Benzopyran Derivative

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Yungjin Kim - One of the best experts on this subject based on the ideXlab platform.

  • KR-31831, a new synthetic anti-ischemic agent, inhibits in vivo and in vitro angiogenesis
    Experimental & Molecular Medicine, 2006
    Co-Authors: Shiyoung Park, Hyun Seok Song, Myung Jin Son, Sung-en Yoo, Yungjin Kim
    Abstract:

    Angiogenesis is considered to be an integral process to the growth and spread of solid tumors. Anti-angiogenesis therapy recently has been found to be one of the most promising anti-cancer therapeutic strategies. In this study, we provide several lines of evidences showing that KR-31831, a new Benzopyran Derivative, has anti-angiogenic activities. KR-31831 inhibited the proliferation, migration, invasion and tube formation of bovine aortic endothelial cells (BAECs), and suppressed the release of matrix metalloproteinase-2 (MMP-2) of BAECs. KR-31831 also inhibited in vivo angiogenesis in mouse Matrigel plug assay. Furthermore, the mRNA expressions of basic fibroblast growth factor (bFGF), fibroblast growth factor receptor-2 (FGFR-2), and vascular endothelial growth factor receptor-2 (VEGFR-2) were decreased by KR-31831. Taken together, these results suggest that KR-31831 acts as a novel angiogenesis inhibitor and might be useful for treating hypervascularized cancers.

  • kr 31831 Benzopyran Derivative inhibits vegf induced angiogenesis of huvecs through suppressing kdr expression
    International Journal of Oncology, 1992
    Co-Authors: Shiyoung Park, Sung-eun Yoo, Eunhee Seo, Hyun Seok Song, Seungyoun Jung, Youngkyoung Lee, Yungjin Kim
    Abstract:

    Angiogenesis is important in the development and progression of cancer, therefore the therapeutic approach based on anti-angiogenesis may represent a promising therapeutic option. KR-31831 is a novel anti-ischemic agent. Previously, we reported the anti-angiogenic activity of KR-31831. In the present study we investigated the molecular mechanisms underlying anti-angiogenic activity of KR-31831. We show that KR-31831 inhibits vascular endothelial growth factor (VEGF)-induced proliferation and tube formation via release of intracellular Ca 2+ and phosphorylation of extra-cellular regulated kinase 1/2 (Erkl/2) in human umbilical vein endothelial cells (HUVECs). Moreover, the expression of VEGF receptor 2 (VEGFR2, known as Flk-1 or KDR) was reduced by the treatment of KR-31831. These results suggest that KR-31831 may have inhibitory effects on tumor angiogenesis through down-regulation of KDR expression.

Shiyoung Park - One of the best experts on this subject based on the ideXlab platform.

  • KR-31831, a new synthetic anti-ischemic agent, inhibits in vivo and in vitro angiogenesis
    Experimental & Molecular Medicine, 2006
    Co-Authors: Shiyoung Park, Hyun Seok Song, Myung Jin Son, Sung-en Yoo, Yungjin Kim
    Abstract:

    Angiogenesis is considered to be an integral process to the growth and spread of solid tumors. Anti-angiogenesis therapy recently has been found to be one of the most promising anti-cancer therapeutic strategies. In this study, we provide several lines of evidences showing that KR-31831, a new Benzopyran Derivative, has anti-angiogenic activities. KR-31831 inhibited the proliferation, migration, invasion and tube formation of bovine aortic endothelial cells (BAECs), and suppressed the release of matrix metalloproteinase-2 (MMP-2) of BAECs. KR-31831 also inhibited in vivo angiogenesis in mouse Matrigel plug assay. Furthermore, the mRNA expressions of basic fibroblast growth factor (bFGF), fibroblast growth factor receptor-2 (FGFR-2), and vascular endothelial growth factor receptor-2 (VEGFR-2) were decreased by KR-31831. Taken together, these results suggest that KR-31831 acts as a novel angiogenesis inhibitor and might be useful for treating hypervascularized cancers.

  • kr 31831 Benzopyran Derivative inhibits vegf induced angiogenesis of huvecs through suppressing kdr expression
    International Journal of Oncology, 1992
    Co-Authors: Shiyoung Park, Sung-eun Yoo, Eunhee Seo, Hyun Seok Song, Seungyoun Jung, Youngkyoung Lee, Yungjin Kim
    Abstract:

    Angiogenesis is important in the development and progression of cancer, therefore the therapeutic approach based on anti-angiogenesis may represent a promising therapeutic option. KR-31831 is a novel anti-ischemic agent. Previously, we reported the anti-angiogenic activity of KR-31831. In the present study we investigated the molecular mechanisms underlying anti-angiogenic activity of KR-31831. We show that KR-31831 inhibits vascular endothelial growth factor (VEGF)-induced proliferation and tube formation via release of intracellular Ca 2+ and phosphorylation of extra-cellular regulated kinase 1/2 (Erkl/2) in human umbilical vein endothelial cells (HUVECs). Moreover, the expression of VEGF receptor 2 (VEGFR2, known as Flk-1 or KDR) was reduced by the treatment of KR-31831. These results suggest that KR-31831 may have inhibitory effects on tumor angiogenesis through down-regulation of KDR expression.

William F Reynolds - One of the best experts on this subject based on the ideXlab platform.

Jinlong Zhang - One of the best experts on this subject based on the ideXlab platform.

  • Characterization of the xiamenmycin biosynthesis gene cluster in Streptomyces xiamenensis 318. PLoS One 2014
    2016
    Co-Authors: Yong Yang, Jinlong Zhang
    Abstract:

    Xiamenmycin (1) is a prenylated Benzopyran Derivative with anti-fibrotic activity. To investigate the genetic basis of xiamenmycin biosynthesis, we performed genome mining in the xiamenmycin-producing Streptomyces xiamenensis wild-type strain 318 to identify a candidate gene cluster. The complete gene cluster, consisting of five genes, was confirmed by a series of gene inactivations and heterologous expression. Based on bioinformatics analyses of each gene and feeding experiments, we found that the structure of an intermediate xiamenmycin B (3) accumulated in a ximA inactivation mutant, allowing us to propose a biosynthetic pathway. All five of the genes in the pathway were genetically and biochemically characterized. XimA was biochemically characterized as an ATP-dependent amide synthetase, catalyzing an amide bond formation in the presence of ATP as the final step in Xiamenmycin biosynthesis. The Km value of XimA was determined to be 474.38 mM for the substrate xiamenmycin B. These studies provide opportunities to use genetic and chemo-enzymati

  • Characterization of the xiamenmycin biosynthesis gene cluster in Streptomyces xiamenensis 318.
    PLOS ONE, 2014
    Co-Authors: Yong Yang, Jinlong Zhang
    Abstract:

    Xiamenmycin (1) is a prenylated Benzopyran Derivative with anti-fibrotic activity. To investigate the genetic basis of xiamenmycin biosynthesis, we performed genome mining in the xiamenmycin-producing Streptomyces xiamenensis wild-type strain 318 to identify a candidate gene cluster. The complete gene cluster, consisting of five genes, was confirmed by a series of gene inactivations and heterologous expression. Based on bioinformatics analyses of each gene and feeding experiments, we found that the structure of an intermediate xiamenmycin B (3) accumulated in a ximA inactivation mutant, allowing us to propose a biosynthetic pathway. All five of the genes in the pathway were genetically and biochemically characterized. XimA was biochemically characterized as an ATP-dependent amide synthetase, catalyzing an amide bond formation in the presence of ATP as the final step in Xiamenmycin biosynthesis. The Km value of XimA was determined to be 474.38 µM for the substrate xiamenmycin B. These studies provide opportunities to use genetic and chemo-enzymatic methods to create new Benzopyran Derivatives as potential therapeutic agents.

Hyun Seok Song - One of the best experts on this subject based on the ideXlab platform.

  • KR-31831, a new synthetic anti-ischemic agent, inhibits in vivo and in vitro angiogenesis
    Experimental & Molecular Medicine, 2006
    Co-Authors: Shiyoung Park, Hyun Seok Song, Myung Jin Son, Sung-en Yoo, Yungjin Kim
    Abstract:

    Angiogenesis is considered to be an integral process to the growth and spread of solid tumors. Anti-angiogenesis therapy recently has been found to be one of the most promising anti-cancer therapeutic strategies. In this study, we provide several lines of evidences showing that KR-31831, a new Benzopyran Derivative, has anti-angiogenic activities. KR-31831 inhibited the proliferation, migration, invasion and tube formation of bovine aortic endothelial cells (BAECs), and suppressed the release of matrix metalloproteinase-2 (MMP-2) of BAECs. KR-31831 also inhibited in vivo angiogenesis in mouse Matrigel plug assay. Furthermore, the mRNA expressions of basic fibroblast growth factor (bFGF), fibroblast growth factor receptor-2 (FGFR-2), and vascular endothelial growth factor receptor-2 (VEGFR-2) were decreased by KR-31831. Taken together, these results suggest that KR-31831 acts as a novel angiogenesis inhibitor and might be useful for treating hypervascularized cancers.

  • kr 31831 Benzopyran Derivative inhibits vegf induced angiogenesis of huvecs through suppressing kdr expression
    International Journal of Oncology, 1992
    Co-Authors: Shiyoung Park, Sung-eun Yoo, Eunhee Seo, Hyun Seok Song, Seungyoun Jung, Youngkyoung Lee, Yungjin Kim
    Abstract:

    Angiogenesis is important in the development and progression of cancer, therefore the therapeutic approach based on anti-angiogenesis may represent a promising therapeutic option. KR-31831 is a novel anti-ischemic agent. Previously, we reported the anti-angiogenic activity of KR-31831. In the present study we investigated the molecular mechanisms underlying anti-angiogenic activity of KR-31831. We show that KR-31831 inhibits vascular endothelial growth factor (VEGF)-induced proliferation and tube formation via release of intracellular Ca 2+ and phosphorylation of extra-cellular regulated kinase 1/2 (Erkl/2) in human umbilical vein endothelial cells (HUVECs). Moreover, the expression of VEGF receptor 2 (VEGFR2, known as Flk-1 or KDR) was reduced by the treatment of KR-31831. These results suggest that KR-31831 may have inhibitory effects on tumor angiogenesis through down-regulation of KDR expression.