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A Novel Suberoylanilide Hydroxamic Acid Histone Deacetylase Inhibitor Derivative, N25, Exhibiting Improved Antitumor Activity in both Human U251 and H460 Cells

  • Zhang, Song;Huang, Wei-Bin;Wu, Li;Wang, Lai-You;Ye, Lian-Bao;Feng, Bing-Hong
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.10
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    • pp.4331-4338
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    • 2014
  • $N^1$-(2, 5-dimethoxyphenyl)-$N^8$-hydroxyoctanediamide (N25) is a novel SAHA cap derivative of HDACi, with a patent (No. CN 103159646). This invention is a hydroxamic acid compound with a structural formula of $RNHCO(CH_2)6CONHOH$ (wherein R=2, 5dimethoxyaniline), a pharmaceutically acceptable salt which is soluble. In the present study, we investigated the effects of N25 with regard to drug distribution and molecular docking, and anti-proliferation, apoptosis, cell cycling, and $LD_{50}$. First, we designed a molecular approach for modeling selected SAHA derivatives based on available structural information regarding human HDAC8 in complex with SAHA (PDB code 1T69). N25 was found to be stabilized by direct interaction with the HDAC8. Anti-proliferative activity was observed in human glioma U251, U87, T98G cells and human lung cancer H460, A549, H1299 cells at moderate concentrations ($0.5-30{\mu}M$). Compared with SAHA, N25 displayed an increased antitumor activity in U251 and H460 cells. We further analyzed cell death mechanisms activated by N25 in U251 and H460 cells. N25 significantly increased acetylation of Histone 3 and inhibited HDAC4. On RT-PCR analysis, N25 increased the mRNA levels of p21, however, decreased the levels of p53. These resulted in promotion of apoptosis, inducing G0/G1 arrest in U251 cells and G2/M arrest in H460 cells in a time-dependent and dose-dependent manner. In addition, N25 was able to distribute to brain tissue through the blood-brain barrier of mice ($LD_{50}$: 240.840mg/kg). In conclusion, our findings demonstrate that N25 will provide an invaluable tool to investigate the molecular mechanism with potential chemotherapeutic value in several malignancies, especially human glioma.

Activation Factors of Industry Cooperation through Comparison Study on Domestic and International Industry Cooperation Programs (국내외 산학협력프로그램 비교를 통한 산학협력 활성화 방안 연구)

  • Kim, Hye Sun;Kim, Jong Boo;Kim, Hyoung Ro
    • Asia-Pacific Journal of Business Venturing and Entrepreneurship
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    • v.9 no.2
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    • pp.187-200
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    • 2014
  • Industry Cooperation is not the choice of national development but the inevitable component in the world. Industry cooperation results of the reconstruction of the country is an important place as an essential element of the economic development of the national policy in the major economies. Despite several changes in the international economic environment, United States, Canada, Finland, Sweden, Israel settled and maintaining the sustainable development of the countries which successfully established Industry-University Cooperation or Industry-Acaemy Cooperation system in history. In this study, delivered to the realistic ways of Industry cooperation through comparison study on domestic and international cooperation programs. The new activation programs of industry academic cooperation are delivered, that is, The bonus payments system of technology development patent and free technology transfer for joint development, bonus points system and evaluation indicators for joint capacity building program which participate student, industry and academic sector, step-by-step training. system for total employment and entrepreneurship at the same time strengthening management training programs and education opportunity gives to the benefits for the community members. Finally, Intellectual property expert matching program which develops basis of technology trader and expert maps in the smallest unit by administrative area. practice the internet information search services in national wide network for this matching program and government office dedicated to staffing for technology transfer.

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Analysis of Important Indicators of TCB Using GBM (일반화가속모형을 이용한 기술신용평가 주요 지표 분석)

  • Jeon, Woo-Jeong(Michael);Seo, Young-Wook
    • The Journal of Society for e-Business Studies
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    • v.22 no.4
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    • pp.159-173
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    • 2017
  • In order to provide technical financial support to small and medium-sized venture companies based on technology, the government implemented the TCB evaluation, which is a kind of technology rating evaluation, from the Kibo and a qualified private TCB. In this paper, we briefly review the current state of TCB evaluation and available indicators related to technology evaluation accumulated in the Korea Credit Information Services (TDB), and then use indicators that have a significant effect on the technology rating score. Multiple regression techniques will be explored. And the relative importance and classification accuracy of the indicators were calculated by applying the key indicators as independent features applied to the generalized boosting model, which is a representative machine learning classifier, as the class influence and the fitness of each model. As a result of the analysis, it was analyzed that the relative importance between the two models was not significantly different. However, GBM model had more weight on the InnoBiz certification, R&D department, patent registration and venture confirmation indicators than regression model.

Current Status of Registered Korean Patents Related to the Health Functional Food for Skin Care (피부미용 관련 건강기능식품 국내 특허 등록현황)

  • Chung, Kap-Taeck;Lee, Sang-Hyun
    • The Korean Journal of Food And Nutrition
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    • v.25 no.2
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    • pp.308-316
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    • 2012
  • Proper skin care promotes good metabolism and the biological activity of skin, helps maintain the skin in a healthy and beautiful state when combined with nutritional nourishment. Health functional foods are being used for the purpose of enhancing efficient skin care. Health functional foods related to skin care maintain the epidermis, dermal fibroblast layer and subcutaneous tissue that form the skin. Efficient functional foods alleviate the signs of endogenous aging that come with getting older and exogenous aging caused by sunlight. Even though the field of skin care related to health functional foods has received less attention and been the subject of less research compared to functional cosmetics which are developing widely, this area of skin care that maintains and improves the layer of dermal fibroblast through the intake of food, is expected to progress with the commercialization of products in many fields when the related technical research development is galvanized and the related patents are applied for. Research into health functional foods related to skin care in Korea started rather late in comparison to other advanced countries where patents for relevant techniques have been applied for since 1990's together with research conducted on how they might be used for practical purposes. This study used the key words 'skin care, health functional food' to search for Korean patents that have been applied for at the Korean Intellectual Property Office from 1983 to 2011 using the KIPRIS database, in order to help researchers in the related fields by organizing the patented formulas for health functional foods for skin care which have gained attention recently. According to the number of registrations in each industry field, the total number of patents was 1,120 we screened the major patents among them, the field with the largest number was food foodstuff non-alcoholic beverage and preparation or treatment(A23L) with 135, then natural plant medicine & medical supplies and cosmetics(A61K) with 112, microorganisms or enzymes(C12N) with 63, heterocyclic compounds(C07D) with 44, horticulture or cultivation of sea weeds, forestry(A01G) 16 times, listed from the highest to the lowest number of applications. It has been revealed that food, foodstuff, non-alcoholic beverage and preparation or treatment(A23L) was the industry field where the most patents for health functional foods related to skin care were registered.

A Study about Restraint Use in Care of Patients with Psychiatric Disorders (일 정신병원에서 발생한 강박 처치에 관한 연구)

  • An, Hyo Ja;Kim, Eun Ha;Chung, Young Hae;An, Jung Sim;Cho, Won Ae;Park, Joung Hwa
    • Journal of Korean Clinical Nursing Research
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    • v.19 no.3
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    • pp.432-442
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    • 2013
  • Purpose: The purpose of this study was to describe restraint use in care of patients with psychiatric disorders in an attempt to avoid unnecessary restraint use and provide information for developing standards regarding restraint use as a therapeutic maneuver. Methods: For this descriptive study, discharge records from N National Mental Hospital in the year 2009 were reviewed by trained nurses during Dec. 24, 2010 and Mar. 31, 2011. There were 596 restrains applied on 232 of 1,322 discharges. Data collected include general characteristic of patients, the frequency of restraint use, time since admission when restraint was applied, time of the day when restraint was applied, duration of restraint application, place of occurrence, reasons for restraint use, and degree of damage to the patent. Work experience of nurses who applied restraints, number of workforce at the time of restraint, and season of the year was also identified. Descriptive statistics, Chi-square test, t-test, ANOVA, $Scheff{\grave{e}}$ and Jonckheere-Terpstra were applied using SPSS 14.0 to analyze the data. Results: There were 596 restraint uses among 232 patients. Restraints were applied most frequently on males in their 40s, patients diagnosed with schizophrenia, and patients repeating admissions more than 6 times. Restraints were frequently applied within first week following admission, between 16:00 and 20:00, and the average duration of restraint was 5 hours. There were significant differences according to diagnoses of patients in the season restraint occured, time, place of occurrence, reason for restraint, and duration of restraint. Patients with alcoholism received longer restraint application. Conclusion: In order to avoid unnecessary restraint use in patients with psychiatric disorders, nurses and other health care team members need to acknowledge a group of patients such as patients with schizophrenia and alcoholism who relatively frequently restrained or receiving longer restraint. Reasonable and careful decision need to be made when applying restraint in the care of patients with alcohol problem.

A Study on the Research Performance and Efficiency of Convergence Research Projects sponsored by National Research Council of Science & Technology : A Comparative Study of Convergence Research and General Trust Projects Using DEA (국가과학기술연구회 융합연구사업의 연구성과 효율성에 관한 연구 : DEA를 활용한 융합연구 및 일반수탁사업의 비교분석을 중심으로)

  • Yuk, Hyounggab;Kang, Jaeyeol;Pae, Kibong;Kang, Daeseok
    • Journal of the Korea Convergence Society
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    • v.11 no.3
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    • pp.211-218
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    • 2020
  • This study compared and analyzed the efficiency of the research results of the convergence research project operated by the National Science and Technology Research Council and the general research project carried out by the Government-funded research institute and proposed measures to enhance the efficiency of the operation and management of convergence research. Research data were collected from 21 government-funded research institutes through an information disclosure claim and DEA analysis was conducted for efficiency assessment. The SCI papers of convergence research showed high efficiency, and the patent registration and technology transfer sector showed high efficiency of general research projects. This indicates that convergence research projects for securing lead and original technologies are highly efficient, but their performance is low due to lack of participation by businesses in terms of the utilization of derived technologies, and more companies' participation and opportunities are needed for practical use of convergence research results. Through the analysis of efficiency of convergence research project performance, this study provided policy and guidance for R&D planning for rational investment of limited manpower and research costs. Further, future research on identifying efficiency is proposed depending on the type of technology subject to convergence research as a method for managing convergence research.

An Index Structure for Substructure Searching In Chemical Databases (화학 데이타베이스에서 부분구조 검색을 위한 인덱스 구조)

  • Lee Hwangu;Cha Jaehyuk
    • Journal of KIISE:Databases
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    • v.31 no.6
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    • pp.641-649
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    • 2004
  • The relationship between chemical structures and biological activities is researched briskly in the area of 'Medicinal Chemistry' At the base of these structure-based drug design tries, medicinal chemists search the existing drugs of similar chemical structure to target drug for the development of a new drug. Therefore, it is such necessary that an automatic system selects drug files that have a set of chemical moieties matching a user-defined query moiety. Substructure searching is the process of identifying a set of chemical moieties that match a specific query moiety. Testing for substructure searching was developed in the late 1950s. In graph theoretical terms, this problem corresponds to determining which graphs in a set are subgraph isomorphic to a specified query moiety. Testing for subgraph isomorphism has been proved, in the general case, to be an NP- complete problem. For the purpose of overcoming this difficulty, there were computational approaches. On the 1990s, a US patent has been granted on an atom-centered indexing scheme, used by the RS3 system; this has the virtue that the indexes generated can be searched by direct text comparison. This system is commercially used(http://www.acelrys.com/rs3). We define the RS3 system's drawback and present a new indexing scheme. The RS3 system treats substructure searching with substring matching by means of expressing chemical structure aspredefined strings. However, it has insufficient 'rerall' and 'precision‘ because it is impossible to index structures uniquely for same atom and same bond. To resolve this problem, we make the minimum-cost- spanning tree for one centered atom and describe a structure with paths per levels. Expressing 2D chemical structure into 1D a string has limit. Therefore, we break 2D chemical structure into 1D structure fragments. We present in this paper a new index technique to improve recall and precision surprisingly.

Influencing Factors on the Knowledge-Transfer Channel of the Korean Academics Engaged in Science and Engineering (한국 이공계 대학교수 지식이전 경로의 영향요인)

  • Kwon, Ki-Seok;Park, Mun-Su
    • Journal of Information Technology and Architecture
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    • v.9 no.3
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    • pp.287-301
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    • 2012
  • Against Nonaka's seminal work in 1999, this study aims to investigate various influencing factors on knowledge-transfer channels of Korean academics. To do this, we surveyed 20,000 Korean academics in science and engineering with regard to factors involved in their formal and informal collaborative activities with firms. In particular, we focus on the individual characteristics of the academics when the channels are changed from informal channels (e.g. consulting) to formal channels (e.g. licensing), as the codification of knowledge is important when it is spilled over. According to the results, male academics with a longer career and in the field of applied disciplines in a big laboratories are likely to join the transformation of the channels. Interestingly, application capacity as measured by the number of patent application is significantly and positively related to the participation of formal channels. In contrast, scientific capacity as measured by the number of papers is significantly and negatively, or in some case weakly, related to the participation. Finally, based on the findings, some policy implications are put forwarded.

ICT Trend Analysis Based on Research Papers and Patents (논문 및 특허 기반의 ICT 동향 분석 연구)

  • Son, Yeonbin;Kim, Solha;Choi, Yerim
    • Journal of the Korea Convergence Society
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    • v.12 no.12
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    • pp.1-18
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    • 2021
  • ICT is the main driving force of Korea's economic growth. Korea has the world's best ICT competitiveness, and several policies are being implemented to maintain it. However, for successful policy implementation, it is crucial to understand ICT trends accurately. Therefore, this study analyzes the trends of 18 core technologies in the ICT field. In particular, the degree of scientific development and commercialization by technology are investigated through research paper analysis and patent analysis, respectively. Then, the trends shown by document type are compared based on the two analysis results. As a result, artificial intelligence and virtual reality are at the stage where commercialization is actively taking place after scientific development, and at the same time, since research is being conducted, it is expected to develop continuously. On the other hand, quantum computer and implantable device are in the basic research stage. It is necessary to understand the current research status and determine the direction of future support. The results of the ICT trend analysis conducted in this study can be used as a criterion for determining the future direction of Korean policy.

Data-Driven Technology Portfolio Analysis for Commercialization of Public R&D Outcomes: Case Study of Big Data and Artificial Intelligence Fields (공공연구성과 실용화를 위한 데이터 기반의 기술 포트폴리오 분석: 빅데이터 및 인공지능 분야를 중심으로)

  • Eunji Jeon;Chae Won Lee;Jea-Tek Ryu
    • The Journal of Bigdata
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    • v.6 no.2
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    • pp.71-84
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    • 2021
  • Since small and medium-sized enterprises fell short of the securement of technological competitiveness in the field of big data and artificial intelligence (AI) field-core technologies of the Fourth Industrial Revolution, it is important to strengthen the competitiveness of the overall industry through technology commercialization. In this study, we aimed to propose a priority related to technology transfer and commercialization for practical use of public research results. We utilized public research performance information, improving missing values of 6T classification by deep learning model with an ensemble method. Then, we conducted topic modeling to derive the converging fields of big data and AI. We classified the technology fields into four different segments in the technology portfolio based on technology activity and technology efficiency, estimating the potential of technology commercialization for those fields. We proposed a priority of technology commercialization for 10 detailed technology fields that require long-term investment. Through systematic analysis, active utilization of technology, and efficient technology transfer and commercialization can be promoted.