Design, synthesis, and biological evaluation of Bcr-Abl PROTACs to overcome T315I mutation.

Jiang, Liang; Wang, Yuting; Li, Qian; Tu, Zhengchao; Zhu, Sihua; Tu, Sanfang; Zhang, Zhang; Ding, Ke; Lu, Xiaoyun

Jiang, Liang; Wang, Yuting; Li, Qian; Tu, Zhengchao; Zhu, Sihua; Tu, Sanfang; Zhang, Zhang; Ding, Ke; Lu, Xiaoyun.

Afiliação

Jiang L; International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of China, School of Pharmacy, Jinan University, Guangzhou 510632, China.
Wang Y; International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of China, School of Pharmacy, Jinan University, Guangzhou 510632, China.
Li Q; International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of China, School of Pharmacy, Jinan University, Guangzhou 510632, China.
Tu Z; International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of China, School of Pharmacy, Jinan University, Guangzhou 510632, China.
Zhu S; International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of China, School of Pharmacy, Jinan University, Guangzhou 510632, China.
Tu S; Department of Hematology, Zhujiang Hospital, Southern Medical University, Guangzhou 510282, China.
Zhang Z; International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of China, School of Pharmacy, Jinan University, Guangzhou 510632, China.
Ding K; International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of China, School of Pharmacy, Jinan University, Guangzhou 510632, China.
Lu X; International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development, Ministry of Education (MOE) of China, School of Pharmacy, Jinan University, Guangzhou 510632, China.

Acta Pharm Sin B ; 11(5): 1315-1328, 2021 May.

Article em En | MEDLINE | ID: mdl-34094836

Palavras-chave

ALL, acute lymphoblastic leukemia; CML; CML, chronic myeloid leukemia; CRBN, cereblon; Clinical resistance; Co-IP, co-immunoprecipitation; DR, degradation rate; Degradation; IC50, cellular inhibition; LSCs, leukemic stem cells; NMPA, National Medical Products Administration; PROTAC; PROTAC, proteolysis-targeting chimeric; Ph+, Philadelphia chromosome; T315I mutation; T315I, threonine 315 to isoleucine 315; TGI, tumor growth inhibition; VHL, von Hippel-Lindau; cIAP1, cellular inhibitor of apoptosis protein 1

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Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: Acta Pharm Sin B Ano de publicação: 2021 Tipo de documento: Article País de afiliação: China

Texto completo

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XML

PubMed Links

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Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: Acta Pharm Sin B Ano de publicação: 2021 Tipo de documento: Article País de afiliação: China