Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Weston, Lane"'
Autor:
Richard Tjhen, Noriko Uchiyama, Michiko Tawada, Yohei Kosugi, Satoshi Endo, Huikai Sun, Kei Masuda, Makoto Fushimi, Tatsuki Koike, Weston Lane
Publikováno v:
Journal of Medicinal Chemistry. 64:1103-1115
O-GlcNAcase (OGA) has received increasing attention as an attractive therapeutic target for tau-mediated neurodegenerative disorders; however, its role in these pathologies remains unclear. Therefore, potent chemical tools with favorable pharmacokine
Autor:
Yuichi Kajita, Shuhei Ikeda, Masato Yoshikawa, Hiromi Fukuda, Etsurou Watanabe, Jason Yano, Weston Lane, Maki Miyamoto, Tsuyoshi Ishii, Toshiya Nishi, Tatsuki Koike
Publikováno v:
Journal of medicinal chemistry. 65(4)
Cholesterol 24-hydroxylase (CH24H or CYP46A1) is a brain-specific cytochrome P450 enzyme that metabolizes cholesterol into 24
Autor:
Wei-Sheng, Huang, Feng, Li, Yongjin, Gong, Yun, Zhang, Willmen, Youngsaye, Yongjin, Xu, Xiaotian, Zhu, Matthew T, Greenfield, Anna, Kohlmann, Paul M, Taslimi, Angela, Toms, Stephan G, Zech, Tianjun, Zhou, Biplab, Das, Hyun G, Jang, Meera, Tugnait, Yihua E, Ye, Francois, Gonzalvez, Theresa E, Baker, Sara, Nadworny, Yaoyu, Ning, Scott D, Wardwell, Sen, Zhang, Alexandra E, Gould, Yongbo, Hu, Weston, Lane, Robert J, Skene, Hua, Zou, Tim, Clackson, Narayana I, Narasimhan, Victor M, Rivera, David C, Dalgarno, William C, Shakespeare
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 80:129084
In the treatment of non-small cell lung cancer (NSCLC), patients harboring exon 20 insertion mutations in the epidermal growth factor receptor (EGFR) gene (EGFR) have few effective therapies because this subset of mutants is generally resistant to mo
Autor:
Shuhei Ikeda, Yuichi Kajita, Maki Miyamoto, Kouta Matsumiya, Tsuyoshi Ishii, Toshiya Nishi, Sean C. Gay, Weston Lane, Cristian C. Constantinescu, David Alagille, Caroline Papin, Gilles Tamagnan, Takanobu Kuroita, Tatsuki Koike
Publikováno v:
European Journal of Medicinal Chemistry. 240:114612
Cholesterol 24-hydroxylase (CH24H, CYP46A1) is a cytochrome P450 family enzyme that maintains the homeostasis of brain cholesterol. Soticlestat, a potent and selective CH24H inhibitor, is in development as a therapeutic agent for Dravet syndrome and
Autor:
Fukuda Hiromi, Weston Lane, Shinichiro Matsunaga, Masayuki Gotoh, Tomohiro Kawamoto, Masashi Takahashi, Seiji Miwatashi, Sachiko Itono, Rei Okamoto, Satoko Unno, Kengo Okada, Takahiro Miyazaki, Toshimasa Tanaka, Hiroshi Sugimoto, Kumar Singh Saikatendu, Akira Kaieda, Yuri Hori, Terufumi Takagi, Shinji Morimoto, Bi-Ching Sang
Publikováno v:
ChemMedChem. 14:2093-2101
We identified novel potent inhibitors of p38 mitogen-activated protein (MAP) kinase using a structure-based design strategy, beginning with lead compound, 3-(butan-2-yl)-6-(2,4-difluoroanilino)-1,3-dihydro-2H-imidazo[4,5-b]pyridin-2-one (1). To enhan
Autor:
Osamu Kurasawa, Yasutomi Asano, Ke Li, Hiroshi Banno, Jun Fujimoto, Georgia Kefala, Gyorgy Snell, Irena Levin, Takuto Kojima, Ryo Mizojiri, Bi-Ching Sang, Richard Tjhen, Michael G. Klein, Scott Weston Lane, Isaac Hoffman, Tsuyoshi Ishii, Douglas R. Cary, Xin Liu, Akito Hata, Tadahiro Nambu, Yasuyuki Debori, Tomoya Sameshima, Terufumi Takagi, Steve C. Ding, Akito Nakamura, Maki Miyamoto
Publikováno v:
ACS Med Chem Lett
[Image: see text] General control nonderepressible 2 (GCN2) is a master regulator kinase of amino acid homeostasis and important for cancer survival in the tumor microenvironment under amino acid depletion. We initiated studies aiming at the discover
Autor:
Xingyue He, Mark G. Qian, Matthew O. Duffey, Larry Cohen, Michael D. Sintchak, Mi-Sook Kim, Jessica Riceberg, Vaishali Shindi, Kelly Connolly, Jianping Guo, Agatha Zawadzka, Rachel E. Gershman, Teresa A. Soucy, Neil Bence, Zhigen Hu, Xiaofeng Yang, Shumet A. Hailu, Nina Molchinova, Nanda Gulavita, Ji Zhang, Hirotake Mizutani, Keli Song, A D Patil, Scott Freeze, Jessica Grieves, Dylan Bradley England, Roushan Afroze, James J. Minissale, Anya Lublinsky, Mitsuhiro Ito, David Lok, Scott Weston Lane, William D. Mallender, Stephen Grossman, Kara Hoar, Nitya Durvasula, Bei-Ching Chuang, Yongbo Hu, Steven P. Langston, Sai M. Pulukuri, Miho Mizutani, Ryan Chau, Nancy Bump, Katherine M. Galvin, Christopher F. Claiborne, Paul D. Greenspan, He Xu, Gaulin Jeffrey L, Melissa Gallery, Douglas Bowman, Yana Wang, Koji Ono, Mcintyre Charles
Publikováno v:
Journal of medicinal chemistry. 64(5)
SUMOylation is a reversible post-translational modification that regulates protein function through covalent attachment of small ubiquitin-like modifier (SUMO) proteins. The process of SUMOylating proteins involves an enzymatic cascade, the first ste
Autor:
Michiko, Tawada, Makoto, Fushimi, Kei, Masuda, Huikai, Sun, Noriko, Uchiyama, Yohei, Kosugi, Weston, Lane, Richard, Tjhen, Satoshi, Endo, Tatsuki, Koike
Publikováno v:
Journal of medicinal chemistry. 64(2)
Autor:
Robert E. Davis, Lawrence P. Wennogle, Peng Li, Joseph P. Hendrick, Satoshi Sogabe, Wei Yao, Gyorgy Snell, Hailin Zheng, J. David Beard, Zhao Jun, Gretchen L. Snyder, Lei Zhang, Weston Lane, Koh Ida, Charles J. Heyser, Hongwen Zhu, Kimberly E. Vanover
Publikováno v:
Journal of Medicinal Chemistry. 59:1149-1164
A diverse set of 3-aminopyrazolo[3,4-d]pyrimidinones was designed and synthesized. The structure-activity relationships of these polycyclic compounds as phosphodiesterase 1 (PDE1) inhibitors were studied along with their physicochemical and pharmacok
Autor:
Junichi Sakamoto, Takeshi Yasui, Hiroshi Inooka, Kouhei Asano, Satoshi Sogabe, Masashi Iwata, Nozomu Sakai, Gyorgy Snell, Takafumi Takai, Yoshihisa Nakada, Yasuhiro Imaeda, Melinda Davis, Kotaro Sakamoto, Yoshitomi Yayoi, Yusuke Kamada, Takeshi Yamamoto, Terufumi Takagi, Masayuki Goto, Weston Lane
Publikováno v:
Bioorganicmedicinal chemistry. 25(17)
B-cell lymphoma 6 (BCL6) is a transcriptional repressor that can form complexes with corepressors via protein-protein interactions (PPIs). The complexes of BCL6 and corepressors play an important role in the formation of germinal centers (GCs), and d