• 한국응용약물학회:학술대회논문집
• /
• 한국응용약물학회 1997년도 추계학술대회
• /
• pp.47-50
• /
• 1997

Drug development began with the finding of biologically active compounds which are obtained by chemical synthesis or from natural sources. The advent of Combinatorial Chemistry is recognized as a strategy which has a potential to change the methodology of research and development(R&D) of new drugs. Drug development has been carried out with diverse strategies. In the past several decades a variety of new methodology have been introduced in R&D. Random screening of accumulated synthetic samples which had been synthesized for development of other drugs led to the discovery of new drugs. The typical examples are anti-asthma drug trimethoquinol and calcium antagonist diltiazem. (herbesser). In particular the latter drug has been used as a calcium antagonist worldwide, however it was first synthesized to find new tranquilizer and this is the reason why diltiazem has benzodiazepam skeleton. The random screening contributed in the finding of new drugs were carried out with whole animal test and it is a standard methodology in R&D of new drugs. Aspirin is the first synthetic non-steroidal antiinflammatory drug(NSAID) and has been used for more than one hundred years. It is the first example of drug developed from natural product. Salicin is the main constituent of willow bark which had been used in Europe for a long time to treat arthritis and aspirin was developed from salicin. Most of NSAID used clinically were developed from the structure of aspirin, however it took 70 years to clarify why aspirin exhibits its antiinflammatory, analgesic and antipyretic activities. The target of aspirin is cyclooxygenase(COX)which is the first enzyme involved in arachidonate cascade leading to the production of prostaglandins(PG) and thromboxan(TX). Side effect of aspirin causing ulcer in stomach is rather serious problem, since aspirin is so popular drug easily obtained in drug store(OTP). This problem is now going to be solved by a new finding on COX, which have two different types, one is constitutionally expressed COX 1 in almost all organs and the other is inducible COX 2. COX 2 is the responsible enzyme in inflammation etc and now the search of COX 2 specific inhibitors is the target of R&D of next generation NSAID.

• Journal of Microbiology and Biotechnology
• /
• 제16권12호
• /
• pp.1968-1976
• /
• 2006

Recombinant E. coli ACV 1003 (recA:: lacZ) was used to measure low concentrations of DNA-damaging chemicals, which produce $\beta$-galactosidase via an SOS regulon system. Very low $\beta$-galactosidase activities of less than 0.01 unit/ml, $\beta$-galactosidase produced through an SOS response corresponding to the 10 ng/ml (ppb) of DNA damaging chemicals in the environment, can be rapidly determined by using an alternative interferometric biosensor with optically flat thin films of porous silicon rather than by the conventional time-consuming Miller's enzyme assay as well as the ELISA method. fu order to enhance the sensitivity in the interferometry, it needs to obtain more uniform distribution and higher biolinking efficiency, whereas interferometric sensing is rapid, cheap, and advantageous in high throughput by using a multiple-well-type chip. In this study, pore size adjusted to 60 nm for the target enzyme $\beta$-galactosidase to be bound on both walls of a Si pore and a calyx crown derivative was apllied as a more efficient biolinker. Furthermore, anti-$\beta$-galactosidase was previously functionalized with the biolinker for the target $\beta$-galactosidase to be specifically bound. When anti-$\beta$-galactosidase was bound to the calyx-crown derivative-linked surface, the effective optical thickness was found to be three times as high as that obtained without using anti-$\beta$-galactosidase. The resolution obtained was very similar to that afforded by the time-consuming ELISA method; however, the reproducibility was still unsatisfactory, below 1 unit $\beta$-galactosidase/ml, owing to the microscopic non-uniform distribution of the pores in the etched silicon surface.

• 대한전자공학회논문지TC
• /
• 제48권11호
• /
• pp.60-66
• /
• 2011

LTE는 다양한 서비스 클래스를 가지고 QoS를 지원한다. 각각의 트래픽 클래스에 대해 BER 요구사항이 크게 다르다. 이는 다양한 클래스의 트래픽에 대해 전송 전력이 상이함을 의미한다. 본 논문에서는 우선순위와 목표 BER을 고려하여 서비스 클래스를 지원하는 새로운 LTE를 위한 스케줄러를 제안한다. CQI와 QCI에 의해 각 사용자당 크래픽 클래스에 대한 목표 BER로 부터 최소 전송 전력이 할당된다. 따라서 사용자의 과거 사용 전송율과 트래픽의 우선순위와 같은 다른 정보를 이용하여 점유 채널의 확률이 결정된다. 서비스 클래스 스케줄링의 시뮬레이션 결과는 최대전송율 및 비례균일과 비교될 것이다. 실험결과는 서비스 클래스 기반의 스케줄링이 전체 시스템 수율을 개선할 수 있음을 보여주고 있다.

• Molecules and Cells
• /
• 제40권8호
• /
• pp.587-597
• /
• 2017

MicroRNAs (miRNAs) are essential small RNA molecules that regulate the expression of target mRNAs in plants and animals. Here, we aimed to identify miRNAs and their putative targets in Hibiscus syriacus, the national flower of South Korea. We employed high-throughput sequencing of small RNAs obtained from four different tissues (i.e., leaf, root, flower, and ovary) and identified 33 conserved and 30 novel miRNA families, many of which showed differential tissuespecific expressions. In addition, we computationally predicted novel targets of miRNAs and validated some of them using 5' rapid amplification of cDNA ends analysis. One of the validated novel targets of miR477 was a terpene synthase, the primary gene involved in the formation of disease-resistant terpene metabolites such as sterols and phytoalexins. In addition, a predicted target of conserved miRNAs, miR396, is SHORT VEGETATIVE PHASE, which is involved in flower initiation and is duplicated in H. syriacus. Collectively, this study provides the first reliable draft of the H. syriacus miRNA transcriptome that should constitute a basis for understanding the biological roles of miRNAs in H. syriacus.

• 한국음향학회지
• /
• 제26권2호
• /
• pp.87-94
• /
• 2007

LFM 신호를 이용한 능동소나 신호처리에서는 Split-beam을 이용한 좌우 두 빔 사이의 상호상관관계를 측정함으로써 표적의 자세각과 길이 정보를 추정할 수 있다. 그러나 탐지된 원거리 표적의 정보를 추정하기 위해서는 고분해능의 방위각 및 거리 해상도가 요구된다. 이를 위해 나이키스트(Nyquist) 샘플링 주파수보다 높은 샘플링 주파수가 필요하므로, 일반적으로 보간기법을 이용하여 과도샘플링(over-sampling) 을 해야 한다. 하지만 과도 샘플링된 좌우 빔신호를 이용하여 상호상관관계를 구할 경우, 요구되는 연산량과 메모리 용량이 일반적으로 상용 DSP 프로세서들의 처리용량과 내부 메모리 용량을 초과하게 되어 DSP를 이용한 실시간 구현이 어렵게 된다. 본 논문에서는 이러한 문제를 해결하기 위해 누적처리기법을 이용한 Split-beam처리 방법을 제안하였다. 제안한 기법의 성능을 모의실험을 통하여 검증하고, ADSP-TS101을 사용하여 실시간 시스템으로 구현하였다.

• 대한기계학회논문집B
• /
• 제36권10호
• /
• pp.1011-1017
• /
• 2012

본 논문에서는 롤타입 마스크를 사용한 마이크로/나노 구조 제작용 광학 리소그래피 방법을 소개한다. 이 생산 방법은 다양한 목표 해상도에 따라 위상지연 리소그래피방법과 포토리소그래피로 나뉜다. 사용되는 빛의 파장대보다 작은 해상도를 갖는 패턴을 제작하기 위해서 실린더 형태의 위상지연 마스크를 활용한 근거리 노광 방식을 사용한다. 또한 필름 형태의 금속 마스크를 써서 포토리소그래피를 연속방식으로 수행하였는데 이 방식은 실린더 마스크의 회전수를 조절함으로써 노광 결과 패턴의 주기를 실시간으로 조절할 수 있다. 이 기술의 응용으로 금속 그물패턴으로 만들어진 100 $mm^2$ 넓이의 투명전극을 제작하였다.

• KSII Transactions on Internet and Information Systems (TIIS)
• /
• 제4권3호
• /
• pp.205-223
• /
• 2010

In this paper, we analyze the impact of different frame types on self-similarity and burstiness characteristics of the aggregated frame traffic from a real 802.11 wireless local area network. We find that characteristics of aggregated frame traffic are affected by both mean frame size and the proportion of specified frame types. Based on this new knowledge, an adaptative frame size optimization (AFSO) mechanism is proposed to improve the transmission efficiency by adaptively adjusting data frame size according to the proportions of different frame types. Simulation results show that our proposed mechanism can effectively regulate the burstiness of aggregated frame traffic and improve the successful delivery rate of data frames when a fixed throughput target is set for 802.11 wireless networks.

• The Plant Pathology Journal
• /
• 제24권3호
• /
• pp.245-268
• /
• 2008

The outcome of plant-pathogen interactions is influenced significantly by endogenous small molecules that coordinate plant defence responses. There is currently tremendous scientific and commercial interest in identifying chemicals whose exogenous application activates plant defences and affords protection from pathogen infection. In this review, we provide a survey of compounds known to induce disease resistance in plants, with particular emphasis on how each compound was originally identified, its putative or demonstrated mechanism of defence induction, and the known biological target(s) of each chemical. Larger polymeric structures and peptides/proteins are also discussed in this context. The quest for novel defence-inducing molecules would be aided by the capability for high-throughput analysis of candidate compounds, and we describe some issues associated with the development of these types of screens. Subsequent characterization of hits can be a formidable challenge, especially in terms of identifying chemical targets in plant cells. A variety of powerful molecular tools are available for this characterization, not only to provide insight into methods of plant defence activation, but also to probe fundamental biological processes. Furthermore, these investigations can reveal molecules with significant commercial potential as crop protectants, although a number of factors must be considered for this potential to be realized. By highlighting recent progress in the application of chemical biology techniques for the modulation of plant-pathogen interactions, we provide some perspective on the exciting opportunities for future progress in this field of research.

• Toxicological Research
• /
• 제22권1호
• /
• pp.15-22
• /
• 2006

Many of endocrine disrupting chemicals induce effects via interaction with hormone receptors and responsive elements in target cells. We investigated endocrine disrupting effects of some food additives and contaminants including BHA, BHT, ethoxyquin, propionic acid, sorbic acid, benzoic acid, CPM, aflatoxin B1, cadmium chloride, genistein, TCDD and PCBs in yeast transformants expressing human steroid hormone receptors along with steroid responsive elements. The response limit of genetically recombinant yeast to $17{\beta}$-estradiol, testosterone and progesterone was $1{\times}10^{-16},\;1{\times}10^{-12}\;and\;1{\times}10^{-13}M$, respectively. BHT induced weak transcriptional activity in estrogen sensitive yeast, while BHA and sorbic acid interacted weakly with androgen receptor/responsive element. CPM induced transcriptional activities in all types of yeasts sensitive to steroid hormones. Zearalenone and genistein induced high transcriptional activation in estrogen sensitive yeast with relative potencies almost $10^8$ folds lower than $17{\beta}$-estradiol. TCDD induced transcriptional activation weakly in estrogen- and progesterone- sensitive yeasts. This study elucidated that recombinant yeast is a sensitive and high-throughput system and can be used for the direct assessment on chemical interactions with steroid receptors and responsive elements. Also, the present study raises the requirement of evaluation on the endocrine disrupting effects of BHT, BHA, sorbic acid, CPM and TCDD for their transcription activity in yeast screening system though weak in intensity.

• Asian Pacific Journal of Cancer Prevention
• /
• 제17권7호
• /
• pp.3025-3033
• /
• 2016

Chronic myeloid leukaemia (CML) is a clonal myeloproliferative hematopoietic stem cell disorder. Deregulated BCR-ABL fusion tyrosine kinase activity is the main cause of CML disease pathogenesis, making BCR-ABL an ideal target for inhibition. Current tyrosine kinase inhibitors (TKIs) designed to inhibit BCR-ABL oncoprotein activity, have completely transformed the prognosis of CML. Interruption of TKI treatment leads to minimal residual disease reside (MRD), thought to reside in TKI-insensitive leukaemia stem cells which remain a potential reservoir for disease relapse. This highlights the need to develop new therapeutic strategies for CML either as small molecule master TKIs or phytopharmaceuticals derived from nature to achieve chronic molecular remission. This review outlines the past, present and future therapeutic approaches for CML including coverage of relevant mechanisms, whether ABL dependent or independent, and epigenetic factors responsible for developing resistance against TKIs. Appearance of mutant clones along the course of therapy either pre-existing or induced due to therapy is still a challenge for the clinician. A proposed in-vitro model of generating colony forming units from CML stem cells derived from diagnostic samples seems to be achievable in the era of high throughput technology which can take care of single cell genomic profiling.