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  1. Artikel ; Online: Targeting EGFR degradation by autophagosome degraders.

    Zhu, ZhongFeng / Li, Jiaying / Shen, Shujun / Al-Furas, Hawaa / Li, Shengrong / Tong, Yichen / Li, Yi / Zeng, Yucheng / Feng, Qianyi / Chen, Kaiyue / Ma, Nan / Zhou, Fengtao / Zhang, Zhang / Li, Zhengqiu / Pang, Jiyan / Ding, Ke / Xu, Fang

    European journal of medicinal chemistry

    2024  Band 270, Seite(n) 116345

    Abstract: Several generations of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors have been developed for the treatment of non-small cell lung cancer (NSCLC) in clinic. However, emerging drug resistance mediated by new EGFR mutations or ... ...

    Abstract Several generations of epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors have been developed for the treatment of non-small cell lung cancer (NSCLC) in clinic. However, emerging drug resistance mediated by new EGFR mutations or activations by pass, leads to malignant progression of NSCLC. Proteolysis targeting chimeras (PROTACs) have been utilized to overcome the drug resistance acquired by mutant EGFR, newly potent and selective degraders are still need to be developed for clinical applications. Herein, we developed autophagosome-tethering compounds (ATTECs) in which EGFR can be anchored to microtubule-associated protein-1 light chain-3B (LC3B) on the autophagosome with the assistance of the LC3 ligand GW5074. A series of EGFR-ATTECs have been designed and synthesized. Biological evaluations showed that these compounds could degrade EGFR and exhibited moderate inhibitory effects on certain NSCLC cell lines. The ATTEC 12c potently induced the degradation of EGFR with a DC
    Mesh-Begriff(e) Humans ; Carcinoma, Non-Small-Cell Lung/drug therapy ; Carcinoma, Non-Small-Cell Lung/pathology ; Lung Neoplasms/pathology ; Cell Proliferation ; Autophagosomes/metabolism ; Protein Kinase Inhibitors/pharmacology ; Protein Kinase Inhibitors/therapeutic use ; Cell Line, Tumor ; ErbB Receptors ; Mutation ; Drug Resistance, Neoplasm
    Chemische Substanzen Protein Kinase Inhibitors ; ErbB Receptors (EC 2.7.10.1) ; EGFR protein, human (EC 2.7.10.1)
    Sprache Englisch
    Erscheinungsdatum 2024-03-26
    Erscheinungsland France
    Dokumenttyp Journal Article
    ZDB-ID 188597-2
    ISSN 1768-3254 ; 0009-4374 ; 0223-5234
    ISSN (online) 1768-3254
    ISSN 0009-4374 ; 0223-5234
    DOI 10.1016/j.ejmech.2024.116345
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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  2. Artikel: [Effect of environmental factors on growth of Huperzia serrata].

    Wang, Zhi-an / Xu, Jian-zhong / Yu, Xue-ping / Shen, Shu-jun

    Zhongguo Zhong yao za zhi = Zhongguo zhongyao zazhi = China journal of Chinese materia medica

    2008  Band 33, Heft 15, Seite(n) 1814–1816

    Abstract: Objective: To establish and optimize the cultivation systems for wild Huperzia serrata, through assessing the effects of environmental factors on its growth.: Method: H. serrata was planted under natural field condition, the growth status of H. ... ...

    Abstract Objective: To establish and optimize the cultivation systems for wild Huperzia serrata, through assessing the effects of environmental factors on its growth.
    Method: H. serrata was planted under natural field condition, the growth status of H. serrata under different light intensities, temperatures, relative humidity (R. H.), fertilizer levels, and so on were investigated and analyzed.
    Result: H. serrata grew nicely under following environmental conditions: temperature ranging from 18.9-26.3 degrees C, R. H. ranging from 81%-90% and 1330-3000 lx light intensity. A cultivation system, in which H. serrata was planted in the bamboo forest and did not occupy the arable land, was established through the study.
    Conclusion: Concluded that light intensity and R. H are the two factors which greatly confine the growth of H. serrata. As long as the levels of the above two factors meets the demands, H. serrata could be cultivated.
    Mesh-Begriff(e) Fertilizers ; Humidity ; Huperzia/growth & development ; Light ; Temperature
    Chemische Substanzen Fertilizers
    Sprache Chinesisch
    Erscheinungsdatum 2008-08
    Erscheinungsland China
    Dokumenttyp English Abstract ; Journal Article
    ZDB-ID 1004649-5
    ISSN 1001-5302 ; 0254-0029
    ISSN 1001-5302 ; 0254-0029
    Datenquelle MEDical Literature Analysis and Retrieval System OnLINE

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