Effective degradation of EGFR<sup>L858R+T790M</sup> mutant proteins by CRBN-based PROTACs through both proteosome and autophagy/lysosome degradation systems.

Qu, Xiaojuan; Liu, Haixia; Song, Xiaoling; Sun, Ning; Zhong, Hui; Qiu, Xing; Yang, Xiaobao; Jiang, Biao

Effective degradation of EGFR^L858R+T790M mutant proteins by CRBN-based PROTACs through both proteosome and autophagy/lysosome degradation systems.

Qu, Xiaojuan; Liu, Haixia; Song, Xiaoling; Sun, Ning; Zhong, Hui; Qiu, Xing; Yang, Xiaobao; Jiang, Biao.

Afiliação

Qu X; Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Shanghai, 201210, China; School of Life Science, ShanghaiTech University, China; University of Chinese Academy of Sciences, Beijing, 100049, China.
Liu H; Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Shanghai, 201210, China; School of Physical Science and Technology, ShanghaiTech University, China; University of Chinese Academy of Sciences, Beijing, 100049, China.
Song X; Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Shanghai, 201210, China. Electronic address: songxl@shanghaitech.edu.cn.
Sun N; Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Shanghai, 201210, China.
Zhong H; Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Shanghai, 201210, China; School of Pharmaceutical Engineering and Life Science, Changzhou University, Jiangsu, 213164, China.
Qiu X; Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Shanghai, 201210, China; Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China.
Yang X; Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Shanghai, 201210, China. Electronic address: yangxb@shanghaitech.edu.cn.
Jiang B; Shanghai Institute for Advanced Immunochemical Studies, ShanghaiTech University, 393 Middle Huaxia Road, Shanghai, 201210, China; Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, 345 Lingling Road, Shanghai, 200032, China. Electronic address: jiangbiao@shanghaitech.edu.cn.

Eur J Med Chem ; 218: 113328, 2021 Jun 05.

Article em En | MEDLINE | ID: mdl-33773286

Assuntos

Autofagia/efeitos dos fármacos; Morfolinas/farmacologia; Complexo de Endopeptidases do Proteassoma/metabolismo; Inibidores de Proteínas Quinases/farmacologia; Talidomida/análogos & derivados; Apoptose/efeitos dos fármacos; Linhagem Celular; Proliferação de Células/efeitos dos fármacos; Relação Dose-Resposta a Droga; Receptores ErbB/antagonistas & inibidores; Receptores ErbB/genética; Receptores ErbB/metabolismo; Humanos; Lisossomos/efeitos dos fármacos; Estrutura Molecular; Morfolinas/síntese química; Morfolinas/química; Mutação; Inibidores de Proteínas Quinases/síntese química; Inibidores de Proteínas Quinases/química; Relação Estrutura-Atividade; Talidomida/síntese química; Talidomida/química; Talidomida/farmacologia

Palavras-chave

Autophagy/ lysosome; Degradation; EGFR; Non-small cell lung cancer; PROTAC; Resistance; T790M

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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Autofagia / Talidomida / Morfolinas / Complexo de Endopeptidases do Proteassoma / Inibidores de Proteínas Quinases Limite: Humans Idioma: En Revista: Eur J Med Chem Ano de publicação: 2021 Tipo de documento: Article País de afiliação: China

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