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Identification of lipid-like salicylic acid-based derivatives as potent and membrane-permeable PTP1B inhibitors.
Li, Liang; Tavallaie, Mojdeh S; Xie, Fangzhou; Xia, Yu; Liang, Yaoyao; Jiang, Faqin; Fu, Lei.
Afiliação
  • Li L; Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University (SJTU), 800 Dongchuan Road, Shanghai 200240, China.
  • Tavallaie MS; Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University (SJTU), 800 Dongchuan Road, Shanghai 200240, China.
  • Xie F; Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University (SJTU), 800 Dongchuan Road, Shanghai 200240, China.
  • Xia Y; Viva Biotech (Shanghai) Limited, Shanghai 201203, China.
  • Liang Y; Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University (SJTU), 800 Dongchuan Road, Shanghai 200240, China.
  • Jiang F; Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University (SJTU), 800 Dongchuan Road, Shanghai 200240, China.
  • Fu L; Shanghai Key Laboratory for Molecular Engineering of Chiral Drugs, School of Pharmacy, Shanghai Jiao Tong University (SJTU), 800 Dongchuan Road, Shanghai 200240, China. Electronic address: leifu@sjtu.edu.cn.
Bioorg Chem ; 93: 103296, 2019 12.
Article em En | MEDLINE | ID: mdl-31585268
Developing protein tyrosine phosphatase-1B (PTP1B) inhibitors is an important strategy to treat type 2 diabetes mellitus (T2DM). Most existing ionic PTP1B inhibitors aren't of clinical useful due to their low cell-permeability, however. Herein, we introduced a series of lipid-like acid-based (salicylic acid) modules to prepare PTP1B inhibitors, and demonstrated a marked improvement of cell-permeability while maintaining excellent PTP1B inhibitory activity (e.g. compound B12D, IC50 = 0.37 µM against PTP1B and Papp = 1.5 × 10-6 cm/s). We believe that this strategy can be widely utilized to modify potent lead compounds with low cell-permeability.
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ácido Salicílico / Inibidores Enzimáticos / Proteína Tirosina Fosfatase não Receptora Tipo 1 / Lipídeos Tipo de estudo: Diagnostic_studies Limite: Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2019 Tipo de documento: Article País de afiliação: China

Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Ácido Salicílico / Inibidores Enzimáticos / Proteína Tirosina Fosfatase não Receptora Tipo 1 / Lipídeos Tipo de estudo: Diagnostic_studies Limite: Humans Idioma: En Revista: Bioorg Chem Ano de publicação: 2019 Tipo de documento: Article País de afiliação: China