• 제목/요약/키워드: Novel target

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Target Identification: A Challenging Step in Forward Chemical Genetics

  • Das, Raj Kumar;Samanta, Animesh;Ghosh, Krishnakanta;Zhai, Duanting;Xu, Wang;Su, Dongdong;Leong, Cheryl;Chang, Young-Tae
    • Interdisciplinary Bio Central
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    • 제3권1호
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    • pp.3.1-3.16
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    • 2011
  • Investigation of the genetic functions in complex biological systems is a challenging step in recent year. Hence, several valuable and interesting research projects have been developed with novel ideas to find out the unknown functions of genes or proteins. To validate the applicability of their novel ideas, various approaches are built up. To date, the most promising and commonly used approach for discovering the target proteins from biological system using small molecule is well known a forward chemical genetics which is considered to be more convenient than the classical genetics. Although, the forward chemical genetics consists of the three basic components, the target identification is the most challenging step to chemical biology researchers. Hence, the diverse target identification methods have been developed and adopted to disclose the small molecule bound protein. Herein, in this review, we briefly described the first two parts chemical toolbox and screening, and then the target identifications in forward chemical genetics are thoroughly described along with the illustrative real example case study. In the tabular form, the different biological active small molecules which are the successful examples of target identifications are accounted in this research review.

Maneuvering Target Tracking with the Modified VDIE Filter

  • Ahn, Byeong-Wan;Whang, Tae-Hyun;Choi, Jae-Won;Song, Taek-Lyul
    • 제어로봇시스템학회:학술대회논문집
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    • 제어로봇시스템학회 2001년도 ICCAS
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    • pp.53.6-53
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    • 2001
  • In this paper, we are concerned with a tracking filter algorithm which can track a maneuvering target. Among the novel tracking filter algorithms, the input estimation (IE) filter can be summarized as estimating the unknown maneuver input and compensating the state according to the estimated input, and the variable dimension filter (VDF) can be summarized as detecting the maneuver of target and changing the dimension of the target dynamics to accomodate the maneuver of target They have some goods and bads with respect to each other. The variable dimension filter with input estimation (VDIEF) is constructed by combining the two filtering algorithms. However, it requires too much computational burden while it has good performance. We propose another variable dimension with input estimation ...

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5-(Heteroaryl)isoxazole계 화합물의 합성 및 항균 활성 (Synthesis and Antibacterial Activity of Novel 5-(heteroaryl)isoxazole Derivatives)

  • RamaRao, R. Janaki;Rao, A.K.S. Bhujanga;Sreenivas, N.;Kumar, B. Suneel;Murthy, Y. L. N.
    • 대한화학회지
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    • 제55권2호
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    • pp.243-250
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    • 2011
  • Isoxazole계 화합물을 합성하고 항균활성연구를 수행하였다. 3-Di(alkylamino)acryloalkanones을 hydroxylamine hydrochloride 또는 hydroxylamine-O-sulphonic acid와 반응시켜서 target isoxazole계 화합물을 합성하였다.

Antimicrobial Agents That Inhibit the Outer Membrane Assembly Machines of Gram-Negative Bacteria

  • Choi, Umji;Lee, Chang-Ro
    • Journal of Microbiology and Biotechnology
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    • 제29권1호
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    • pp.1-10
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    • 2019
  • Gram-negative pathogens, such as Klebsiella pneumoniae, Pseudomonas aeruginosa, and Acinetobacter baumannii, pose a serious threat to public health worldwide, due to high rates of antibiotic resistance and the lack of development of novel antimicrobial agents targeting Gram-negative bacteria. The outer membrane (OM) of Gram-negative bacteria is a unique architecture that acts as a potent permeability barrier against toxic molecules, such as antibiotics. The OM is composed of phospholipids, lipopolysaccharide (LPS), outer membrane ${\beta}-barrel$ proteins (OMP), and lipoproteins. These components are synthesized in the cytoplasm or in the inner membrane, and are then selectively transported to the OM by the specific transport machines, including the Lol, BAM, and Lpt pathways. In this review, we summarize recent studies on the assembly systems of OM components and analyze studies for the development of inhibitors that target these systems. These analyses show that OM assembly machines have the potential to be a novel attractive drug target of Gram-negative bacteria.

Development of Frequency Discriminated Simulative Target Generator Based on DRFM for Radar System Performance Evaluation

  • Chung, Myung-Soo;Kim, Woo-Sung;Bae, Chang-Ok;Kang, Seung-Min;Park, Dong-Chul
    • Journal of electromagnetic engineering and science
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    • 제11권3호
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    • pp.213-219
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    • 2011
  • Simulative target generators are needed for testing and calibrating various radar systems. The generator in this study discriminates the transmitting frequency from a radar and simulates parameters like target range, range rate, and atmospheric attenuation using the digital RF memory technique. The simulative target echo is then sent to the radar for testing and evaluation. This paper proposes a novel architecture for controlling the digital RF memory so it continually writes ADC data to the memory and reads it for the DAC with increasing one step address in order to control the delay of target range in a simple way. The target echo is programmed according to various preprogrammed scenarios and is generated in real time using a wireless local area network (LAN). To analyze the detected and generated target information easily, the system times for the radar and simulative target generator are synchronized using a global positioning system (GPS).

Molecular Mechanisms of Apoptosis and Roles in Cancer Development and Treatment

  • Goldar, Samira;Khaniani, Mahmoud Shekari;Derakhshan, Sima Mansoori;Baradaran, Behzad
    • Asian Pacific Journal of Cancer Prevention
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    • 제16권6호
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    • pp.2129-2144
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    • 2015
  • Programmed cell death (PCD) or apoptosis is a mechanism which is crucial for all multicellular organisms to control cell proliferation and maintain tissue homeostasis as well as eliminate harmful or unnecessary cells from an organism. Defects in the physiological mechanisms of apoptosis may contribute to different human diseases like cancer. Identification of the mechanisms of apoptosis and its effector proteins as well as the genes responsible for apoptosis has provided a new opportunity to discover and develop novel agents that can increase the sensitivity of cancer cells to undergo apoptosis or reset their apoptotic threshold. These novel targeted therapies include those targeting anti-apoptotic Bcl-2 family members, p53, the extrinsic pathway, FLICE-inhibitory protein (c-FLIP), inhibitor of apoptosis (IAP) proteins, and the caspases. In recent years a number of these novel agents have been assessed in preclinical and clinical trials. In this review, we introduce some of the key regulatory molecules that control the apoptotic pathways, extrinsic and intrinsic death receptors, discuss how defects in apoptotic pathways contribute to cancer, and list several agents being developed to target apoptosis.

혈관신생 분자핵의학 영상 (Molecular Nuclear imaging of Angiogenesis)

  • 이경한
    • 대한핵의학회지
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    • 제38권2호
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    • pp.171-174
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    • 2004
  • Angiogenesis, the formation of new capillaries from existing vessels, increases oxygenation and nutrient supply to ischemic tissue and allows tumor growth and metastasis. As such, angiogenesis targeting provides a novel approach for cancer treatment with easier drug delivery and less drug resistance. Therapeutic anti-angiogenesis has shown impressive effects in animal tumor models and are now entering clinical trials. However, the successful clinical introduction of this new therapeutic approach requires diagnostic tools that can reliably measure angiogenesis in a noninvasive and repetitive manner. Molecular imaging is emerging as an exciting new discipline that deals with imaging of disease on a cellular or genetic level. Angiogenesis imaging is an important area for molecular imaging research, and the use of radiotracers offers a particularly promising technique for its development. While current perfusion and metabolism radiotracers can provide useful information related to tissue vascularity, recent endeavors are focused on the development of novel radioprobes that specifically and directly target angiogenic vessels. Presently available proges include RGD sequence containing peptides that target ${\alpha}_v\;{\beta}_3$ integrin, endothelial growth factors such as VEGF or FGF, metalloptoteinase inhibitors, and specific antiangiogenic drugs. It is now clear that nuclear medicine techniques have a remarkable potential for angiogenesis imaging, and efforts are currently continuing to develop new radioprobes with superior imaging properties. With future identification of novel targets, design of better probes, and improvements in instrumentation, radiotracer angiogenesis imaging promises to play an increasingly important role in the diagnostic evaluation and treatment of cancer and other angiogenesis related diseases.

Determination of nickel and cadmium in fish, canned tuna, black tea, and human urine samples after extraction by a novel quinoline thioacetamide functionalized magnetite/graphene oxide nanocomposite

  • Naghibzadeh, Leila;Manoochehri, Mahboobeh
    • Carbon letters
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    • 제26권
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    • pp.43-50
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    • 2018
  • In this research, a novel and efficient quinoline thioacetamide functionalized magnetic graphene oxide composite ($GO@Fe_3O_4@QTA$) was synthesized and utilized for dispersive magnetic solid phase preconcentration of Cd(II) and Ni(II) ions in urine and various food samples. A number of diverse methods were employed for characterization of the new nanosorbent. The design of experiments approach and response surface methodology were applied to monitor and find the parameters that affect the extraction performance. After sorption and elution steps, the concentrations of target analytes were measured by employing FAAS. The highest extraction performance was achieved under the following experimental conditions: pH, 5.8; sorption time, 6.0 min; $GO@Fe_3O_4@QTA$ amount, 17 mg; 2.4 mL $1.1mol\;L^{-l}$ $HNO_3$ solution as the eluent and elution time, 13.0 min. The detection limit is 0.02 and $0.2ng\;mL^{-1}$ for Cd(II), and Ni(II) ions, respectively. The accuracy of the new method was investigated by analyzing two certified reference materials (sea food mix, Seronorm LOT NO 2525 urine powder). The interfering study revealed that there are no interferences from commonly occurring ions on the extractability of target ions. Finally, the new method was satisfactorily employed for rapid extraction and determination of target ions in urine and various food samples.

온도 보상을 이용한 자기변형 위치 센서의 정확도 향상 방법 (A Novel Method for Improving the Positioning Accuracy of a Magnetostrictive Position Sensor Using Temperature Compensation)

  • 유은주;박영우;노명규
    • 센서학회지
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    • 제28권6호
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    • pp.414-419
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    • 2019
  • An ultrasonic based magnetostrictive position sensor (MPS) provides an indication of real target position. It determines the real target position by multiplying the propagation speed of ultrasonic wave and the time-of-flight between the receiving signals; one is the initial signal by an excitation current and the other is the reflection signal by the ultrasonic wave. The propagation speed of the ultrasonic wave depends on the temperature of the waveguide. Hence, the change of the propagation speed in various environments is a critical factor in terms of the positioning accuracy in the MPS. This means that the influence of the changes in the waveguide temperature needs to be compensated. In this paper, we presents a novel way to improve the positioning accuracy of MPSs using temperature compensation for waveguide. The proposed method used the inherent measurement blind area for the structure of the MPS, which can simultaneously measure the position of the moving target and the temperature of the waveguide without any additional devices. The average positional error was approximately -23.9 mm and -1.9 mm before and after compensation, respectively. It was confirmed that the positioning accuracy was improved by approximately 93%.

Identification and Function Prediction of Novel MicroRNAs in Laoshan Dairy Goats

  • Ji, Zhibin;Wang, Guizhi;Zhang, Chunlan;Xie, Zhijing;Liu, Zhaohua;Wang, Jianmin
    • Asian-Australasian Journal of Animal Sciences
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    • 제26권3호
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    • pp.309-315
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    • 2013
  • MicroRNAs are a class of endogenous small RNAs that play important roles in post-transcriptional gene regulation by directing degradation of mRNAs or facilitating repression of target gene translation. In this study, three small RNA cDNA libraries from the mammary gland tissues of Laoshan dairy goats (Capra hircus) were constructed and sequenced, individually. Through Solexa high-throughput sequencing and bioinformatics analysis, we obtained 50 presumptive novel miRNAs candidates, and 55,448 putative target genes were predicted. GO annotations and KEGG pathway analyses showed the majority of target genes were involved in various biological processes and metabolic pathways. Our results discovered more information about the regulation network between miRNAs and mRNAs and paved a foundation for the molecular genetics of mammary gland development in goats.