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1. Synthesis and Biological Evaluation of Oleanolic Acid Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B | |||
Li Hui,Zou-Hui,Gao Lixin,Liu Ting,Yang Fan,Li Jingya,Li Jia,Qiu Wen-Wei,Tang Jie | |||
Pharmacy 18 January 2012 | |||
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Abstract:A series of oleanolic acid (OA) derivatives have been synthesized and their inhibitory effects on PTP1B, TCPTP and related PTPs are evaluated. Some compounds with five-membered heterocyclic ring fused at C-2, C-3 positions showed a dramatic increase in inhibition, the two most potent PTP1B inhibitors 19 (IC50 = 0.91 μM) and 21 (IC50 = 0.98 μM) showed about 3-fold more potent than lead compound OA. Some compounds with C-ring modified showed high selectivity for PTP1B over TCPTP, among them, 50 possessed the best selectivity of 6.6-fold. | |||
TO cite this article:Li Hui,Zou-Hui,Gao Lixin, et al. Synthesis and Biological Evaluation of Oleanolic Acid Derivatives as Novel Inhibitors of Protein Tyrosine Phosphatase 1B[OL].[18 January 2012] http://en.paper.edu.cn/en_releasepaper/content/4463053 |
2. Modeling the Interaction between Glycogen Synthase Kinase 3β (GSK-3β) and Its Non-ATP Competitive Inhibitors | |||
Yong Chu,Keng-Chang Tsai,Deyong Ye,Minyong Li | |||
Pharmacy 27 September 2009 | |||
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Abstract:Glycogen synthase kinase-3 (GSK-3) plays an important role in a diverse number of regulatory pathways. GSK-3 inhibitors, particularly the non-ATP-competitive inhibitors, have been evaluated as promising drug candidates for a lot of unmet pathologies, such as Alzheimer’s disease and diabetes. In this paper, a molecular docking study with the published GSK-3β crystal structure and receptor-based pharmacophore modeling of four highly active non-ATP-competitive GSK-3 inhibitors were performed by DOCK 5.4 and Catalyst 4.11, respectively. The results could provide an exquisite understanding on their mechanism of interaction within the non-ATP-binding pocket of GSK-3β, meanwhile the finding of the common properties shared by these pharmacological inhibitors of GSK-3β could be helpful to further chemical optimization of such potent drug candidates. | |||
TO cite this article:Yong Chu,Keng-Chang Tsai,Deyong Ye, et al. Modeling the Interaction between Glycogen Synthase Kinase 3β (GSK-3β) and Its Non-ATP Competitive Inhibitors[OL].[27 September 2009] http://en.paper.edu.cn/en_releasepaper/content/35514 |
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