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  • Bentham Science Publishers Ltd.  (2)
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  • Bentham Science Publishers Ltd.  (2)
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  • 1
    Online Resource
    Online Resource
    Gossypetin Inhibits Solar-UV Induced Cutaneous Basal Cell Carcinoma Through Direct Inhibiting PBK/TOPK Protein Kinase
    Bentham Science Publishers Ltd. ; 2019
    In:  Anti-Cancer Agents in Medicinal Chemistry Vol. 19, No. 8 ( 2019-08-21), p. 1029-1036
    Details
    In: Anti-Cancer Agents in Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 19, No. 8 ( 2019-08-21), p. 1029-1036
    Abstract: Skin photoaging, skin inflammation and skin cancer are related with excessive exposure to solar UV. PDZ-binding kinase/T-LAK cell-originated protein kinase (PBK/TOPK), a member of the serine/threonine protein kinase, which regulates the signaling cascades of p38 mitogen-activated protein kinase (p38 MAPK) and extracellular signal regulated kinase 1/2 (ERK1/2). PBK/TOPK plays a significant role in solar-UV-induced cutaneous basal cell carcinoma (BCC), and targeting PBK/TOPK can be supposed to treat and prevent cutaneous BCC. Methods: The pathological feature and the expression level of PBK/TOPK in cutaneous BCC tissues of human were studied in clinical samples. SUV-induced the phosphorylation of p38 MAPK and ERK1/2 were demonstrated ex vivo. Moreover, the interaction between Gossypetin and PBK/TOPK were detected by in vitro kinase assay and Microscale thermophoresis (MST) assay. Furthermore, the effect of Gossypetin to solar UV-induced the activity of PBK/TOPK were detected ex vivo and in vivo. Results: The clinical samples showed that the expression levels of PBK/TOPK, phosphor-p38 MAPK and phosphor- ERK1/2 were up-regulated in cutaneous BCC tissues of human. The expression of phosphor-p38 MAPK or phosphor-ERK1/2 increased in a dose and time dependent manner after solar UV treatment in HaCaT cells. MTT cytotoxicity assay results showed that Gossypetin has no effect on HaCaT cells. In vitro kinase assay and MST assay results showed that Gossypetin bound with PBK/TOPK and suppressed PBK/TOPK activity. Ex vivo results showed Gossypetin inhibited solar UV-induced phosphorylation of PBK/TOPK, p38 MAPK, ERK1/2 and H2AX by suppressing PBK/TOPK activity. In vivo test results indicated that Gossypetin suppressed solar UV-induced increase of PBK/TOPK, phosphor-p38 MAPK, phosphor-ERK1/2 and phosphor- H2AX in SKH-1 hairless mice. Conclusion: Our data demonstrated that Gossypetin can alleviate solar-UV-induced cutaneous BCC by blocking PBK/TOPK, and Gossypetin could be a remarkable agent for treating solar-UV induced cutaneous basal cell carcinoma.
    Type of Medium: Online Resource
    ISSN: 1871-5206
    URL: Article
    DOI: 10.2174/1871520619666190301123131
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2019
    SSG: 15,3
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  • 2
    Online Resource
    Online Resource
    Scutellarin Suppresses RPMI7951 Melanoma Cell Proliferation by Targeting TOPK
    Bentham Science Publishers Ltd. ; 2021
    In:  Anti-Cancer Agents in Medicinal Chemistry Vol. 21, No. 5 ( 2021-03), p. 640-648
    Details
    In: Anti-Cancer Agents in Medicinal Chemistry, Bentham Science Publishers Ltd., Vol. 21, No. 5 ( 2021-03), p. 640-648
    Abstract: T-LAK cell-Originated Protein Kinase (TOPK) belongs to the serine/threonine protein kinase family. It is highly expressed in RPMI7951 melanoma cells. Scutellarin (SCU) is an active ingredient extracted from Erigeron breviscapus (Vant.) Hand.–Mazz. Its main physiological functions are related to its anti-inflammatory and antitumour activities. Methods: The relationship between SCU and TOPK was assessed by molecular docking, an in vitro binding assay and an in vitro kinase assay. The effect of SCU on RPMI7951 cells was detected by MTS and soft agar assays. TOPK knockdown was induced by lentiviral infection. The TOPK downstream signalling pathway was detected by western blot and immunohistochemical analyses in vitro and in vivo. Results: SCU was found to directly bind with TOPK and inhibit TOPK activity in vitro. SCU inhibited the proliferation and colony formation of RPMI7951 cells in a dose-dependent manner. Silencing TOPK decreased the sensitivity of colon cancer cells to SCU. SCU inhibited the phosphorylation levels of Extracellular Regulated protein Kinases 1/2 (ERK1/2) and histone H3 in a time- and dose-dependent manner in RPMI7951 cells. In addition, SCU inhibited the growth of xenograft tumours of RPMI7951 cells and decreased the phosphorylation levels of extracellular regulated protein kinases 1/2 and histone H3 in vivo. Conclusion: The results showed that SCU exerts promising antitumour effects on human RPMI7951 cells by inhibiting the activity of TOPK.
    Type of Medium: Online Resource
    ISSN: 1871-5206
    URL: Article
    DOI: 10.2174/1871520620666200811112156
    Language: English
    Publisher: Bentham Science Publishers Ltd.
    Publication Date: 2021
    SSG: 15,3
    Location Call Number Limitation Availability
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    Online Resource
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