• Title/Summary/Keyword: New drug development

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Inhibitory Effect of 4-Aryl 2-Substituted Aniline-thiazole Analogs on Growth of Human Prostate Cancer LNCap Cells

  • Baek, Seung-Hwa;Kim, Nak-Jeong;Kim, Seong-Hwan;Park, Kwang-Hwa;Jeong, Kyung-Chae;Park, Bae-Keun;Kang, Nam-Sook
    • Bulletin of the Korean Chemical Society
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    • v.33 no.1
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    • pp.111-114
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    • 2012
  • Androgen receptor (AR) is ligand-inducible nuclear hormone receptor which has been focused on key molecular target in growth and progression of prostate cancer. We synthesized a series of 4-aryl 2-substituted aniline-thiazole analogs and evaluated their anti-cancer activity in AR-dependent human prostate cancer LNCap cells. Among them, the compound 6 inhibited the tumor growth in LNCap-inoculated xenograft model.

DNA의 구조적, 기능적 특성과 이의 환경, 의료 분야에의 응용

  • Lee, Jeong-Heon;Odom, Teri;Lu, Yi
    • Proceedings of the Materials Research Society of Korea Conference
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    • 2012.05a
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    • pp.55.1-55.1
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    • 2012
  • In the first part of this talk, I will introduce an effort to use gold nanoparticles and UO22+ (uranyl) specific DNAzyme for development of highly sensitive and selective colorimetric uranyl sensors. In addition, I will discuss how DNA aptamers can be delivered by nanoparticles to cancer cell nucleus and released by ultrafast femtosecond pulsed laser for targeted cancer therapy. Finally, I will show how proteins such as streptavidin and myoglobin, or nanoparticles can be precisely aligned on DNA with nanometer resolution via backbone-modified phosphorothioate DNA and bifunctional linkers. These interesting functional and structural properties of DNA can provide new opportunities to develop dynamic DNA structures for potential use as intracellular sensors and drug delivery agents.

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Enterovirus infection in Korean children and antienteroviral potential candidate agents

  • Park, Kwi Sung;Choi, Young Jin;Park, Joon Soo
    • Clinical and Experimental Pediatrics
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    • v.55 no.10
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    • pp.359-366
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    • 2012
  • Although most enterovirus infections are not serious enough to be life threatening, several enteroviruses such as enterovirus 71 are responsible for severe, potentially life-threatening disease. The epidemic patterns of enteroviruses occur regularly during the year, but they may change due to environmental shifts induced by climate change due to global warming. Therefore, enterovirus epidemiological studies should be performed continuously as a basis for anti-viral studies. A great number of synthesized antiviral compounds that work against enteroviruses have been developed but only a few have demonstrated effectiveness in vivo. No proven effective antiviral agents are available for enterovirus disease therapy. The development of a new antiviral drug is a difficult task due to poor selective toxicity and cost. To overcome these limitations, one approach is to accelerate the availability of other existing antiviral drugs approved for antiviral effect against enteroviruses, and the other way is to screen traditional medicinal plants.

A Short Review on Human Functional Neuropeptide Y Receptors

  • Kothandan, Gugan;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.5 no.2
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    • pp.65-71
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    • 2012
  • Neuropeptide Y (NPY), a 36-amino acid polypeptide, is a member of the pancreatic polypeptide family, which consists of NPY, peptide YY (PYY) and pancreatic polypeptide (PP). The neuropeptide Y (NPY) receptors called Y receptors belongs to G-protein coupled that are involved in a variety of physiological functions such as appetite regulation, circadian rhythm and anxiety. Five receptor subtypes have been cloned in mammals (Y1, Y2, Y4, Y5, and Y6) of which four are functional. In this short review, information about the functional NYP receptors was analyzed. Sequence analyses were done between these receptors to identify the relationships between them. Phylogram was generated between these receptors to identify the close homologue between these receptors. Our sequence analyses found that Y1 and Y4 receptors are close than the other receptors. Further structure based analysis could be useful to identify subtype selective antagonists and dual antagonists targeting Y1 and Y4 receptors.

A Possible Role of Ginseng Root for Maintaining a Quality of Life in Womens

  • Yoshimura, Hiroyuki
    • Proceedings of the EASDL Conference
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    • 2010.11a
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    • pp.47-47
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    • 2010
  • Chilliness is a complaint among menopausal women in Japan, but increasing evidence indicates that young women also suffer from chilliness. However, neither diagnostic criteria nor drug therapies exist for treating chilliness. We noticed it and recently elucidated methodological issues related to identifying women with chills. Using a discriminant analysis, we demonstrated that four parameters were important determinants of chilliness. On the other hand, after repeated reports of serious adverse effects with hormone replacement therapy, much attention has been given to the development of new remedies to alleviate menopausal depressive state in women, but methods for their preclinical evaluation have not been clarified. We previously developed a procedure to predict the effect of candidate substance on the menopausal depressive-like state in female mice. Since either chilliness or mood disorder is known to disturb a quality of life in women, in this symposium, the efficacy of Korean red ginseng on chilliness in women and depressive-like state will be discussed.

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Temperature Dependency on Conformational Sampling of 12-Crown-4 by Simulated Annealing

  • Gadhe, Changdev G.;Cho, Seung Joo
    • Journal of Integrative Natural Science
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    • v.6 no.1
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    • pp.8-11
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    • 2013
  • In this manuscript, we report a protocol to determine most of the lowest energy conformations from the ensemble of conformations. 12-crown-4 was taken as study compound to get the most of energy minima conformations. Molecular dynamic (MD) simulation for 1 nanosecond (ns) was performed at 300, 500, 700, 900 and 1100 K temperature. At particular interval conformations were sampled. Then Gaussian program was used to minimize compounds using PM6 energy levels. Duplicates were removed by checking energy as well as mirror image conformations, and only unique conformations were retained for the next $6-31+G^*$ level minimization. It was observed that upto certain increment in temperature the number of unique conformations were increased, but afterword it decreased.

Protective Effect of Licorice Water Extract against Cadmium-induced Nephro-toxicity in Rats

  • Lee, Jong-Rok;Kim, Sang-Chan
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.21 no.3
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    • pp.771-775
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    • 2007
  • Licorice has been used for cure of injuries and for detoxification in East Asia. This study investigated the protective effect of licorice water extract against cadmium (CdCl$_2$, Cd)-induced nephro-toxicity in rats. To induce acute toxicity, Cd (4 mg/kg body weight) was dissolved in normal saline and then, intravenously (i.v.) injected to animals. In experiments, animals were orally administrated with vehicle or licorice water extract (50-100 mg/kg) for 3 days, exposed to a single injection of Cd after 24 h the last licorice/vehicle treatment. Licorice protected kidney injuries by Cd treatment. The number of glomeruli showing vasodilatation and thickening of Bowman's capsule was dose-dependently decreased by licorice. These results suggest that licorice might be a potent preventive protector against Cd-induced nephro-toxicity in rats.

Human Induced Pluripotent Stem Cells : Clinical Significance and Applications in Neurologic Diseases

  • Chang, Eun-Ah;Jin, Sung-Won;Nam, Myung-Hyun;Kim, Sang-Dae
    • Journal of Korean Neurosurgical Society
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    • v.62 no.5
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    • pp.493-501
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    • 2019
  • The generation of human induced pluripotent stem cells (iPSCs) from somatic cells using gene transfer opens new areas for precision medicine with personalized cell therapy and encourages the discovery of essential platforms for targeted drug development. iPSCs retain the genome of the donor, may regenerate indefinitely, and undergo differentiation into virtually any cell type of interest using a range of published protocols. There has been enormous interest among researchers regarding the application of iPSC technology to regenerative medicine and human disease modeling, in particular, modeling of neurologic diseases using patient-specific iPSCs. For instance, Parkinson's disease, Alzheimer's disease, and spinal cord injuries may be treated with iPSC therapy or replacement tissues obtained from iPSCs. In this review, we discuss the work so far on generation and characterization of iPSCs and focus on recent advances in the use of human iPSCs in clinical setting.

Regulation of post-translational modification in breast cancer treatment

  • Heo, Kyung-Sun
    • BMB Reports
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    • v.52 no.2
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    • pp.113-118
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    • 2019
  • The small ubiquitin-related modification molecule (SUMO), one of the post-translational modification molecules, is involved in a variety of cellular functions where it regulates protein activity and stability, transcription, and cell cycling. Modulation of protein SUMOylation or deSUMOylation modification has been associated with regulation of carcinogenesis in breast cancer. In the dynamic processes of SUMOylation and deSUMOylation in a variety of cancers, SUMO proteases (SENPs), reverse SUMOylation by isopeptidase activity and SENPs are mostly elevated, and are related to poor patient prognosis. Although underlying mechanisms have been suggested for how SENPs participate in breast cancer tumorigenesis, such as through regulation of target protein transactivation, cancer cell survival, cell cycle, or other post-translational modification-related machinery recruitment, the effect of SENP isoform-specific inhibitors on the progression of breast cancer have not been well evaluated. This review will introduce the functions of SENP1 and SENP2 and the underlying signaling pathways in breast cancer for use in discovery of new biomarkers for diagnosis or therapeutic targets for treatment.

Introduction of Vaccinomics to Develop Personalized Vaccines in Light of Changes in the Usage of Hantaan Virus Vaccine (Hantavax®) in Korea

  • Bae, Jong-Myon
    • Journal of Preventive Medicine and Public Health
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    • v.52 no.5
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    • pp.277-280
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    • 2019
  • The Ministry of Food and Drug Safety of Korea made an official announcement in March 2018 that the total number of inoculations of Hantaan virus vaccine ($Hantavax^{(R)}$) would change from 3 to 4. Some aspects of this decision remain controversial. Based on the characteristics of Hantaan virus (HTNV) and its role in the pathogenesis of hemorrhagic fever with renal syndrome, it might be difficult to develop an effective and safe HTNV vaccine through the isolate-inactivate-inject paradigm. With the development of high-through-put 'omics' technologies in the 21st century, vaccinomics has been introduced. While the goal of vaccinomics is to develop equations to describe and predict the immune response, it could also serve as a tool for developing new vaccine candidates and individualized approaches to vaccinology. Thus, the possibility of applying the innovative field of vaccinomics to develop a more effective and safer HTNV vaccine should be considered.