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Lee, Sang Jae,Choi, Jang-Sik,Bong, Seoung Min,Hwang, Hae-Jun,Lee, Jaesang,Song, Ho-Juhn,Lee, Jaekyoo,Kim, Jung-Ho,Koh, Jong Sung,Lee, Byung Il Korean Society for Molecular and Cellular Biology 2018 Molecules and cells Vol.41 No.6
Spleen tyrosine kinase (SYK) is a cytosolic non-receptor protein tyrosine kinase. Because SYK mediates key receptor signaling pathways involving the B cell receptor and Fc receptors, SYK is an attractive target for autoimmune disease and cancer treatments. To date, representative oral SYK inhibitors, including fostamatinib (R406 or R788), entospletinib (GS-9973), cerdulatinib (PRT062070), and TAK-659, have been assessed in clinical trials. Here, we report the crystal structures of SYK in complex with two newly developed inhibitors possessing 4-aminopyrido[4,3-D]pyrimidine moieties (SKI-G-618 and SKI-O-85). One SYK inhibitor (SKI-G-618) exhibited moderate inhibitory activity against SYK, whereas the other inhibitor (SKI-O-85) exhibited a low inhibitory profile against SYK. Binding mode analysis indicates that a highly potent SYK inhibitor might be developed by modifying and optimizing the functional groups that interact with Leu377, Gly378, and Val385 in the G-loop and the nearby region in SYK. In agreement with our structural analysis, one of our SYK inhibitor (SKI-G-618) shows strong inhibitory activities on the ${\beta}$-hexosaminidase release and phosphorylation of SYK/Vav in RBL-2H3 cells. Taken together, our findings have important implications for the design of high affinity SYK inhibitors.
Application of a NDI Method Using Magneto-Optical Film for Micro-Cracks
Jaekyoo Lim,Hyoungno Lee,Jinyi Lee,Tetsuo Shoji 대한기계학회 2002 JOURNAL OF MECHANICAL SCIENCE AND TECHNOLOGY Vol.16 No.5
Leakage magnetic flux is occurred in the cracked area of magnetized specimens, and also it changes the magnetic domain area of the magneto-optical film positioned on the specimen. It causes the change of the optical permeability of the magnetic domain on the crack area. So crack images can be obtained easily using this principle. On the other hand, utilizing a laser in this method makes possible to perform a remote sensing by detecting the light intensity contrast between cracked area and normal area. This paper shows the application of non-destructive inspection system taking advantage of magneto-optical method for micro-cracks and presents examples applied to the several types of specimens having fatigue cracks and fabricated cracks using this method. Also the authors prove the possibility of this method as a remote sensing system under the oscillation load considering application to real fields.
Jin, Younghee,Seung, Hyunjung,Oh, Younghee,Jung, Jihun,Jeon, Sujin,Lee, Jaekyoo,Kim, ChangKyu,Choi, Sungmin,Chae, Youngzoo 대한미생물학회 2013 Journal of Bacteriology and Virology Vol.43 No.1
Of total 1,438 specimens of patients with diarrhea in Seoul, 2011, 217 samples (15%) were found pathogenic Escherichia coli that included 192 strains (89%) of enterotoxigenic E. coli (ETEC) and enteroaggregative E. coli (EAEC). The highest isolation rate for ETEC and EAEC was found in August and September. Sixty two pathogenic E. coli strains (34 ETEC and 28 EAEC strains) were selected from 175 strains (94 ETEC and 81 EAEC strains) isolated in August and September. Of 94 strains characterized for ETEC phenotype, 76 (81%) expressed heat-stable toxin (ST) only. Antimicrobial susceptibility test was carried out by using sixteen types of antibiotics. A high level of antimicrobial resistance to tetracycline (57%), ampicillin and ticarcillin (54%) was observed among EAEC isolates while the highest resistance rate of ETEC was found for nalidixic acid (47%), followed by tetracycline (32%). As to the antimicrobial susceptibility test, EAEC showed the complicated multi-drug resistant patterns in which the resistance was higher than ETEC. Pulsed-field gel electrophoresis (PFGE) was carried out to examine the genetic relatedness among ETEC and EAEC isolates. Except for 11 strains, 51 strains were divided by eight pulsotypes. In PFGE analysis, isolates from foodborne disease outbreaks in August and September 2011 showed close relation.