• Title/Summary/Keyword: CR229

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Discovery of Cyclin-dependent Kinase Inhibitor, CR229, Using Structure-based Drug Screening

  • Kim, Min-Kyoung;Min, Jae-Ki;Choi, Bu-Young;Lim, Hae-Young;Cho, Youl-Hee;Lee, Chul-Hoon
    • Journal of Microbiology and Biotechnology
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    • v.17 no.10
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    • pp.1712-1716
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    • 2007
  • To generate new scaffold candidates as highly selective and potent cyelin-dependent kinase (CDK) inhibitors, structure-based drug screening was performed utilizing 3D pharmacophore conformations of known potent inhibitors. As a result, CR229 (6-bromo-2,3,4,9-tetrahydro-carbolin-1-one) was generated as the hit-compound. A computational docking study using the X-ray crystallographic structure of CDK2 in complex with CR229 was evaluated. This predicted binding mode study of CR229 with CDK2 demonstrated that CR229 interacted effectively with the Leu83 and Glu81 residues in the ATP-binding pocket of CDK2 for the possible hydrogen bond formation. Furthermore, biochemical studies on inhibitory effects of CR229 on various kinases in the human cervical cancer HeLa cells demonstrated that CR229 was a potent inhibitor of CDK2 ($IC_{50}:\;3\;{\mu}M$), CDKI ($IC_{50}:\;4.9\;{\mu}M$), and CDK4 ($IC_{50}:\;3\;{\mu}M$), yet had much less inhibitory effect ($IC_{50}:>20\;{\mu}M$) on other kinases, such as casein kinase 2-${\alpha}1$ (CK2-${\alpha}1$), protein kinase A (PKA), and protein kinase C (PKC). Accordingly, these data demonstrate that CR229 is a potent CDK inhibitor with anticancer efficacy.

Immediate Effects of Various Contract-Relax Techniques on the Peck Force and Range of Motion of Knee Extension -A Pilot Study- (수축-이완 기법 방법에 다른 최대 힘과 무릎관절 가동 범위에 미치는 즉각적인 효과 비교 -예비연구-)

  • Shin, Seung-Sub
    • PNF and Movement
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    • v.16 no.2
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    • pp.229-238
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    • 2018
  • Purpose: This study aimed to compare the immediate effects of various contract-relax (CR) techniques on the peck force and passive range of motion (ROM) of knee extension. Methods: This study recruited 17 adult males and females who obtained below $90^{\circ}$ in straight leg raising. The subjects randomly performed one of three different CR techniques (direct CR, indirect CR, and modified CR) on the right knee extension four times per day for three days. The subjects' peck force during each CR and their passive knee extension on the hip at a $90^{\circ}$ flexed position before and after each CR were measured. Results: The peck force was significantly higher in the direct and modified CR than in the indirect CR. The ROM in the passive knee extension significantly increased after direct and indirect CR. Comparing between each CR, the passive knee extension range was significantly more improved in the direct and indirect CR than in the modified CR. Conclusion: Direct and indirect CR are more effective than modified CR in the ROM of passive knee extension. The study results suggest that the modified CR did not have the same effect on the ROM of the knee extension as the direct and indirect CR and that further research is needed to recruit more subjects and to determine the effects on different muscles after modified CR.

Fabrication and characteristics of ITO thin films on CR39 substrate for transparent OTFT

  • Kwon, Sung-Yeol
    • Journal of Sensor Science and Technology
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    • v.16 no.3
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    • pp.229-233
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    • 2007
  • The indium tin oxide (ITO) films were deposited on CR39 substrate using DC magnetron sputtering. The ITO thin films deposited at room temperature because CR39 substrate its glass-transition temperature is $130^{\circ}C$. The ITO thin films used bottom and top electrode and for organic thin film transparent transistors (OTFTs). The ITO thin film electrodes electrical properties and optical transparency properties in the visible wavelength range (300-800 nm) strongly dependent on volume of oxygen percent. For the optimum resistivity and transparency of the ITO thin film electrode achieved with a 75 W plasma power, 10 % volume of oxygen and a 27 nm/min deposition rate. Above 85 % transparency in the visible wavelength range (300-800 nm) measured without post annealing process and a low resistivity value $9.83{\times}10^{-4}{\Omega}cm$ was measured thickness of 300 nm. All fabrication process of ITO thin films did not exceed $80^{\circ}C$.

The Effect of Sputter-textured Mo Thin Film on Magnetic properties of CoCrTa/Cr Magnetic Recording Media (Sputter-textured Mo 박막이 CoCrTa/Cr 자기기록매체의 자기적 성질에 미치는 영향)

  • Jo, Sung-Mook;Nam, In-Tak
    • Journal of Industrial Technology
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    • v.21 no.A
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    • pp.221-229
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    • 2001
  • The effect of Mo underlayer on the magnetic properties of CoCrTa/Cr films deposited on glass substrates were investigated. The coercivity increased and the coercivity squareness decreased by introducing Mo underlayer. The coercivity increase was attributed to the increase of in-plane c-axis orientation and magnetic isolation of Co grains deposited on Cr/Mo underlayer. The decrease of coercivity squarenesses seemed to be caused by the increase of magnetic isolation. The increase of magnetic isolation of Co grains was attributed to the diffusion of Mo atoms into grain boundaries of Co films and the physical isolation of Co grains. The coercivity of CoCrTa/Cr/Mo showed maximum values at Mo thickness of $400{\AA}$. The appearance of the maximum coercivity at that thickness was attributed to the development of strong $Co(10{\bar{1}}0)$ and $Co(10{\bar{1}}1)$ preferred orientation.

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Difference between Manifest Refraction (MR) and Cycloplegic Refraction (CR) with Age and Myopic Value (연령과 근시도에 따른 현성굴절검사와 조절마비굴절검사의 비교)

  • Jeong, Woo-Jae;Kang, Ji-Hun;Jeon, In-Chul
    • Journal of Korean Ophthalmic Optics Society
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    • v.18 no.1
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    • pp.85-91
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    • 2013
  • Purpose: The purpose of this study is to investigate difference between manifest refraction (MR) and cycloplegic refraction (CR) with age and myopic value. Methods: Manifest and cycloplegic refractions were carried out on the patients of 229 myopic patients ($25.3{\pm}11.9$ years old). Results: The average results from a pre- and a postcycloplegic refraction showed a reduction of 0.19 D in myopia, 0.02 D in astigmatism and $1.85^{\circ}$ in astigmatism direction. Change of myopic value was higher in 30~40 age. Total 73 eyes of 229 patients who showed 0.50 diopter (D) in spherical, and a high degree of myopia group showed a higher discrepancy rate. Conclusions: The results found in the comparison of the value of the manifest refraction and cycloplegic refractions showed changes of myopic value was not significant with age of patient, but the group of high degree of myopia showed higher discrepancy rate.

The effect of stable oxide dispersoid on the high temperature oxidation behavior of Ni-Cr alloys (Ni-Cr 합금의 고온산화특성에 미치는 안정한 산화물 분산체 효과)

  • 유재민;박상환;강성군
    • Journal of the Korean institute of surface engineering
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    • v.24 no.4
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    • pp.222-229
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    • 1991
  • The oxidation behavior of Ni-6wt.% Cr alloys with various concentration of alumina dispersions(5vol.% 10vol.%) was determined at 1000 and 110$0^{\circ}C$ in oxygen of 1 atm. pressure. Some general observations were ascertained. These include: (a) the addition of alumina dispersoids significantly increased the oxidation resistance of Ni-6wt.% Cr alloy; (b) the rate of oxidation was distinctly decreased as a function of the volume percent of oxide dispersion; and (c) the presence of alumina dispersions promoted the formation of continous, protective Cr2O3 layer at 6 wt.% Cr.

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Influence of Chlorine Treatment on Measurement of Crosslink Density of Wiper Blade

  • Son, Chae Eun;Choi, Sung-Seen
    • Elastomers and Composites
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    • v.55 no.3
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    • pp.229-234
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    • 2020
  • Automobile wiper blades are generally treated with chlorine to lower their friction coefficient with the windshield surface. This treatment could affect the crosslink density measurement of rubber vulcanizates, a material used in windshield wipers, which would consequently alter its chemical and physical properties. Therefore, this study evaluated the influence of chlorination on crosslink density measurements of natural rubber (NR) vulcanizates using a vehicle wiper blade. A method for determining the degree of chlorination was developed where the interaction parameter between the rubber and the swelling solvent was corrected. A decrease in the rubber sample swelling ratio was observed upon chlorination, and the chlorination penetrated less than 1% of the sample thickness. The chlorinated NR was assumed to be chloroprene rubber (CR), which was used to correct the interaction parameter. The results showed the CR contributed approximately 7% to the parameter.

Fabrication of $TiO_2$ Electrode with Seawater; Production of Hydrogen and Cr(VI) Reduction (해수전해질을 활용한 광전극제조 및 광활성 평가)

  • Shim, Eun-Jung;Park, Min-Sung;Her, A-Young;Joo, Hyun-Ku;Yoon, Jae-Kyung
    • 한국신재생에너지학회:학술대회논문집
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    • 2009.11a
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    • pp.226-229
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    • 2009
  • The present works were performed that titanium foil was anodized in various dilution ratios of seawater and distilled water with 10V external voltage applied, then annealed at $450^{\circ}C$ to obtain $TiO_2$ on the Ti substrate. The prepared samples were characterized by instruments (XRD, SEM, and photocurrent) and used to investigate rate of hydrogen production in photoelectrochemical cell as well as Cr(VI) reduction. As the results of experiments, the anodized $TiO_2$ in seawater electrolytes, which are ranged from 15 to 50 times dilution of seawater, was showed a relatively higher hydrogen production (ca. 97~110 umol/hr-$cm^2$) and Cr(VI) reduction (ca. 95% reduction).

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Ultrasonographic Evaluation of Surgically Induced Cranial Cruciate Ligament Rupture in the Dog (개에서 전십자 인대 단열의 초음파적 평가)

  • 성윤상;엄기동;장광호
    • Journal of Veterinary Clinics
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    • v.20 no.2
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    • pp.229-232
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    • 2003
  • Ultrasonographic examination of the stifle joint four clinically and radiographically normal adult dogs was performed before and after inducing the cranial cruciate ligament (CrCL) rupture of the bilateral stifle surgically. At Pre- or post-surgery, the hyperechoic patella ligament and the echogenic infrapatella fat interfered the visualization of the CrCL by the plain scanning method. However when the stifle joint was imaged by the scanning method injecting normal saline within the joint capsule, the hyperechogenic ligament was visualized by the separation of the infrapatella fat and the CrCL and the contrast effect of anechoic saline. When the stifle joint was imaged by the real time scanning method after the induction of the surgical rupture, fluttering of the ligament and anechoic area between the bone and the CrCL was identified due to the lack of tonicity and continuity of the ligament. Enlargement of the ligament because of its increased diameter as well as fluttering of the CrCL and the increased joint space's thickness was visualized. Consequently, confirming fluttering of the CrCL, increased ligament diameter and anechoic region between the CrCL and the bone, ultrasonographic examination is a valuable diagnostic tool as well as cranial drawer test and radiographic examination.