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Luteolin suppresses cancer cell proliferation by targeting vaccinia-related kinase 1

หน่วยงาน Nanyang Technological University, Singapore

รายละเอียด

ชื่อเรื่อง : Luteolin suppresses cancer cell proliferation by targeting vaccinia-related kinase 1
นักวิจัย : Kim, Ye Seul , Kim, Seong-Hoon , Shin, Joon , Harikishore, Amaravadhi , Lim, Jong-Kwan , Jung, Youngseob , Lyu, Ha-Na , Baek, Nam-In , Choi, Kwan Yong , Yoon, Ho Sup , Kim, Kyong-Tai
คำค้น : DRNTU::Science::Biological sciences
หน่วยงาน : Nanyang Technological University, Singapore
ผู้ร่วมงาน : Amin, A. R. M. Ruhul
ปีพิมพ์ : 2557
อ้างอิง : Kim, Y. S., Kim, S.-H., Shin, J., Harikishore, A., Lim, J.-K., Jung, Y., et al. (2014). Luteolin suppresses cancer cell proliferation by targeting vaccinia-related kinase 1. PLoS One, 9(10). , 1932-6203 , http://hdl.handle.net/10220/24139 , http://dx.doi.org/10.1371/journal.pone.0109655
ที่มา : -
ความเชี่ยวชาญ : -
ความสัมพันธ์ : PLoS One
ขอบเขตของเนื้อหา : -
บทคัดย่อ/คำอธิบาย :

Uncontrolled proliferation, a major feature of cancer cells, is often triggered by the malfunction of cell cycle regulators such as protein kinases. Recently, cell cycle-related protein kinases have become attractive targets for anti-cancer therapy, because they play fundamental roles in cellular proliferation. However, the protein kinase-targeted drugs that have been developed so far do not show impressive clinical results and also display severe side effects; therefore, there is undoubtedly a need to investigate new drugs targeting other protein kinases that are critical in cell cycle progression. Vaccinia-related kinase 1 (VRK1) is a mitotic kinase that functions in cell cycle regulation by phosphorylating cell cycle-related substrates such as barrier-to-autointegration factor (BAF), histone H3, and the cAMP response element (CRE)-binding protein (CREB). In our study, we identified luteolin as the inhibitor of VRK1 by screening a small-molecule natural compound library. Here, we evaluated the efficacy of luteolin as a VRK1-targeted inhibitor for developing an effective anti-cancer strategy. We confirmed that luteolin significantly reduces VRK1-mediated phosphorylation of the cell cycle-related substrates BAF and histone H3, and directly interacts with the catalytic domain of VRK1. In addition, luteolin regulates cell cycle progression by modulating VRK1 activity, leading to the suppression of cancer cell proliferation and the induction of apoptosis. Therefore, our study suggests that luteolin-induced VRK1 inhibition may contribute to establish a novel cell cycle-targeted strategy for anti-cancer therapy.

บรรณานุกรม :
Kim, Ye Seul , Kim, Seong-Hoon , Shin, Joon , Harikishore, Amaravadhi , Lim, Jong-Kwan , Jung, Youngseob , Lyu, Ha-Na , Baek, Nam-In , Choi, Kwan Yong , Yoon, Ho Sup , Kim, Kyong-Tai . (2557). Luteolin suppresses cancer cell proliferation by targeting vaccinia-related kinase 1.
    กรุงเทพมหานคร : Nanyang Technological University, Singapore.
Kim, Ye Seul , Kim, Seong-Hoon , Shin, Joon , Harikishore, Amaravadhi , Lim, Jong-Kwan , Jung, Youngseob , Lyu, Ha-Na , Baek, Nam-In , Choi, Kwan Yong , Yoon, Ho Sup , Kim, Kyong-Tai . 2557. "Luteolin suppresses cancer cell proliferation by targeting vaccinia-related kinase 1".
    กรุงเทพมหานคร : Nanyang Technological University, Singapore.
Kim, Ye Seul , Kim, Seong-Hoon , Shin, Joon , Harikishore, Amaravadhi , Lim, Jong-Kwan , Jung, Youngseob , Lyu, Ha-Na , Baek, Nam-In , Choi, Kwan Yong , Yoon, Ho Sup , Kim, Kyong-Tai . "Luteolin suppresses cancer cell proliferation by targeting vaccinia-related kinase 1."
    กรุงเทพมหานคร : Nanyang Technological University, Singapore, 2557. Print.
Kim, Ye Seul , Kim, Seong-Hoon , Shin, Joon , Harikishore, Amaravadhi , Lim, Jong-Kwan , Jung, Youngseob , Lyu, Ha-Na , Baek, Nam-In , Choi, Kwan Yong , Yoon, Ho Sup , Kim, Kyong-Tai . Luteolin suppresses cancer cell proliferation by targeting vaccinia-related kinase 1. กรุงเทพมหานคร : Nanyang Technological University, Singapore; 2557.