• 제목/요약/키워드: therapeutic potential

검색결과 2,195건 처리시간 0.028초

Matrix Metalloproteinase: Inhibitory Effect of Marine Substances on MMP-2 and MMP-9

  • Nguyen, Van-Tinh;Qian, Zhong-Ji;Jung, Won-Kyo
    • 통합자연과학논문집
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    • 제4권4호
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    • pp.255-265
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    • 2011
  • Marine ecosystems are often characterized by a high biological diversity, and it corresponds to a high chemical diversity. Up to present, more than 20,000 new bioactive substances have been isolated from marine organisms, where considerable numbers of these naturally occurring derivatives are developed as potential candidates for pharmaceutical application. In this process, screening of natural products from marine organisms that could potentially inhibit the expression of metalloproteinases has gained a huge popularity. Cancer is considered as one of the deadliest diseases in the medical field. Matrix metalloproteinase (MMPs) can degrade extracellular matrix (ECM) components and play important roles in a variety of biological and pathological processes. Matrix metalloproteinase inhibitors (MMPIs) have been identified as potential therapeutic candidates for metastasis, arthritis, chronic inflammation and wrinkle formation.

Homology Modelling of Chemerin like Receptor-1 (CMKLR1): Potential Target for Treating Type II Diabetes

  • B, Sathya.
    • 통합자연과학논문집
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    • 제10권1호
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    • pp.20-26
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    • 2017
  • Chemerin receptor, which predominantly expressed in immune cells as well as adipose tissue, was found to stimulate chemotaxis of dendritic cells and macrophages to the site of inflammation. Chemerin is a widely distributed multifunctional secreted protein implicated in immune cell migration, adipogenesis, osteoblastogenesis, angiogenesis, myogenesis, and glucose homeostasis. Recent studies suggest chemerin may play an important role in the pathogenesis of obesity and insulin resistance and it becomes a potential therapeutic target for treating type II diabetes. The crystal structure of chemerin receptor has not yet been resolved. Therefore, in the present study, homology modelling of CMKLR1 was done utilizing the crystal structure of human angiotension receptor in complex with inverse agonist olmesartan as the template. Since the template has low sequence identity, we have incorporated both threading and comparative modelling approach to generate the three dimensional structure. 3D models were generated and validated. The reported models can be used to characterize the critical amino acid residues in the binding site of CMKLR1.

Synthesis of Flavokawain Analogues and their Anti-neoplastic Effects on Drug-resistant Cancer Cells Through Hsp90 Inhibition

  • Seo, Young Ho;Park, Sun You
    • Bulletin of the Korean Chemical Society
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    • 제35권4호
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    • pp.1154-1158
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    • 2014
  • Hsp90 is an ubiquitous molecular chaperone protein, which plays an important role in regulating maturation and stabilization of many oncogenic proteins. Due to its potential to simultaneously disable multiple signaling pathways, Hsp90 represents great promise as a therapeutic target of cancer. In this study, we synthesized flavokawain analogues and evaluated their biological activities against drug-resistant cancer cells. The study indicated that compound 1i impaired the growth of gefitinib-resistant non-small cell lung cancer (H1975), down-regulated the expression of Hsp90 client proteins including EGFR, Her2, Met, Akt and Cdk4, and upregulated the expression of Hsp70. The result strongly suggested that compound 1i inhibited the proliferation of cancer cells through Hsp90 inhibition. Overall, compound 1i could serve as a potential lead compound to overcome the drug resistance in cancer chemotherapy.

BDNF가 ADHD의 병인과 치료에 미치는 영향 (Association between the Brain-Derived Neurotropic Factor and Attention Deficit Hyperactivity Disorder)

  • 강나리;송재민;곽영숙
    • 생물정신의학
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    • 제25권2호
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    • pp.21-30
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    • 2018
  • Attention deficit hyperactivity disorder (ADHD) is a common childhood psychiatric disorder. Recently, it has been suggested that brain-derived neurotropic factor (BDNF) may play a role in the pathogenesis of ADHD. Our aim of this review is to understand the physiological functions of BDNF and its potential relationship with ADHD and therapeutic approaches of ADHD. Searches were conducted in Pubmed and Research Information Service System (RISS). In this review, we summarized important literatures for the physiological functions of BDNF in neurodevelopment, change of serum BDNF level in ADHD, association of BDNF polymorphism and ADHD and potential association of treatment of ADHD with serum BDNF level. Further studies are required to more clearly understand the source and the role of BDNF in ADHD and to develop BDNF based-ADHD treatement.

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Sphingolipids in neuroinflammation: a potential target for diagnosis and therapy

  • Lee, Ju Youn;Jin, Hee Kyung;Bae, Jae-sung
    • BMB Reports
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    • 제53권1호
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    • pp.28-34
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    • 2020
  • Sphingolipids are ubiquitous building blocks of eukaryotic cell membranes that function as signaling molecules for regulating a diverse range of cellular processes, including cell proliferation, growth, survival, immune-cell trafficking, vascular and epithelial integrity, and inflammation. Recently, several studies have highlighted the pivotal role of sphingolipids in neuroinflammatory regulation. Sphingolipids have multiple functions, including induction of the expression of various inflammatory mediators and regulation of neuroinflammation by directly effecting the cells of the central nervous system. Accumulating evidence points to sphingolipid engagement in neuroinflammatory disorders, including Alzheimer's and Parkinson's diseases. Abnormal sphingolipid alterations, which involves an increase in ceramide and a decrease in sphingosine kinase, are observed during neuroinflammatory disease. These trends are observed early during disease development, and thus highlight the potential of sphingolipids as a new therapeutic and diagnostic target for neuroinflammatory diseases.

접골목 추출물에 의한 항산화 활성이 정상 간세포의 t-BHP 유발 산화스트레스에 미치는 영향 (Antioxidant Activity and Protective Effects of Extracts from Sambucus williamsii var. coreana on t-BHP Induced Oxidative Stress in Chang cells)

  • 김기태
    • 대한한의진단학회지
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    • 제17권3호
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    • pp.275-286
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    • 2013
  • In the present study, antioxidant activity and protective effect of extracts from Sambucus williamsii var. coreana stems (SWC) were evaluated on tert-butyl hydroperoxide (t-BHP) induced oxidative stress in human liver (Chang) cells. Antioxidant activities of the SWC extracts were determined by various radical scavenging activities, such as DPPH, ferric reducing antioxidant power (FRAP), 2,2'-azinobis-(3-ethybenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activity and oxygen radical absorbance capacity (ORAC) assay. SWC extracts showed strong antioxidant effect on various assay. To determine the hepatoprotective effects of SWC on t-BHP induced oxidative damage, cell viability was measured using MTT assay. Pretreatment of SWC extracts showed increasing cell viability, decreasing ROS and restoring mitochondria membrane potential on t-BHP induced oxidative stress in Chang cells. Our findings suggest that SWC extracts may be considered a potential agent for therapeutic protective effect from oxidative stress through its antioxidant activity.

Receptor for Advanced Glycation Endproducts (RAGE), Its Ligands, and Soluble RAGE: Potential Biomarkers for Diagnosis and Therapeutic Targets for Human Renal Diseases

  • Lee, Eun Ji;Park, Jong Hoon
    • Genomics & Informatics
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    • 제11권4호
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    • pp.224-229
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    • 2013
  • Receptor for advanced glycation endproducts (RAGE) is a multi-ligand receptor that is able to bind several different ligands, including advanced glycation endproducts, high-mobility group protein (B)1 (HMGB1), S-100 calcium-binding protein, amyloid-${\beta}$-protein, Mac-1, and phosphatidylserine. Its interaction is engaged in critical cellular processes, such as inflammation, proliferation, apoptosis, autophagy, and migration, and dysregulation of RAGE and its ligands leads to the development of numerous human diseases. In this review, we summarize the signaling pathways regulated by RAGE and its ligands identified up to date and demonstrate the effects of hyper-activation of RAGE signals on human diseases, focused mainly on renal disorders. Finally, we propose that RAGE and its ligands are the potential targets for the diagnosis, monitoring, and treatment of numerous renal diseases.

Genomic Profiling of Liver Cancer

  • Lee, Ju-Seog
    • Genomics & Informatics
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    • 제11권4호
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    • pp.180-185
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    • 2013
  • Development of liver cancers is driven largely by genomic alterations that deregulate signaling pathways, influencing growth and survival of cancer cells. Because of the hundreds or thousands of genomic/epigenomic alterations that have accumulated in the cancer genome, it is very challenging to find and test candidate genes driving tumor development and progression. Systematic studies of the liver cancer genome have become available in recent years. These studies have uncovered new potential driver genes, including those not previously known to be involved in the development of liver cancer. Novel approaches combining multiple datasets from patient tissues have created an unparalleled opportunity to uncover potential new therapeutic targets and prognostic/predictive biomarkers for personalized therapy that can improve clinical outcomes of the patients with liver cancer.

Therapeutic Potential of Membrane Fatty Acid Modifiaction in Tumor Cells

  • Shon, Yun-Hee;Park, Kun-Young;Kim, Kwang-Soo
    • Preventive Nutrition and Food Science
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    • 제1권1호
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    • pp.143-150
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    • 1996
  • The membrane fatty acid composition of tumor cell can be modified either in cell by altering the lipid composition of the medium of during growth in animals by changing the dietaty fat composition. These modifications are associated with changes in membrane physical properties and certain cellular functions, including carrier-mediated transport and enzyme contained within the membrane. Such effects influence the transport of nutrients and chemotherapeutic agents in cancer cells .Fatty acid modification also can enhance the sensitivity of the neoplastic cell to chemotherapy. The alteration in plasma membrane composition will be affected through dietary supplementations and the potential value to cancer patients could be a better understanding of the effects of diet on responsiveness of neoplasms to chemotherapy, i.e. cancer patients' chances for a "cure" can be improved by diet changes prior to treatment.

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Toxicity of disulfiram, a therapeutic agent for chronic alcoholism, to mouse spleen cells

  • Han, Yong;Joo, Hong-Gu
    • Journal of Preventive Veterinary Medicine
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    • 제42권4호
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    • pp.177-181
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    • 2018
  • Disulfiram is a drug used to treat alcohol dependence. Recent studies have shown that disulfiram also has anti-cancer effects. Considering that many anti-cancer agents have side effects, including immunosuppression, it is important to check if disulfiram has some cytotoxicity to immune cells. In this study, mouse spleen cells were treated with disulfiram and the metabolic activity was measured. Disulfiram increased the cell death of spleen cells according to annexin V-FITC/PI staining analysis. In addition, disulfiram decreased the mitochondrial membrane potential of spleen cells. The toxicity of disulfiram was concentration dependent. Interestingly, disulfiram affected the population of lymphocytes and the subset of spleen cells was altered. This study provides clinicians and researchers with valuable information regarding the toxicity of disulfiram to mouse spleen cells, particularly lymphocytes.