Search Results - "Luo, Lusong"

Discovery of Zanubrutinib (BGB-3111), a Novel, Potent, and Selective Covalent Inhibitor of Bruton’s Tyrosine Kinase by Guo, Yunhang, Liu, Ye, Hu, Nan, Yu, Desheng, Zhou, Changyou, Shi, Gongyin, Zhang, Bo, Wei, Min, Liu, Junhua, Luo, Lusong, Tang, Zhiyu, Song, Huipeng, Guo, Yin, Liu, Xuesong, Su, Dan, Zhang, Shuo, Song, Xiaomin, Zhou, Xing, Hong, Yuan, Chen, Shuaishuai, Cheng, Zhenzhen, Young, Steve, Wei, Qiang, Wang, Haisheng, Wang, Qiuwen, Lv, Lei, Wang, Fan, Xu, Haipeng, Sun, Hanzi, Xing, Haimei, Li, Na, Zhang, Wei, Wang, Zhongbo, Liu, Guodong, Sun, Zhijian, Zhou, Dongping, Li, Wei, Liu, Libin, Wang, Lai, Wang, Zhiwei

“…Aberrant activation of Bruton’s tyrosine kinase (BTK) plays an important role in pathogenesis of B-cell lymphomas, suggesting that inhibition of BTK is useful…”
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Discovery and Preclinical Characterization of GSK1278863 (Daprodustat), a Small Molecule Hypoxia Inducible Factor-Prolyl Hydroxylase Inhibitor for Anemia by Ariazi, Jennifer L, Duffy, Kevin J, Adams, David F, Fitch, Duke M, Luo, Lusong, Pappalardi, Melissa, Biju, Mangatt, DiFilippo, Erin Hugger, Shaw, Tony, Wiggall, Ken, Erickson-Miller, Connie

“…Decreased erythropoietin (EPO) production, shortened erythrocyte survival, and other factors reducing the response to EPO contribute to anemia in patients who…”
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Epigallocatechin gallate (EGCG), a major component of green tea, is a dual phosphoinositide-3-kinase/mTOR inhibitor by Van Aller, Glenn S., Carson, Jeff D., Tang, Wei, Peng, Hao, Zhao, Lin, Copeland, Robert A., Tummino, Peter J., Luo, Lusong

“…► Epigallocatechin-3-gallate (EGCG) is an ATP-competitive inhibitor of PI3K and mTOR with Ki values around 300nM. ► EGCG inhibits cell proliferation and AKT…”
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BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal Cancers by Tang, Zhiyu, Yuan, Xi, Du, Rong, Cheung, Shing-Hu, Zhang, Guoliang, Wei, Jing, Zhao, Yuan, Feng, Yingcai, Peng, Hao, Zhang, Yi, Du, Yunguang, Hu, Xiaoxia, Gong, Wenfeng, Liu, Yong, Gao, Yajuan, Liu, Ye, Hao, Rui, Li, Shengjian, Wang, Shaohui, Ji, Jiafu, Zhang, Lianhai, Li, Shuangxi, Sutton, David, Wei, Min, Zhou, Changyou, Wang, Lai, Luo, Lusong

“…Oncogenic BRAF, which drives cell transformation and proliferation, has been detected in approximately 50% of human malignant melanomas and 5% to 15% of…”
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RAF dimer inhibition enhances the antitumor activity of MEK inhibitors in K‐RAS mutant tumors by Yuan, Xi, Tang, Zhiyu, Du, Rong, Yao, Zhan, Cheung, Shing‐Hu, Zhang, Xinwen, Wei, Jing, Zhao, Yuan, Du, Yunguang, Liu, Ye, Hu, Xiaoxia, Gong, Wenfeng, Liu, Yong, Gao, Yajuan, Huang, Zhiyue, Cao, Zongfu, Wei, Min, Zhou, Changyou, Wang, Lai, Rosen, Neal, Smith, Paul D., Luo, Lusong

“…The mutation of K‐RAS represents one of the most frequent genetic alterations in cancer. Targeting of downstream effectors of RAS, including of MEK and ERK,…”
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Discovery of a potent hedgehog pathway inhibitor capable of activating caspase8-dependent apoptosis by Chen, Qin, Zhang, Haoran, Wu, Meng, Wang, Qin, Luo, Lusong, Ma, Haikuo, Zhang, Xiaohu, He, Sudan

“…Aberrant activation of Hedgehog (Hh) signaling is associated with the development of numerous human cancers. Vismodegib is the first Hh inhibitor approved for…”
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Mechanism of Inhibition of Human KSP by Ispinesib by Lad, Latesh, Luo, Lusong, Carson, Jeffrey D., Wood, Kenneth W., Hartman, James J., Copeland, Robert A., Sakowicz, Roman

“…KSP, also known as HsEg5, is a kinesin that plays an essential role in the formation of a bipolar mitotic spindle and is required for cell cycle progression…”
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Novel ATP-Competitive Kinesin Spindle Protein Inhibitors by Parrish, Cynthia A, Adams, Nicholas D, Auger, Kurt R, Burgess, Joelle L, Carson, Jeffrey D, Chaudhari, Amita M, Copeland, Robert A, Diamond, Melody A, Donatelli, Carla A, Duffy, Kevin J, Faucette, Leo F, Finer, Jeffrey T, Huffman, William F, Hugger, Erin D, Jackson, Jeffrey R, Knight, Steven D, Luo, Lusong, Moore, Michael L, Newlander, Ken A, Ridgers, Lance H, Sakowicz, Roman, Shaw, Antony N, Sung, Chiu-Mei M, Sutton, David, Wood, Kenneth W, Zhang, Shu-Yun, Zimmerman, Michael N, Dhanak, Dashyant

“…Kinesin spindle protein (KSP), an ATPase responsible for spindle pole separation during mitosis that is present only in proliferating cells, has become a novel…”
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Discovery of the First Potent and Selective Inhibitor of Centromere-Associated Protein E: GSK923295 by Qian, Xiangping, McDonald, Andrew, Zhou, Han-Jie, Adams, Nicholas D, Parrish, Cynthia A, Duffy, Kevin J, Fitch, Duke M, Tedesco, Rosanna, Ashcraft, Luke W, Yao, Bing, Jiang, Hong, Huang, Jennifer K, Marin, Melchor V, Aroyan, Carrie E, Wang, Jianchao, Ahmed, Seyed, Burgess, Joelle L, Chaudhari, Amita M, Donatelli, Carla A, Darcy, Michael G, Ridgers, Lance H, Newlander, Ken A, Schmidt, Stanley J, Chai, Deping, Colón, Mariela, Zimmerman, Michael N, Lad, Latesh, Sakowicz, Roman, Schauer, Stephen, Belmont, Lisa, Baliga, Ramesh, Pierce, Daniel W, Finer, Jeffrey T, Wang, Zhengping, Morgan, Bradley P, Morgans, David J, Auger, Kurt R, Sung, Chiu-Mei, Carson, Jeff D, Luo, Lusong, Hugger, Erin D, Copeland, Robert A, Sutton, David, Elliott, John D, Jackson, Jeffrey R, Wood, Kenneth W, Dhanak, Dashyant, Bergnes, Gustave, Knight, Steven D

“…Inhibition of mitotic kinesins represents a novel approach for the discovery of a new generation of anti-mitotic cancer chemotherapeutics. We report here the…”
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Timing of Epimerization and Condensation Reactions in Nonribosomal Peptide Assembly Lines:  Kinetic Analysis of Phenylalanine Activating Elongation Modules of Tyrocidine Synthetase B by Luo, Lusong, Kohli, Rahul M, Onishi, Megumi, Linne, Uwe, Marahiel, Mohamed A, Walsh, Christopher T

“…The cyclic decapeptide antibiotic tyrocidine has d-Phe residues at positions 1 and 4, produced during peptide chain growth from l-Phe residues by 50 kDa…”
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Abstract 1298: CD40L-CD40 signaling on B-cell lymphoma response to BTK inhibitors by Sun, Zhijian, Luo, Lusong

“…Abstract The aberrant activation of B cells receptor (BCR) signaling plays an essential role in the pathogenesis of B-cell lymphomas. Targeting BCR signaling…”
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Abstract C62: Identification of GSK2126458, a highly potent inhibitor of phosphoinositide 3-kinase (PI3K) and the mammalian target of rapamycin (mTOR) by Knight, Steven D., Adams, Nicholas D., Burgess, Joelle L., Chaudhari, Amita M., Darcy, Michael G., Donatelli, Carla A., Newlander, Ken A., Parrish, Cynthia A., Ridgers, Lance H., Sarpong, Martha A., Schmidt, Stanley J., Van Aller, Glenn, Carson, Jeff D., Elkins, Patricia A., Diamond, Melody, Gardiner, Christine M., Garver, Eric, Luo, Lusong, Raha, Kaushik, Sung, Chiu-Mei, Tummino, Peter J., Auger, Kurt R., Dhanak, Dashyant

“…Abstract Phosphoinositide 3-kinase (PI3K) is a critical regulator of cell growth and transformation and its signaling pathway is one of the most commonly…”
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BRAF Mutants Evade ERK-Dependent Feedback by Different Mechanisms that Determine Their Sensitivity to Pharmacologic Inhibition by Yao, Zhan, Torres, Neilawattie M., Tao, Anthony, Gao, Yijun, Luo, Lusong, Li, Qi, de Stanchina, Elisa, Abdel-Wahab, Omar, Solit, David B., Poulikakos, Poulikos I., Rosen, Neal

“…ERK signaling requires RAS-induced RAF dimerization and is limited by feedback. Activated BRAF mutants evade feedback inhibition of RAS by either of two…”
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C-Methyltransferase and Cyclization Domain Activity at the Intraprotein PK/NRP Switch Point of Yersiniabactin Synthetase by Miller, Deborah Ann, Walsh, Christopher T., Luo, Lusong

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Phase I, Open-Label, Dose-Escalation/Dose-Expansion Study of Lifirafenib (BGB-283), an RAF Family Kinase Inhibitor, in Patients With Solid Tumors by Desai, Jayesh, Gan, Hui, Barrow, Catherine, Jameson, Michael, Atkinson, Victoria, Haydon, Andrew, Millward, Michael, Begbie, Stephen, Brown, Michael, Markman, Ben, Patterson, William, Hill, Andrew, Horvath, Lisa, Nagrial, Adnan, Richardson, Gary, Jackson, Christopher, Friedlander, Michael, Parente, Phillip, Tran, Ben, Wang, Lai, Chen, Yunxin, Tang, Zhiyu, Huang, Wendy, Wu, John, Zeng, Dewan, Luo, Lusong, Solomon, Benjamin

“…Lifirafenib is an investigational, reversible inhibitor of B-RAF , wild-type A-RAF, B-RAF, C-RAF, and EGFR. This first-in-human, phase I,…”
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Discovery of potent and novel smoothened antagonists via structure-based virtual screening and biological assays by Lu, Wenfeng, Zhang, Dihua, Ma, Haikuo, Tian, Sheng, Zheng, Jiyue, Wang, Qin, Luo, Lusong, Zhang, Xiaohu

“…The Hedgehog (Hh) signaling pathway plays a critical role in controlling patterning, growth and cell migration during embryonic development. Aberrant…”
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Discovery of Pamiparib (BGB-290), a Potent and Selective Poly (ADP-ribose) Polymerase (PARP) Inhibitor in Clinical Development by Wang, Hexiang, Ren, Bo, Liu, Ye, Jiang, Beibei, Guo, Yin, Wei, Min, Luo, Lusong, Kuang, Xianzhao, Qiu, Ming, Lv, Lei, Xu, Hong, Qi, Ruipeng, Yan, Huibin, Xu, Dexu, Wang, Zhiwei, Huo, Chang-Xin, Zhu, Yutong, Zhao, Yuan, Wu, Yiyuan, Qin, Zhen, Su, Dan, Tang, Tristin, Wang, Fan, Sun, Xuebing, Feng, Yingcai, Peng, Hao, Wang, Xing, Gao, Yajuan, Liu, Yong, Gong, Wenfeng, Yu, Fenglong, Liu, Xuesong, Wang, Lai, Zhou, Changyou

“…Poly (ADP-ribose) polymerase (PARP) plays a significant role in DNA repair responses; therefore, this enzyme is targeted by PARP inhibitors in cancer therapy…”
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Abstract 5496: Effect of BTK inhibitors on differentiation of human monocyte-derived dendritic cells by Sun, Zhijian, Zhou, Dongping, Luo, Lusong

“…Abstract Dendritic cells (DCs) are primary antigen-presenting cells (APCs), which process tumor antigen and present it on the cell surface to the T cells of…”
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Modulating Electron Density in the Bound Product, 4-Hydroxybenzoyl-CoA, by Mutations in 4-Chlorobenzoyl-CoA Dehalogenase Near the 4-Hydroxy Group by Dong, Jian, Xiang, Hong, Luo, Lusong, Dunaway-Mariano, Debra, Carey, Paul R

“…The enzyme 4-chlorobenzoyl-CoA dehalogenase hydrolyzes 4-chlorobenzoyl-CoA (4-CBA-CoA) to 4-hydroxybenzoyl-CoA (4-HBA-CoA). Biochemical and crystallographic…”
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Design, synthesis, and evaluation of pyrrolidine based CXCR4 antagonists with in vivo anti-tumor metastatic activity by Li, Zhanhui, Wang, Xu, Lin, Yu, Wang, Yujie, Wu, Shuwei, Xia, Kaijiang, Xu, Chen, Ma, Haikuo, Zheng, Jiyue, Luo, Lusong, Zhu, Fang, He, Sudan, Zhang, Xiaohu

“…The chemokine receptor CXCR4 has been proposed as a drug target based on its important functions in HIV infection, inflammation/autoimmune diseases and cancer…”
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