Literature DB >> 25225654

Virtual screening and optimization of Type II inhibitors of JAK2 from a natural product library.

Dik-Lung Ma1, Daniel Shiu-Hin Chan, Guo Wei, Hai-Jing Zhong, Hui Yang, Lai To Leung, Elizabeth A Gullen, Pauline Chiu, Yung-Chi Cheng, Chung-Hang Leung.   

Abstract

Amentoflavone has been identified as a JAK2 inhibitor by structure-based virtual screening of a natural product library. In silico optimization using the DOLPHIN model yielded analogues with enhanced potency against JAK2 activity and HCV activity in cellulo. Molecular modeling and kinetic experiments suggested that the analogues may function as Type II inhibitors of JAK2.

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Year:  2014        PMID： 25225654      PMCID： PMC4521218          DOI： 10.1039/c4cc04498c

Source DB:  PubMed          Journal:  Chem Commun (Camb)        ISSN： 1359-7345            Impact factor:   6.222


  13 in total

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3.  Hepatitis C virus (HCV) constitutively activates STAT-3 via oxidative stress: role of STAT-3 in HCV replication.

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4.  The structural basis of Janus kinase 2 inhibition by a potent and specific pan-Janus kinase inhibitor.

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Review 7.  Janus kinases in immune cell signaling.

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8.  Hepatitis C virus core protein differently regulates the JAK-STAT signaling pathway under interleukin-6 and interferon-gamma stimuli.

Authors:  Atsushi Hosui; Kazuyoshi Ohkawa; Hisashi Ishida; Aki Sato; Fumihiko Nakanishi; Keiji Ueda; Tetsuo Takehara; Akinori Kasahara; Yutaka Sasaki; Masatsugu Hori; Norio Hayashi
Journal:  J Biol Chem       Date:  2003-05-22       Impact factor: 5.157

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10.  Activation of STAT3 by the hepatitis C virus core protein leads to cellular transformation.

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  10 in total

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6.  A natural product-like JAK2/STAT3 inhibitor induces apoptosis of malignant melanoma cells.

Authors:  Ke-Jia Wu; Jie-Min Huang; Hai-Jing Zhong; Zhen-Zhen Dong; Kasipandi Vellaisamy; Jin-Jian Lu; Xiu-Ping Chen; Pauline Chiu; Daniel W J Kwong; Quan-Bin Han; Dik-Lung Ma; Chung-Hang Leung
Journal:  PLoS One       Date:  2017-06-01       Impact factor: 3.240

7.  Aurone derivatives as Vps34 inhibitors that modulate autophagy.

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Review 9.  Insights Into Amentoflavone: A Natural Multifunctional Biflavonoid.

Authors:  Xifeng Xiong; Nan Tang; Xudong Lai; Jinli Zhang; Weilun Wen; Xiaojian Li; Aiguo Li; Yanhua Wu; Zhihe Liu
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  10 in total

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