• Title/Summary/Keyword: iTS

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Synthesis of Nonclassical Quinazolinone Antifolates as Thymidylate Synthase Inhibitors and Their Antitumor Activity In Vitro

  • Baek, Du-Jong;Kang, Tae-Beom;Kim, Hyun-Ju
    • Bulletin of the Korean Chemical Society
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    • v.25 no.12
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    • pp.1898-1906
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    • 2004
  • Nonclassical quinazolinone analogs I, II, and III, in which the glutamic acid moiety of the classical antifolates is substituted by phenylglycine, phenylalanine or aminobenzoic acid and their methyl esters, were synthesized and evaluated as lipophilic inhibitors of thymidylate synthase (TS). The target compounds were generally potent inhibitors of L. casei and human TS with $IC_{50}$ values within the narrow range of 0.2-10 ${\mu}$M and 0.003-0.03 ${\mu}$M, respectively. Further, most of the target compounds showed cytotoxicity against tumor cell lines of murine and human origin with $IC_{50}$ values of as low as 0.050 ${\mu}$M. Substitution of another hydroxyl or carboxylic acid/ester group at the phenyl ring further increased the potency of TS inhibition and cell growth inhibition. Most effective were compounds If and Ic in which extra carboxylic acid/ester was present at the phenyl ring with nanomolar $IC_{50}$ values of 0.0044 and 0.0093 ${\mu}$M against human TS and submicromolar cytotoxic growth inhibition against all four tumor cell lines.

Epitaxy of Si and Si1-xGex(001) by ultrahigh vacuum ion-beam sputter deposition

  • Lee, N. E.;Greene, J. E.
    • Journal of Korean Vacuum Science & Technology
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    • v.2 no.2
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    • pp.107-117
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    • 1998
  • Epitaxial undoped and Sb-doped si films have been grown on Si(001) substrates at temperatures T between 80 and 750$^{\circ}C$ using energetic Si in ultra-high-vacuum Kr+-ion-beam sputter deposition(IBSD). Critical epitaxial thicknesses te, The average thickness of epitaxial layers, in undoped films were found to range from 8nm at Ts=80$^{\circ}C$ to > 1.2 ${\mu}$m at Ts=300$^{\circ}C$ while Sb incorporation probabilities $\sigma$sb varied from unity at Ts 550$^{\circ}C$ to 0.1 at 750$^{\circ}C$. These te and $\sigma$Sb values are approximately one and one-to-three orders of magnitude, respectively, higher than reported results achieved with molecular-beam epitaxy. Plan-view and cross-sectional transmission electron microscopy, high-resolution x-ray diffraction, channeling and axial angular-yield profiles by Rutherford back scattering spectroscopy for epitaxial Si1-x Gex(001) alloy films (0.15$\leq$x$\leq$0.30) demonstrated that the films are of extremely high crystalline quality. critical layer thicknesses hc the film thickness where strain relaxation starts, I these alloys wre found to increase rapidly with decreasing growth temperature. For Si0.70 Ge0.30, hc ranged from 35nm at Ts=550$^{\circ}C$ to 650nm at 350$^{\circ}C$ compared to an equilibrium value of 8nm.

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Expression of TS, RRM1, ERCC1, TUBB3 and STMN1 Genes in Tissues of Non-small Cell Lung Cancer and its Significance in Guiding Postoperative Adjuvant Chemotherapy

  • Zou, Zhi-Qiang;Du, Yi-Ying;Sui, Gang;Xu, Shi-Ning
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.8
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    • pp.3189-3194
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    • 2015
  • Background: To explore the expression of TS, RRM, ERCC1, TUBB3 and STMN1 genes in the tissues of patients with non-small cell lung cancer (NSCLC) and its significance in guiding the postoperative adjuvant chemotherapy. Materials and Methods: Real time polymerase chain reaction (PCR) was applied to detect the expression of TS, RRM, ERCC1, TUBB3 and STMN1 genes in the tissues of NSCLC patients so as to analyze the relationship between the expression of each gene and the clinical characteristics and to guide the postoperative individualized chemotherapy according to the detection results of NSCLC patients. Results: Expression of TS gene was evidently higher in patients with adenocarcinoma than those with non-adenocarcinoma (P=0.013) and so was the expression of ERCC1 (P=0.003). The expression of TUBB3 gene was obviously higher in NSCLC patients in phases I/II and IV than those in phase III ($P_1=0.021$; $P_2=0.004$), and it was also markedly higher in patients without lymph node metastasis than those with (P=0.008). The expression of STMN1 gene was apparently higher in patients in phase I/II than those in phase IV (P=0.002). There was no significant difference between the rest gene expression and the clinical characteristics of NSCLC patients (P>0.05). Additionally, the diseasefree survival (DFS) was significantly longer in patients receiving gene detections than those without (P=0.021). Conclusions: The selection of chemotherapeutic protocols based singly on patients' clinical characteristics has certain blindness. However, the detection of tumor-susceptible genes can guide the postoperative adjuvant chemotherapy and prolong the DFS of NSCLC patients.

Correlation between Electrical Conduction and Dielectric Relaxation in the Glass System $Cul-Cu_2S-Cu_2O-MoO_3$ ($Cul-Cu_2S-Cu_2O-MoO_3$계 유리의 전기전도 및 유전환화와의 상관)

  • 이재형;임기조
    • The Transactions of the Korean Institute of Electrical Engineers
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    • v.43 no.7
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    • pp.1152-1157
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    • 1994
  • The glasses were prpared in the system CuI-CuS12TS-CuS12TO-MoOS13T by rapid quenching technique. These glasses have high ionic conductivities at 2$0^{\circ}C$ in the range of 10S0-1T[S/m], and the conductivities increase with increasing CuI and CuS12TS content. The value of activation energy for dielectric relaxation is nearly identical with that for conductivity. The cole-Cole parameter $\beta$ for representation of the distribution of dielectric relaxation times varies the range from 0.92 to 0.96. This parameter has a weak dependence on the composition of glass, and is independent of temperature. The correlation factors P for the glasses shows from 1.1 to 1.7.

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Test Method with TSS in Bluetooth Baseband (블루투스 베이스밴드의 Test Suite Structure에 의한 테스트 방안)

  • Moon, Sang-ook
    • Proceedings of the Korean Institute of Information and Commucation Sciences Conference
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    • v.9 no.2
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    • pp.997-999
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    • 2005
  • In order for efficient Bluetooth Baseband functional test, Bluetooth SIG (Special Interest Group) provides with Test Suite Structure (TSS) in the Bluetooth specification version 1.1. Bluetooth Baseband hardware which needs to be authenticated should implement the test specification defined in the TSS part I.1 through I.3. In this paper, we discuss the method to verify and test a Bluetooth Baseband implementation based on the TSS version 1.0. Also, we describe various senario and implementation possibilities to perform the Bluetooth Baseband authentication test.

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Performance Assessment of Two-stream Convolutional Long- and Short-term Memory Model for September Arctic Sea Ice Prediction from 2001 to 2021 (Two-stream Convolutional Long- and Short-term Memory 모델의 2001-2021년 9월 북극 해빙 예측 성능 평가)

  • Chi, Junhwa
    • Korean Journal of Remote Sensing
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    • v.38 no.6_1
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    • pp.1047-1056
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    • 2022
  • Sea ice, frozen sea water, in the Artic is a primary indicator of global warming. Due to its importance to the climate system, shipping-route navigation, and fisheries, Arctic sea ice prediction has gained increased attention in various disciplines. Recent advances in artificial intelligence (AI), motivated by a desire to develop more autonomous and efficient future predictions, have led to the development of new sea ice prediction models as alternatives to conventional numerical and statistical prediction models. This study aims to evaluate the performance of the two-stream convolutional long-and short-term memory (TS-ConvLSTM) AI model, which is designed for learning both global and local characteristics of the Arctic sea ice changes, for the minimum September Arctic sea ice from 2001 to 2021, and to show the possibility for an operational prediction system. Although the TS-ConvLSTM model generally increased the prediction performance as training data increased, predictability for the marginal ice zone, 5-50% concentration, showed a negative trend due to increasing first-year sea ice and warming. Additionally, a comparison of sea ice extent predicted by the TS-ConvLSTM with the median Sea Ice Outlooks (SIOs) submitted to the Sea Ice Prediction Network has been carried out. Unlike the TS-ConvLSTM, the median SIOs did not show notable improvements as time passed (i.e., the amount of training data increased). Although the TS-ConvLSTM model has shown the potential for the operational sea ice prediction system, learning more spatio-temporal patterns in the difficult-to-predict natural environment for the robust prediction system should be considered in future work.

The α-Effect in Nucleophilic Substitution Reactions of Y-Substituted-Phenyl X-Substituted-Cinnamates with Butane-2,3-dione Monoximate

  • Kim, Min-Young;Son, Yu-Jin;Um, Ik-Hwan
    • Bulletin of the Korean Chemical Society
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    • v.34 no.10
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    • pp.2877-2882
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    • 2013
  • Second-order rate constants ($k_{Ox^-}$) have been measured spectrophotometrically for nucleophilic substitution reactions of 4-nitrophenyl X-substituted-cinnamates (7a-7e) and Y-substituted-phenyl cinnamates (8a-8e) with butane-2,3-dione monoximate ($Ox^-$) in 80 mol % $H_2O$/20 mol % DMSO at $25.0{\pm}0.1^{\circ}C$. The Hammett plot for the reactions of 7a-7e consists of two intersecting straight lines while the Yukawa-Tsuno plot exhibits an excellent linearity with ${\rho}_X$=0.85 and r=0.58, indicating that the nonlinear Hammett plot is not due to a change in the rate-determining step but is caused by resonance stabilization of the ground state (GS) of the substrate possessing an electron-donating group (EDG). The Br${\o}$nsted-type plot for the reactions of Y-substituted-phenyl cinnamates (8a-8e) is linear with ${\beta}_{lg}$ = -0.64, which is typical of reactions reported previously to proceed through a concerted mechanism. The ${\alpha}$-nucleophile ($Ox^-$) is more reactive than the reference normal-nucleophile ($4-ClPhO^-$). The magnitude of the ${\alpha}$-effect (i.e., the $k_{Ox^-}/k_{4-ClPhO^-}$ ratio) is independent of the electronic nature of the substituent X in the nonleaving group but increases linearly as the substituent Y in the leaving group becomes a weaker electron-withdrawing group (EWG). It has been concluded that the difference in solvation energy between $Ox^-$ and $4-ClPhO^-$ (i.e., GS effect) is not solely responsible for the ${\alpha}$-effect but stabilization of transition state (TS) through a cyclic TS structure contributes also to the Y-dependent ${\alpha}$-effect trend (i.e., TS effect).

Purification and Characterization of Clostridium thermocellum Xylanase from Recombinant Escherichia coli

  • Koo, Bon-Joon;Oh, Hwa-Gyun;Cho, Ki-Haeng;Yang, Chang-Kun;Jung, Kyung-Hwa;Ryu, Dai-Young
    • Journal of Microbiology and Biotechnology
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    • v.6 no.6
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    • pp.414-419
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    • 1996
  • The xylnX gene encoding a xylanase from Clostridium thermocellum ATCC27405 was cloned in the plasmid pJH27, an E. coli-Bacillus shuttle vector and the resultant recombinant plasmid, pJX18 was transformed into E. coli HB101. The overexpressed xylanase was found to be secreted into the periplasmic space of the recombinant E. coli cells. The crude enzyme was obtained by treating the E. coli cells with lysozyme, and purified by DEAE-Sepharose column chromatography. Molecular wieght of the xylanase was estimated to be 53 kDa by gel filtration. The pI value was determined to be pH 8.8. The N-terminal sequence of the enzyme protein was Asp-Asp-Asn-Asn-Ala-Asn-Leu-Val-Ser-Asn which was considered to be the sequence of that of the mature form protein. The Km value of the enzyme for oat spelt xylan was calculated to be 2.63 mg/ml and the Vmax value was $0.47 {\mu}mole/min$. The xylanase had a pH optimum for its activity at pH 5.4 and a temperature optimum at $60^{\circ}C$. The enzyme hydrolyzed xylan into xylooligosaccharides which were composed mainly of xylobiose (40%) and xyloltriose (12%) after 5 hour reaction. This result indicates that the xylanase from C. thermocellum ATCC27405 is an endo-acting enzyme.

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Acoustic Target Strength of Live Japanese Common Squid(Todarodes pacifica) for Applying Biomass Estimation (살오징어 (Todarodes pacifica)의 음향 반사강도 측정)

  • KANG Donhyug;HWANG Doojin;MUKAI Tohru;IIDA KohjI;LEE Kyounghoon
    • Korean Journal of Fisheries and Aquatic Sciences
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    • v.37 no.4
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    • pp.345-353
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    • 2004
  • Target strength (TS) of Japanese common squids (Todarodes pacificus) were measured using 38 and 120 kHz split beam scientific echosounders under the live condition. For the TS measurement of an individual, a total of 3 squids (mantle length (ML): 22.8, 25, and 27 cm) were used using small fishhook method, whereas for measurement of swimming angle, a total of 8 squids (ML: 21-27 cm) were used under live condition, confined with net cage with 2 m diameter At the same time, two underwater video cameras enabled continuous monitoring of squid behavior. Considering normal behavior, the mean TS at 38 and 120 kHz varied from -48.6 to -45.9 dB, and from -46.5 to -44.6 dB, respectively In both frequencies, mean TS at 120 kHz is relatively higher than that of 38 kHz, approximately 1.3-2.5 dB. From free living condition, the mean swimming angle of the squlds was $-24^{\circ}$. The results of the measurement will be provided basic information for conducting acoustic surveys of the squid.

Maxillary Distraction Osteogenesis Using $TS-MD^{(R)}$ (Trans-sinusoidal Maxillary distractor) on Cleft Patients (Trans-sinusoidal maxillary distractor($TS-MD^{(R)}$)를 이용한 구순구개열 환자에서의 상악골 골신장술)

  • Paeng, Jun-Young;Lee, Il-Gu;Myoung, Hoon;Hwang, Soon-Jung;Seo, Byoung-Moo;Choe, Jin-Yeong;Lee, Jong-Ho;Choung, Pill-Hoon;Kim, Myung-Jin
    • Korean Journal of Cleft Lip And Palate
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    • v.8 no.2
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    • pp.71-79
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    • 2005
  • Purpose: Maxillary hypoplasia is a common developmental problem of cleft lip and palate. Fair results with distraction osteogenesis have been reported especially when these patients need a large amount of maxillary advancement, instead of orthognathic surgery. The purpose of this study is to evaluate the clinical results with a relatively new distractor, $TS-MD^{(R)}$ (Trans-sinusoidal maxillary distractor, KLS Martin, Tuttlingen, Germany) which was used for the advancement of the maxilla in the cleft patients. Patients and Method: Distraction osteogenesis using $TS-MD^{(R)}$ was performed for four CLP patients (three males and one female) who had maxillary hypoplasia. All patients were over 16 years old. As three patients showed mandibular prognathism as well, bilateral sagittal split ramus osteotomy for mandibular setback was performed at the same time. After consolidation periods of 4 to 12 weeks, the distraction devices were removed and miniplates were placed for simultaneous internal fixation. Results: Three patients showed a large amount of incisal overbite but one patient did not have sufficient maxillary advancement. Le Fort I osteotomy, maxillary advancement and internal fixation should have been performed for the patient when removing the distraction devices. Different from the $clinician{\box}s$ expectation, the amount of maxillary advancement using $TS-MD^{(R)}$ was not sufficient, although the device has rigid mechanical property. Rotation of maxilla during distraction forward and downward was also observed. Conclusion: Even though the maxillary advancement with $TS-MD^{(R)}$ device could be achieved, the clinical control of some characteristics related with the device was necessary. More clinical studies on $TS-MD^{(R)}$ should be performed.

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