to P. brassicae. All CR cultivars showed very clear resistance response, on the other hand all CS cultivars severly infected with the pathogen. The results suggest that this method is efficient screening method of Chinese cabbage for resistance to clubroot disease.

• Research in Plant Disease
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• v.17 no.1
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• pp.13-18
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• 2011

This study was conducted to establish the efficient screening method for resistant cabbage to Fusarium wilt caused by Fusarium oxysporum f. sp. conglutinans. The resistance degrees of nine commercial cabbage cultivars to the disease were evaluated. Among them, five cultivars (YR-honam, Ogane, Greenhot, Redmat, and Ccoccoma) showing different resistance to the fungus were selected. Then development of Fusarium wilt of the cultivars according to several conditions including root wounding, dipping period of roots in spore suspension, inoculum concentration, and incubation temperature to develop the disease was investigated. Highly resistant cultivars such as 'YR-honam' and 'Ogane' hardly showed change of resistance to the disease by root wounding, dipping period, and inoculum concentration, while disease severity of Fusarium wilt on the cultivars was changed with incubation temperatures ($20^{\circ}C$, $25^{\circ}C$ and $30^{\circ}C$). When the cabbage cultivars were incubated at $25^{\circ}C$, they represented the most difference of resistance and susceptibility to Fusarium wilt. From above results, we suggest that an efficient screening method for resistant cabbage to F. oxysporum f. sp. conglutinans is to dip the non-cut roots of 14-day-old seedlings in spore suspension of $1{\times}10^7$ conidia/ml for 0.5 hr and to transplant the seedlings to plastic pots with a fertilized soil, and then to cultivate the plants in a growth chamber at $25^{\circ}C$ for 3 weeks to develop Fusarium wilt.

• Korean Chemical Engineering Research
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• v.54 no.6
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• pp.812-816
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• 2016

We isolated a novel methylotrophic bacterium from soil collected in Dongducheon Environment Affairs Agency. The isolate was identified as Methylobacterium sp. WJ4 based on phylogenetic analysis. Plackett-Burman design was employed for screening eight parameters of nitrate mineral salts (NMS) medium for cell growth of a newly isolated Methylobacterium sp. WJ4 with experimental validation. Trace element solution and vitamin stock were found to affect cell growth, which can be further optimized for increased cell growth. This is the first report of screening parameters of NMS medium which affect cell growth of strain belonging to the genus Methylobacterium using Plackett-Burman design.

• Bulletin of the Korean Chemical Society
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• v.30 no.8
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• pp.1873-1876
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• 2009

• The Korean Journal of Pesticide Science
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• v.4 no.3
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• pp.19-26
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• 2000

In order to select potent bioactive isolates, 70 Fusarium isolates obtained from soil and 21 plant species were screened by antifungal, insecticidal, herbicidal, and duckweed bioassays after culturing in potato dextrose broth and rice solid media. Eight (11.4%) of the 70 liquid broth cultures showed disease-controlling activities more than 80% against at least one of the 6 plant diseases tested. Fusarium sp. FO-68 isolate exhibited the most potent antifungal activity; it controlled rice blast, wheat leaf rust, and barley powdery mildew with control values more than 95%. Out of 70 solid cultures, 21 (30.0%) controlled at least one plant disease more than 80% and F. equiseti FO-68 isolate showed disease-controlling activities more than 95% against 3 plant diseases such as rice blast, tomato late blight, and wheat leaf rust. As for tile insecticidal activities, 2 liquid and 1 solid cultures showed potent insecticidal activities against pest insects more than 80%, Liquid cultures of F. oxysporum FO-61 and Fusarium sp. FO-80 isolates exhibited insecticidal activities more than 80% against green peach aphid and diamondback moth, respectively. The solid culture of Fusarium sp. FO-510 isolate had 80% insecticidal activity against green peach aphid. However, none of liquid and solid cultures of the 70 Fusarium isolates showed potent herbicidal activities against 10 upland weeds. As the results of duckweed assay, 3 liquid cultures showed 70% growth inhibitory activity at concentrations less than 1.25% of culture supernatants and 9 solid cultures had a potent inhibitory activity against duckweed growth. On the other hand, there was a significant correlation between antifungal activities and herbicidal activities against duckweed of both liquid and solid cultures of tile 70 Fusarium isolates.

• Weed & Turfgrass Science
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• v.4 no.2
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• pp.118-123
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• 2015

Metagenomics is a powerful tool to isolate novel biocatalyst and biomolecules directly from the environmental DNA libraries. Since the metagenomics approach bypasses cultivation of microorganisms, un-cultured microorganisms that are majority of exists can be the richest reservoir for natural products discovery. To discover novel herbicidal substances from soil metagenome, we established three easy, simple and effective high throughput screening methods such as cucumber cotyledon leaf disc assay, microalgae assay and seed germination assay. Employing the methods, we isolated two active single clones (9-G1 and 9-G12) expressing herbicidal activity which whitened leaf discs, inhibited growth of microalgae and inhibited root growth of germinated Arabidopsis seeds. Spraying butanol fraction of the isolated active clones' culture broth led to growth retardation or desiccation of Digitalia sanguinalis (L) Scop. in vivo. These results represent that the screening methods established in this study are useful to screen herbicidal substances from metagenome libraries. Further identifying molecular structure of the herbicidal active substances and analyzing gene clusters encoding synthesis systems for the active substances are in progress.

• Bulletin of the Korean Chemical Society
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• v.30 no.5
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• pp.1177-1180
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• 2009

• Bulletin of the Korean Chemical Society
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• v.35 no.9
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• pp.2655-2659
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• 2014

Dual specificity protein phosphatase 4 (DUSP4) has been considered a promising target for the development of therapeutics for various human cancers. Here, we report the first example for a successful application of the structure-based virtual screening to identify the novel small-molecule DUSP4 inhibitors. As a consequence of the virtual screening with the modified scoring function to include an effective molecular solvation free energy term, five micromolar DUSP4 inhibitors are found with the associated $IC_{50}$ values ranging from 3.5 to $10.8{\mu}M$. Because these newly identified inhibitors were also screened for having desirable physicochemical properties as a drug candidate, they may serve as a starting point of the structure-activity relationship study to optimize the medical efficacy. Structural features relevant to the stabilization of the new inhibitors in the active site of DUSP4 are discussed in detail.