• Title/Summary/Keyword: Molecular targets

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Inhibitory effects of [6]-gingerol on phorbol ester-induced cox-2 expression in mouse skin: p38 mapk and p65/rela as possible molecular targets

  • Kim, Sue-Oko;Chun, Kyung-Soo;Surh, Young-Joon
    • Proceedings of the PSK Conference
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    • 2003.10b
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    • pp.149.3-150
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    • 2003
  • [6]-Gingerol, a major pungent ingredient of ginger (Zingiber officinale Roscoe, Zingiberaceae) has a wide array of pharmacologic effects. Our previous studies have demonstrated that [6]-gingerol inhibits mouse skin tumor promotion and anchorage-independent growth of cultured mouse epidermal cells stimulated with epidermal growth factor. In this study, we have investigated the molecular mechanisms underlying anti-tumor promoting effects of [6]-gingerol on mouse skin carcinogenesis. (omitted)

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Gene Expression Profiling of Human Bronchial Epithelial (BEAS-2B) Cells Treated with Nitrofurantoin, a Pulmonary Toxicant

  • Kim, Youn-Jung;Song, Mee;Ryu, Jae-Chun
    • Molecular & Cellular Toxicology
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    • v.3 no.4
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    • pp.222-230
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    • 2007
  • Some drugs may be limited in their clinical application due to their propensity towards their adverse effects. Toxicogenomic technology represents a useful approach for evaluating the toxic properties of new drug candidates early in the drug discovery process. Nitrofurantoin (NF) is clinical chemotherapeutic agent and antimicrobial and used to treatment of urinary tract infections. However, NF has been shown to result in pulmonary toxic effects. In this research, we revealed the changing expression gene profiles in BEAS-2B, human bronchial epithelial cell line, exposed to NF by using human oligonucleotide chip. Through the clustering analysis of gene expression profiles, we identified 136 up-regulated genes and 379 down-regulated genes changed by more than 2-fold by NF. This study identifies several interesting targets and functions in relation to NF-induced toxicity through a gene ontology analysis method including biological process, cellular components, molecular function and KEGG pathway.

Molecular dynamics simulations approaches for discovering anti-influenza drug

  • Cho, Sungjoon;Choi, Youngjin
    • CELLMED
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    • v.6 no.4
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    • pp.24.1-24.4
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    • 2016
  • The emergence of influenza virus and antigenic drift are potential cause of world-wide pandemic. There are some commercially available drugs in the market to treat influenza. During past decade, however, critical resistances have been raised for biological targets. Because of structural complexity and flexibility of target proteins, applying a computational modeling tool is very beneficial for developing alternative anti-influenza drugs. In this review, we introduced molecular dynamics (MD) simulations approach to reflect full conformational flexibility of proteins during molecular modeling works. Case studies of MD works were summarized for the drug discovery and drug resistance mechanism of anti-influenza pharmaceuticals.

The role of microRNAs in synaptic development and function

  • Corbin, Rachel;Olsson-Carter, Katherine;Slack, Frank
    • BMB Reports
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    • v.42 no.3
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    • pp.131-135
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    • 2009
  • MicroRNAs control gene expression by inhibiting translation or promoting degradation of their target mRNAs. Since the discovery of the first microRNAs, lin-4 and let-7, in C. elegans, hundreds of microRNAs have been identified as key regulators of cell fate determination, lifespan, and cancer in species ranging from plants to humans. However, while microRNAs have been shown to be particularly abundant in the brain, their role in the development and activity of the nervous system is still largely unknown. In this review, we describe recent advances in our understanding of microRNA function at synapses, the specialized structures required for communication between neurons and their targets. We also propose how these advances might inform the molecular model of memory.

Synthesis of dimeric fluorescent TSPO ligand for detection of glioma

  • Tien Tan Bui;Hee-Kwon Kim
    • Journal of Radiopharmaceuticals and Molecular Probes
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    • v.7 no.1
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    • pp.56-65
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    • 2021
  • TSPO, an 18-kDa translocator protein, is a peripheral-type benzodiazepine receptor that has been associated to a variety of biological activities such as apoptosis, steroidogenesis, and cell proliferation. Because TSPO overexpression has been found in various forms of cancer, it has recently become one of the most appealing biological targets for cancer therapies and detection. In order to create new optical imaging agents for improved diagnostics, we synthesized a novel dimeric fluorescent TSPO ligand based on PRB28 structure and SCy5.5. Following the preparation of the novel TSPO ligand, in vivo and ex vivo imaging tests were performed to examine the tumor uptake characteristics of the fluorescent TSPO ligand in a glioma animal model, and it was found that novel TSPO ligand was accumulated in glioma. These results suggested that novel dimeric fluorescent TSPO ligand will be applied to detect glioma.

Identification of Anti-Cancer Targets of Eco-Friendly Waste Punica granatum Peel by Dual Reverse Virtual Screening and Binding Analysis

  • Usha, Talambedu;Goyal, Arvind Kumar;Lubna, Syed;Prashanth, H.P.;Mohan, T. Madhan;Pande, Veena;Middha, Sushil Kumar
    • Asian Pacific Journal of Cancer Prevention
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    • v.15 no.23
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    • pp.10345-10350
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    • 2015
  • Background: Punica granatum (family: Lythraceae) is mainly found in Iran, which is considered to be its primary centre of origin. Studies on pomegranate peel have revealed antioxidant, anti-inflammatory, anti-angiogenesis activities, with prevention of premature aging and reducing inflammation. In addition to this it is also useful in treating various diseases like diabetes, maintaining blood pressure and treatment of neoplasms such as prostate and breast cancer. Objectives: In this study we identified anti-cancer targets of active compounds like corilagin (tannins), quercetin (flavonoids) and pseudopelletierine (alkaloids) present in pomegranate peel by employing dual reverse screening and binding analysis. Materials and Methods: The potent targets of the pomegranate peel were annotated by the PharmMapper and ReverseScreen 3D, then compared with targets identified from different Bioassay databases (NPACT and HIT's). Docking was then further employed using AutoDock pyrx and validated through discovery studio for studying molecular interactions. Results: A number of potent anti-cancerous targets were attained from the PharmMapper server according to their fit score and from ReverseScreen 3D server according to decreasing 3D scores. Conclusion: The identified targets now need to be further validated through in vitro and in vivo studies.

Comparison of Hybridization Behavior between Double and Single Strand of Targets and the Application of Asymmetric PCR Targets in cDNA Microarray

  • Wei, Qing;Liu, Sanzhen;Huang, Jianfeng;Mao, Xueying;Chu, Xiaohui;Wang, Yu;Qiu, Minyan;Mao, Yumin;Xie, Yi;Li, Yao
    • BMB Reports
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    • v.37 no.4
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    • pp.439-444
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    • 2004
  • Double stranded targets on the cDNA microarray contain representatives of both the coding and noncoding strands, which will introduce hybridization competition with probes. Here, the effect of double and single strands of targets on the signal intensity and the ratios of Cy5/Cy3 within the same slide were compared. The results show that single stranded targets can increase the hybridization efficiency without changing the Cy5/Cy3 ratio. Based on these results, a new strategy was established by generating cDNA targets with asymmetric PCR, instead of conventional PCR, to increase the sensitivity of the cDNA microarray. Furthermore, the feasibility of this approach was validated. The results indicate that the cDNA microarray system based on asymmetric PCR is more sensitive, with no decrease in the reliability and reproducibility as compared with that based on conventional symmetric PCR.

mTOR signalling pathway - A root cause for idiopathic autism?

  • Ganesan, Harsha;Balasubramanian, Venkatesh;Iyer, Mahalaxmi;Venugopal, Anila;Subramaniam, Mohana Devi;Cho, Ssang-Goo;Vellingiri, Balachandar
    • BMB Reports
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    • v.52 no.7
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    • pp.424-433
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    • 2019
  • Autism spectrum disorder (ASD) is a complex neurodevelopmental monogenic disorder with a strong genetic influence. Idiopathic autism could be defined as a type of autism that does not have a specific causative agent. Among signalling cascades, mTOR signalling pathway plays a pivotal role not only in cell cycle, but also in protein synthesis and regulation of brain homeostasis in ASD patients. The present review highlights, underlying mechanism of mTOR and its role in altered signalling cascades as a triggering factor in the onset of idiopathic autism. Further, this review discusses how distorted mTOR signalling pathway stimulates truncated translation in neuronal cells and leads to downregulation of protein synthesis at dendritic spines of the brain. This review concludes by suggesting downstream regulators such as p70S6K, eIF4B, eIF4E of mTOR signalling pathway as promising therapeutic targets for idiopathic autistic individuals.