Browsing by Author "Wang, Jinhua"

Now showing items 1-9 of 9

    • Characterization of WZ4003 and HTH-01-015 as selective inhibitors of the LKB1-tumour-suppressor-activated NUAK kinases 

      Banerjee, Sourav; Buhrlage, Sara J.; Huang, Hai-Tsang; Deng, Xianming; Zhou, Wenjun; Wang, Jinhua; Traynor, Ryan; Prescott, Alan R.; Alessi, Dario R.; Gray, Nathanael S. (Portland Press Ltd., 2014)
      The related NUAK1 and NUAK2 are members of the AMPK (AMP-activated protein kinase) family of protein kinases that are activated by the LKB1 (liver kinase B1) tumour suppressor kinase. Recent work suggests they play important ...

    • Discovery of 3,5-Diamino-1,2,4-triazole Ureas as Potent Anaplastic Lymphoma Kinase Inhibitors 

      Deng, Xianming; Wang, Jinhua; Zhang, Jianming; Sim, Taebo; Kim, Nam Doo; Sasaki, Takaaki; Luther, William; George, Rani E.; Jänne, Pasi A.; Gray, Nathanael Schiander (American Chemical Society, 2011)
      A series of novel 3,5-diamino-1,2,4-triazole benzyl ureas was identified as having potent anaplastic lymphoma kinase (ALK) inhibition exemplified by 15a, 20a, and 23a, which exhibited antiproliferative IC50 values of 70, ...

    • Discovery of a Potent and Selective DDR1 Receptor Tyrosine Kinase Inhibitor 

      Kim, Hyung-Gu; Tan, Li; Weisberg, Ellen L.; Liu, Feiyang; Canning, Peter; Choi, Hwan Geun; Ezell, Scott A.; Wu, Hong; Zhao, Zheng; Wang, Jinhua; Mandinova, Anna; Griffin, James D.; Bullock, Alex N.; Liu, Qingsong; Lee, Sam W.; Gray, Nathanael S. (American Chemical Society, 2013)
      The DDR1 receptor tyrosine kinase is activated by matrix collagens and has been implicated in numerous cellular functions such as proliferation, differentiation, adhesion, migration, and invasion. Here we report the discovery ...

    • Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma 

      Wu, Hong; Wang, Wenchao; Liu, Feiyang; Weisberg, Ellen L.; Tian, Bei; Chen, Yongfei; Li, Binhua; Wang, Aoli; Wang, Beilei; Zhao, Zheng; McMillin, Douglas W.; Hu, Chen; Li, Hong; Wang, Jinhua; Liang, Yanke; Buhrlage, Sara J.; Liang, Junting; Liu, Jing; Yang, Guang; Brown, Jennifer R.; Treon, Steven P.; Mitsiades, Constantine S.; Griffin, James D.; Liu, Qingsong; Gray, Nathanael S. (American Chemical Society, 2014)
      BTK is a member of the TEC family of non-receptor tyrosine kinases whose deregulation has been implicated in a variety of B-cell-related diseases. We have used structure-based drug design in conjunction with kinome profiling ...

    • Functional kinomics establishes a critical node of volume-sensitive cation-Cl− cotransporter regulation in the mammalian brain 

      Zhang, Jinwei; Gao, Geng; Begum, Gulnaz; Wang, Jinhua; Khanna, Arjun R.; Shmukler, Boris E.; Daubner, Gerrit M.; de los Heros, Paola; Davies, Paul; Varghese, Joby; Bhuiyan, Mohammad Iqbal H.; Duan, Jinjing; Zhang, Jin; Duran, Daniel; Alper, Seth L.; Sun, Dandan; Elledge, Stephen J.; Alessi, Dario R.; Kahle, Kristopher T. (Nature Publishing Group, 2016)
      Cell volume homeostasis requires the dynamically regulated transport of ions across the plasmalemma. While the ensemble of ion transport proteins involved in cell volume regulation is well established, the molecular ...

    • Ibrutinib selectively and irreversibly targets EGFR (L858R, Del19) mutant but is moderately resistant to EGFR (T790M) mutant NSCLC Cells 

      Wu, Hong; Wang, Aoli; Zhang, Wei; Wang, Beilei; Chen, Cheng; Wang, Wenchao; Hu, Chen; Ye, Zi; Zhao, Zheng; Wang, Li; Li, Xixiang; Yu, Kailin; Liu, Juan; Wu, Jiaxin; Yan, Xiao-E; Zhao, Peng; Wang, Jinhua; Wang, Chu; Weisberg, Ellen L.; Gray, Nathanael S.; Yun, Cai-Hong; Liu, Jing; Chen, Liang; Liu, Qingsong (Impact Journals LLC, 2015)
      Through comprehensive comparison study, we found that ibrutinib, a clinically approved covalent BTK kinase inhibitor, was highly active against EGFR (L858R, del19) mutant driven NSCLC cells, but moderately active to the ...

    • Identification of Novel Small Molecule Inhibitors of Oncogenic RET Kinase 

      Moccia, Marialuisa; Liu, Qingsong; Guida, Teresa; Federico, Giorgia; Brescia, Annalisa; Zhao, Zheng; Choi, Hwan Geun; Deng, Xianming; Tan, Li; Wang, Jinhua; Billaud, Marc; Gray, Nathanael S.; Carlomagno, Francesca; Santoro, Massimo (Public Library of Science, 2015)
      Oncogenic mutation of the RET receptor tyrosine kinase is observed in several human malignancies. Here, we describe three novel type II RET tyrosine kinase inhibitors (TKI), ALW-II-41-27, XMD15-44 and HG-6-63-01, that ...

    • A Landscape of Pharmacogenomic Interactions in Cancer 

      Iorio, Francesco; Knijnenburg, Theo A.; Vis, Daniel J.; Bignell, Graham R.; Menden, Michael P.; Schubert, Michael; Aben, Nanne; Gonçalves, Emanuel; Barthorpe, Syd; Lightfoot, Howard; Cokelaer, Thomas; Greninger, Patricia; van Dyk, Ewald; Chang, Han; de Silva, Heshani; Heyn, Holger; Deng, Xianming; Egan, Regina K.; Liu, Qingsong; Mironenko, Tatiana; Mitropoulos, Xeni; Richardson, Laura; Wang, Jinhua; Zhang, Tinghu; Moran, Sebastian; Sayols, Sergi; Soleimani, Maryam; Tamborero, David; Lopez-Bigas, Nuria; Ross-Macdonald, Petra; Esteller, Manel; Gray, Nathanael S.; Haber, Daniel A.; Stratton, Michael R.; Benes, Cyril H.; Wessels, Lodewyk F.A.; Saez-Rodriguez, Julio; McDermott, Ultan; Garnett, Mathew J. (Cell Press, 2016)
      Summary Systematic studies of cancer genomes have provided unprecedented insights into the molecular nature of cancer. Using this information to guide the development and application of therapies in the clinic is challenging. ...

    • SIKs control osteocyte responses to parathyroid hormone 

      Wein, Marc N.; Liang, Yanke; Goransson, Olga; Sundberg, Thomas B.; Wang, Jinhua; Williams, Elizabeth A.; O'Meara, Maureen J.; Govea, Nicolas; Beqo, Belinda; Nishimori, Shigeki; Nagano, Kenichi; Brooks, Daniel J.; Martins, Janaina S.; Corbin, Braden; Anselmo, Anthony; Sadreyev, Ruslan; Wu, Joy Y.; Sakamoto, Kei; Foretz, Marc; Xavier, Ramnik J.; Baron, Roland; Bouxsein, Mary L.; Gardella, Thomas J.; Divieti-Pajevic, Paola; Gray, Nathanael S.; Kronenberg, Henry M. (Nature Publishing Group, 2016)
      Parathyroid hormone (PTH) activates receptors on osteocytes to orchestrate bone formation and resorption. Here we show that PTH inhibition of SOST (sclerostin), a WNT antagonist, requires HDAC4 and HDAC5, whereas PTH ...