Discovery of novel, high potent, ABC type PTP1B inhibitors with TCPTP selectivity and cellular activity

Protein tyrosine phosphatase 1B (PTP1B) as a key negative regulator of both insulin and leptin receptor pathways has been an attractive therapeutic target for the treatment of type 2 diabetes mellitus (T2DM) and obesity. With the goal of enhancing potency and selectivity of the PTP1B inhibitors, a s...

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Veröffentlicht in:	European journal of medicinal chemistry 2016-08, Vol.118, p.27-33
Hauptverfasser:	Liu, Peihong, Du, Yongli, Song, Lianhua, Shen, Jingkang, Li, Qunyi
Format:	Artikel
Sprache:	eng
Schlagworte:	ABC type PTP1B inhibitor Animals CHO Cells Cricetinae Cricetulus Drug Design Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology Glucose - metabolism Humans Methyl salicylate derivatives Molecular Docking Simulation Protein Conformation Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors Protein Tyrosine Phosphatase, Non-Receptor Type 1 - chemistry Protein Tyrosine Phosphatase, Non-Receptor Type 1 - metabolism Protein Tyrosine Phosphatase, Non-Receptor Type 11 - metabolism Protein Tyrosine Phosphatase, Non-Receptor Type 2 - metabolism Protein Tyrosine Phosphatase, Non-Receptor Type 6 - metabolism Structure-Activity Relationship Substrate Specificity Type 2 diabetes mellitus
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