A5059886217- Natural product bioactivities and synthesis
- Cytokine Signaling Pathways and Interactions
- Phytochemistry and Biological Activities
- Plant biochemistry and biosynthesis
- Cholesterol and Lipid Metabolism
- Bioactive Compounds and Antitumor Agents
- Sesquiterpenes and Asteraceae Studies
- Magnolia and Illicium research
- X-ray Diffraction in Crystallography
- Crystallization and Solubility Studies
- Protein Tyrosine Phosphatases
- Traditional and Medicinal Uses of Annonaceae
- Oxidative Organic Chemistry Reactions
- Chemical Synthesis and Analysis
- Natural Antidiabetic Agents Studies
- Synthesis and biological activity
- Phytochemical compounds biological activities
- Peroxisome Proliferator-Activated Receptors
- Click Chemistry and Applications
- Peptidase Inhibition and Analysis
- Cancer Treatment and Pharmacology
- Microbial Natural Products and Biosynthesis
- Medicinal Plant Pharmacodynamics Research
- Phytochemistry and Bioactive Compounds
- Steroid Chemistry and Biochemistry
Korea Research Institute of Bioscience and Biotechnology
2013-2022
Korea University of Science and Technology
2012-2021
Kyung Hee University
2007-2020
Government of the Republic of Korea
2016
In-Q-Tel
2011
University of Science and Technology
2011
Chungnam National University
2010
Korea Advanced Institute of Science and Technology
2002-2009
University of Pavia
2001-2008
Woosuk University
2008
Abstract Because signal transducer and activator of transcription 3 (STAT3) is constitutively activated in most human solid tumors involved the proliferation, angiogenesis, immune evasion, antiapoptosis cancer cells, researchers have focused on STAT3 as a target for therapy. We screened natural compounds that inhibit activity using dual-luciferase assay. Cryptotanshinone was identified potent inhibitor. rapidly inhibited Tyr705 phosphorylation DU145 prostate cells growth through 96 hours...
Heat shock factor 1 (HSF1) is the master switch for heat protein (HSP) expression in eukaryotes. A synthetic chemical library was screened to identify inhibitors of HSF1 using a luciferase reporter under control element. compound named KRIBB11 (N(2)-(1H-indazole-5-yl)-N(6)-methyl-3-nitropyridine-2,6-diamine) identified its activity abolishing shock-induced with an IC(50) 1.2 μmol/liter. When cells were exposed presence KRIBB11, induction downstream target proteins such as HSP27 and HSP70...
Cancer cells, compared to normal are under oxidative stress associated with an elevated level of reactive oxygen species (ROS) and more vulnerable induced by ROS generating agents. Thus, manipulation the provides a logical approach kill cancer cells preferentially, without significant toxicity great efforts have been dedicated development strategies induce cytotoxic for treatment. Fenton reaction is important biological in which irons convert hydrogen peroxide (H2O2) highly toxic hydroxyl...
Heat shock factor 1 (HSF1) is a transcription for heat proteins (HSPs) expression that enhances the survival of cancer cells exposed to various stresses. HSF1 knockout suppresses carcinogen-induced induction in mice. Therefore, promising therapeutic and chemopreventive target. We performed cell-based screening with natural compound collection identified fisetin, dietary flavonoid, as inhibitor. Fisetin abolished shock-induced luciferase activity an IC50 14 μM HCT-116 cells. The treatment...
Obovatol isolated from the medicinal herb Magnolia obovata exhibits a variety of biological activities. Here, effect obovatol and its mechanism action on microglial activation, neuroinflammation neurodegeneration were investigated.In BV-2 cells stimulated with lipopolysaccharide (LPS), we measured nitric oxide (NO) cytokine production, activation intracellular signalling pathways by reverse transcription-polymerase chain reaction Western blots. Cell death was assayed in co-cultures activated...
Signal transducer and activator of transcription 3 (STAT3) is constitutively activated in human cancers. Therefore, STAT3 a therapeutic target cancer drug discovery. We previously reported that natural products inhibited prostate tumor cells. used dual-luciferase assay to screen 200 isolated from herbal medicines we identified ginkgetin obtained the leaves Ginkgo biloba L. as inhibitor. Ginkgetin both inducible blocked nuclear translocation p-STAT3 DU-145 Furthermore, selectively growth...
Abstract ARPC2 is a subunit of the Arp2/3 complex, which essential for lamellipodia, invadopodia and filopodia, has been identified as migrastatic target molecule. To identify inhibitors, we generated an knockout DLD‐1 human colon cancer cell line using clustered regularly interspaced short palindromic repeats/CRISPR‐associated protein 9 (CRISPR/Cas9) system explored gene signature‐based strategies, such connectivity map (CMap) expression profiling data knockdown cells. From CMap‐based drug...
2′-Hydroxycinnamaldehyde (HCA) was isolated from Cinnamomum cassia Blume (Lauraceae) and 2′-benzoyloxycinna-maldehyde (BCA) prepared by the reaction of HCA benzoyl chloride. BCA strongly inhibited in vitro growth 29 kinds human cancer cells vivo SW-620 tumor xenograft without loss body weight nude mice. prevented adherence to culture surface but did not inhibit oncogenic K-Ras processing, implying its antitumor mechanisms at cellular level.
The flavones 5,6-dihydroxy-7,3′,4′-trimethoxyflavone (1), 5,6,4′-trihydroxy-7,3′-dimethoxyflavone (2), 5-hydroxy-3′,4′,6,7-tetramethoxyflavone, 5,7,3′-trihydroxy-6,4′,5′-trimethoxyflavone, ladanein, and hispidulin were isolated from the methanolic extracts of aerial parts Artemisia argyi structures compounds elucidated on basis their spectral data. These inhibited farnesyl protein transferase with IC50 values 25 - 200 μg/mL. Compound 2 proliferation a couple tumor cell lines also...
Structures of the protein-chromophore complex and apoprotein form neocarzinostatin were determined at 1.8 angstrom resolution. Neocarzinostatin is composed a labile chromophore with DNA-cleaving activity stabilizing protein. The displays marked nonlinearity triple bonds bound noncovalently in pocket formed by two protein domains. π-face interacts phenyl ring edges Phe 52 78 . amino sugar carbonate groups are solvent exposed, whereas epoxide, acetylene groups, carbon C-12, site nucleophilic...