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Identification and Pharmacological Analysis of High Efficacy Small Molecule Inhibitors of EGF-EGFR Interactions in Clinical Treatment of Non-Small Cell Lung Carcinoma: a Computational Approach

  • Gudala, Suresh;Khan, Uzma;Kanungo, Niteesh;Bandaru, Srinivas;Hussain, Tajamul;Parihar, MS;Nayarisseri, Anuraj;Mundluru, Hema Prasad
    • Asian Pacific Journal of Cancer Prevention
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    • v.16 no.18
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    • pp.8191-8196
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    • 2016
  • Inhibition of EGFR-EGF interactions forms an important therapeutic rationale in treatment of non-small cell lung carcinoma. Established inhibitors have been successful in reducing proliferative processes observed in NSCLC, however patients suffer serious side effects. Considering the narrow therapeutic window of present EGFR inhibitors, the present study centred on identifying high efficacy EGFR inhibitors through structure based virtual screening strategies. Established inhibitors - Afatinib, Dacomitinib, Erlotinib, Lapatinib, Rociletinib formed parent compounds to retrieve similar compounds by linear fingerprint based tanimoto search with a threshold of 90%. The compounds (parents and respective similars) were docked at the EGF binding cleft of EGFR. Patch dock supervised protein-protein interactions were established between EGF and ligand (query and similar) bound and free states of EGFR. Compounds ADS103317, AKOS024836912, AGN-PC-0MXVWT, GNF-Pf-3539, SCHEMBL15205939 were retrieved respectively similar to Afatinib, Dacomitinib, Erlotinib, Lapatinib, Rociletinib. Compound-AGN-PC-0MXVWT akin to Erlotinib showed highest affinity against EGFR amongst all the compounds (parent and similar) assessed in the study. Further, AGN-PC-0MXVWT brought about significant blocking of EGFR-EGF interactions in addition showed appreciable ADMET properties and pharmacophoric features. In the study, we report AGN-PC-0MXVWT to be an efficient and high efficacy inhibitor of EGFR-EGF interactions identified through computational approaches.

Multi-focus Image Fusion Technique Based on Parzen-windows Estimates (Parzen 윈도우 추정에 기반한 다중 초점 이미지 융합 기법)

  • Atole, Ronnel R.;Park, Daechul
    • The Journal of the Institute of Internet, Broadcasting and Communication
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    • v.8 no.4
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    • pp.75-88
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    • 2008
  • This paper presents a spatial-level nonparametric multi-focus image fusion technique based on kernel estimates of input image blocks' underlying class-conditional probability density functions. Image fusion is approached as a classification task whose posterior class probabilities, P($wi{\mid}Bikl$), are calculated with likelihood density functions that are estimated from the training patterns. For each of the C input images Ii, the proposed method defines i classes wi and forms the fused image Z(k,l) from a decision map represented by a set of $P{\times}Q$ blocks Bikl whose features maximize the discriminant function based on the Bayesian decision principle. Performance of the proposed technique is evaluated in terms of RMSE and Mutual Information (MI) as the output quality measures. The width of the kernel functions, ${\sigma}$, were made to vary, and different kernels and block sizes were applied in performance evaluation. The proposed scheme is tested with C=2 and C=3 input images and results exhibited good performance.

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A Study on the Forms and Modifications of 'Chang-aelgool'(窓乻骨) in Annex and Pavillion Buildings in Yeong-nam Region during the Chosun Dynasty - Focused on 'Ondol' Rooms and 'Ssang-chang' around the Main Floored Room - (조선시대 영남지방 별당과 정자건축의 '창얼굴' 형식 및 변천에 관한 연구 -온돌방과 대청 주위 쌍창을 중심으로-)

  • Park, Il-Chan;Lee, Ho-Yeol
    • Journal of architectural history
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    • v.21 no.3
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    • pp.73-92
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    • 2012
  • This study mainly inquired characteristics and changes of 'Chang-aelgool' through 38 cases(with 161 Ssang-chang) of annex and pavillion buildings in Yeong-nam region which are built during the Chosun dynasty. The method of inquiry included actual survey of windows along with bibliographical research, and the results are as below. First, through the discovery of the term 'Chang-aelgool' as an indication of the window-forming frame in 'YeongGeonUiGwe'(1680 A.D), it is apparent that the term 'Chang-aelgool' was widely used in Korea from the late 17th century. Second, the 'Chang-aelgool' of study objects are classified into 4 categories. Type I and II are comprised of mitre-joints which cover the 4 corners of 'Chang-aelgool' and mainly used in building annex and pavillion buildings during the early period of the Chosun dynasty. Type III was widely used during the early and middle period of the Chosun dynasty and drastically dropped in number during the late period of the dynasty. Type IV is comprised of mitre-joint of the upper-half, tenon-jointing of the lower-half and widely used in annex and pavillion building during the late period of the Chosun dynasty. Third, the form of 'Chang-aelgool' has changed from rectangular form with longer width during the early period of Chosun dynasty to square form during the middle period and eventually ended up as a rectangular form with longer height during the late period of the dynasty. Fourth, it is considered that while mullion which is located in the center of 'Chang-aelgool' was mainly used around the main floored room during the early period of the Chosun dynasty, became commonly used in main floored room and 'ondol' rooms during the middle period and drastically dropped in number from then and ended up being not in use after the mid 18th century.

Spectroscopic Imaging at 1.0Tesla MR Unit (1.0Tesla 자기공명 영상장치에서의 분광영상기법에 관한 연구)

  • Yi, Y.;Ryu, T.H.;Oh, C.H.;Ahn, C.B.;Lee, H.K.;Cho, Z.H.
    • Proceedings of the KOSOMBE Conference
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    • v.1997 no.11
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    • pp.517-527
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    • 1997
  • Magnetic Resonance Spectroscopic Imaging is a methodology combining the imaging and spectroscopy. It can provide the spectrum of each areas of image so that one can easily compare the spectrum of one position to another position of the image. In this study, we developed pulse sequence or the spectroscopic imaging method, RF wave forms or the saturation of water signal, computer simulations to validate our method, and confirmed the methodology with phantom experiment. Then we applied the spectroscopic method to human subject and identified a few important metabolites in in vivo. To develope a water saturating RF waveform, we used Shinnar-Le-Roux algorithm and obtained maximum phase RF waveform. With this RF pulse, it could suppress the water signal to 1:1000. The magnet is shimmed to under 1.0ppm with auto-shimming technique. The saturation bandwidth is 80Hz(2ppm). The water and fat seperation is 3.3ppm(about 140Hz at 1 Tesla magnet), the bandwidth is enough to resolve the difference. But we are more concerned about the narrow window in between the two peaks, in which the small quantity of metabolites reside. We performed the computer simulation and phantom experiments in 8*8 matrix form and showed good agreement in the image and spectrum. Finally we applied spectroscopic imaging to the brain of human subject. Only the lipid signal was shown in the periphery region which agrees with the at distribution in human head surface area. The spectrum inside the brain shows the important metabolites such as NAA, Cr/PCr, Choline. We here have shown the spectroscopic imaging which is normally done above 1.5 Tesla machine can be performed in the 1 Tesla Magnetic Resonance Imaging Unit.

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Development of Digital Signage System for Remote Video Advertisement in OSGi Service Platform (OSGi 서비스 플랫폼에서 원격 영상광고 송출 디지털 사이니지 시스템 개발)

  • Chung, Kyung Yong;Jeong, In Jae;Lee, Young Sil
    • Journal of the Institute of Convergence Signal Processing
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    • v.20 no.4
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    • pp.232-237
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    • 2019
  • It has recently been combined with advanced technologies such as AR and VR, and its application range is expanding to various forms of smart signage. However, until now, digital signage service that reaches us is installed in many floating populations such as bus stops, elevators, and banks and is used in the form of providing news, weather, and advertisements. In addition, large companies, government offices, and outdoor advertising companies occupy the market. The use of such services in small and medium-sized businesses and small retail stores is costly and expensive to manage. Also, it is difficult to generalize the market because services and solutions are being deployed in the market in the form of top-down. Therefore, in this paper, we proposed a digital signage system for transmitting a remote video advertisement that uses a show window in front of the store as a beam project screen for small retail stores, and can remotely set and manage and update it in OSGi service platform.

Construction of Embedded Data Synchronization Gateway (임베디드 자료동기화 게이트웨이 구축)

  • Park, Ju-Geon;Park, Kee-Hyun;Woo, Jong-Jung
    • Journal of the Korea Institute of Information and Communication Engineering
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    • v.14 no.2
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    • pp.335-342
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    • 2010
  • Nowadays, the major manufacturer of the mobile devices has offered its own solution for the data synchronization. But each manufacturer uses its proprietary data synchronization method so that the compatibility of data can not be guaranteed. To solve such problems, a gateway is needed to convert different forms of data into a unified form of data and vice versa. Some problems have been found in the experiments with the previously implemented gateway. First, a bottleneck state might arise if a number of mobile devices request data synchronization simultaneously. Second, the gateway itself would become a serious vulnerable point to an attack during the process of converting received data. The proposed gateway can solve this bottleneck state and security issue since it converts data and processes synchronization request in a mobile device. In this paper, the proposed gateway is constructed and the results of some experiments with the gateway are presented. According to the results, the proposed gateway operates properly and it is relatively insensitive to the bottleneck state.

Effects of CdCl2 Heat Treatment on the Qualities of CdS Thin Films Deposited by RF Magnetron Sputtering Technique (RF 마그네트론 스퍼터링법으로 증착된 CdS 박막의 CdCl2 열처리 효과)

  • Choi, Su-Young;Chun, Seung-Ju;Jung, Young-Hun;Lee, Seung-Hun;Bae, Soo-Hyun;Tark, Sung-Ju;Kim, Ji-Hyun;Kim, Dong-Hwan
    • Korean Journal of Materials Research
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    • v.21 no.9
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    • pp.497-501
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    • 2011
  • The CdS thin film used as a window layer in the CdTe thin film solar cell transports photo-generated electrons to the front contact and forms a p-n junction with the CdTe layer. This is why the electrical, optical, and surface properties of the CdS thin film influence the efficiency of the CdTe thin film solar cell. When CdTe thin film solar cells are fabricated, a heat treatment is done to improve the qualities of the CdS thin films. Of the many types of heat treatments, the $CdCl_2$ heat treatment is most widely used because the grain size in CdS thin films increases and interdiffusion between the CdS and the CdTe layer is prevented by the heat treatment. To investigate the changes in the electrical, optical, and surface properties and the crystallinity of the CdS thin films due to heat treatment, CdS thin films were deposited on FTO/glass substrates by the rf magnetron sputtering technique, and then a $CdCl_2$ heat treatment was carried out. After the $CdCl_2$ heat treatment, the clustershaped grains in the CdS thin film increased in size and their boundaries became faint. XRD results show that the crystallinity improved and the crystalline size increased from 15 to 42 nm. The resistivity of the CdS single layer decreased from 3.87 to 0.26 ${\Omega}cm$, and the transmittance in the visible region increased from 64% to 74%.

Form-Focused Instruction, Learners' Perceptions, and Second Language Acquisition (형태초점교수활동, 학습자의 인식도, 그리고 제2언어습득)

  • Hwang, Hee Jeong
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.16 no.10
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    • pp.6475-6482
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    • 2015
  • The purpose of the study was two folded: to examine whether form-focused instruction (FFI) with corrective feedback (CF) is effective for the acquisition of the target linguistic forms and to find out the extent to which of the students' perceptions as well as their attitudes towards English instruction that they received. Tests and questionnaires were implemented to 122 Korean EFL students from eight classes enrolled in an English communication course. They were randomly assigned to three groups: the input-based group, who received typographical input enhancement materials, so-called the TIE group, the output-based group, who performed dictogloss tasks, so-called the DICT group, and the control group (CG). The data analysis was made on both tests and questionnaires by using SPSS 21.0 for Windows. The study found that different types of FFI with CF contributed to the improvement of students' grammatical knowledge and both the TIE and DICT task group students positively changed their perceptions and understanding as well as their attitudes towards the English instruction given, and students in all groups preferred pair work activities. In addition, most of the TIE and DICT students showed their interest and satisfaction with English class, whereas the CG group students did not. Based on the findings, this study suggested that well-planned and properly-chosen FFI in the form of pair work activities should be applied in classrooms with consideration of students' instructional preference in Korean EFL contextual settings.

Development of a Seismic Measurement System with a reference for the Reduction of Artificial Noise (인공잡음 제거를 위한 기준점 이용 탄성파 측정시스템 개발)

  • Hwang, Hak-Soo;Lee, Tai-Sup;Sung, Nak-Hoon
    • Geophysics and Geophysical Exploration
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    • v.2 no.4
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    • pp.180-183
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    • 1999
  • A proto-type seismic measurement system with a reference was developed to improve S/N (signal-to-noise ratio) of seismic data, especially in noisy urban areas. Two pairs of correlation measurements (the one for microphone and geophone, and another for electromagnetic (EM) loop and geophone) were carried out near Kimpo Airport and at Kimje. The spectrum analyses were also performed to investigate the correlation of two pairs of time series; one for microphone and geophone, and another for EM loop and geophone. The sound waves measured with the microphone and the geophone are highly correlated. However, differences in the reponses are readily identifiable across 200 Hz; in the vicinity of 100 Hz, the spectral energy for geophone is 20 dB higher than that for microphone, and at near 500 Hz, the spectral energy for microphone is 30 dB higher than that for geophone. Overall, the spectral energy appears concentrated on the frequency window below 600 Hz for geophone. It contrasts with the observation of dominant frequency at the range of above 200 Hz for microphone. The wave forms of EM noise (due to an ACDC inverter) measured with EM loop and geophone are consistently and highly correlated each other. The power spectrum of the EM noise for EM loop shows that the spectral energies at odd harmonic frequencies of 60 Hz are higher than those at even harmonic frequencies of 60 Hz. It is compared to the power spectrum for geophone; the spectral energies at odd harmonics are nearly same as those at even harmonic frequencies.

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A Study on the Application or Fashion Illustration for the VMD Plan - Focusing on POP Advertisement - (VMD 방안으로서 패션 일러스트레이션 활용에 관한 연구 - POP 광고를 중심으로 -)

  • 김정민;김순자
    • The Research Journal of the Costume Culture
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    • v.12 no.4
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    • pp.648-662
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    • 2004
  • These days fashion market is overflown with many brands and their identities are not so clear that the advertisement emphasizing the characteristics of the products don't seem to be adequate in appealing the customers. Therefore it is required that the sensible image advertisement which appeals to the customers by stimulating their feeling and sensitivity to attract customer's interest. At that point, VMD especially of POP advertisement that can be attract direct purchasing plays an important part to build up the accurate image of brand to consumers. Even thought today's individualized consumers take much interested in the fresh and original expressions, the visual expressions of fashion advertisements still focus on using photographs. The most advertisement of photograph has a limit that it shows only an immediate fraction, so it can't present whole image It can deliver more- imaginations and message than photograph if fashion illustration is used in advertisement. Therefore the purpose of this study was to present the application of fashion illustration for the POP advertisement Twelve pieces of fashion illustrations were produced and classified three parts according to their images and expression techniques. Paper sculpture techniques were applied for fashion image expression, for paper is easily meet daily life and ecological materials. For study procedure and contents, the concept and useful functions of fashion illustration and the concept of paper sculpture were examined as a theoretical background, and various uses and techniques of paper sculpture by analysing a number of paper sculpture art works were also studied. Also the concept, roles and functions of POP advertisement were discussed, and then the examples that the fashion illustration applied in the advertisement were analyzed through case study. The theme of my works was jean fashion brand whose brand image is significant, Twelve pieces of fashion illustrations using paper sculpture techniques were produced and various kinds of paper were used in expressing the paper sculpture technique. Each works were cut out the forms and used a pertinent light for making cubic effect shadow when displayed them. In my works Ⅰand Ⅱ, Ⅰ illustrated jeans in two images of sexy and casual, these were created slightly bigger than actual body size in order to attract consumer's gaze at show window or store. In my works Ⅲ, Ⅰ illustrated part or model of a jean product so that it could be used as addition to main display.

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