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10.1038/srep14570

http://scihub22266oqcxt.onion/10.1038/srep14570
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C4585938!4585938 !26412148
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suck abstract from ncbi


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pmid26412148
      Sci+Rep 2015 ; 5 (ä): 14570
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  • Ursolic acid exerts anti-cancer activity by suppressing vaccinia-related kinase 1-mediated damage repair in lung cancer cells #MMPMID26412148
  • Kim SH ; Ryu HG ; Lee J ; Shin J ; Harikishore A ; Jung HY ; Kim YS ; Lyu HN ; Oh E ; Baek NI ; Choi KY ; Yoon HS ; Kim KT
  • Sci Rep 2015[Sep]; 5 (ä): 14570 PMID26412148 show ga
  • Many mitotic kinases have been targeted for the development of anti-cancer drugs, and inhibitors of these kinases have been expected to perform well for cancer therapy. Efforts focused on selecting good targets and finding specific drugs to target are especially needed, largely due to the increased frequency of anti-cancer drugs used in the treatment of lung cancer. Vaccinia-related kinase 1 (VRK1) is a master regulator in lung adenocarcinoma and is considered a key molecule in the adaptive pathway, which mainly controls cell survival. We found that ursolic acid (UA) inhibits the catalytic activity of VRK1 via direct binding to the catalytic domain of VRK1. UA weakens surveillance mechanisms by blocking 53BP1 foci formation induced by VRK1 in lung cancer cells, and possesses synergistic anti-cancer effects with DNA damaging drugs. Taken together, UA can be a good anti-cancer agent for targeted therapy or combination therapy with DNA damaging drugs for lung cancer patients.
  • |Animals [MESH]
  • |Antineoplastic Agents, Phytogenic/chemistry/*pharmacology [MESH]
  • |Binding Sites [MESH]
  • |Catalytic Domain [MESH]
  • |Cell Line, Tumor [MESH]
  • |DNA Damage/drug effects [MESH]
  • |Disease Models, Animal [MESH]
  • |Doxorubicin/pharmacology [MESH]
  • |Drug Synergism [MESH]
  • |Enzyme Activation/drug effects [MESH]
  • |Humans [MESH]
  • |Intracellular Signaling Peptides and Proteins/antagonists & inhibitors/chemistry/*metabolism [MESH]
  • |Lung Neoplasms/drug therapy/*metabolism/pathology [MESH]
  • |Models, Molecular [MESH]
  • |Molecular Conformation [MESH]
  • |Nuclear Magnetic Resonance, Biomolecular [MESH]
  • |Protein Binding [MESH]
  • |Protein Interaction Domains and Motifs [MESH]
  • |Protein Serine-Threonine Kinases/antagonists & inhibitors/chemistry/*metabolism [MESH]
  • |Triterpenes/chemistry/*pharmacology [MESH]
  • |Ursolic Acid [MESH]


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