Zobrazeno 1 - 10
of 39
pro vyhledávání: '"Daigen Xu"'
Autor:
Andrew Bender, Anna Gardberg, Lesley Liu-Bujalski, Jared Head, Igor Mochalkin, Potnick Justin, Johnson Theresa L, Federica Morandi, Roland Grenningloh, Richard D. Caldwell, Reinaldo Jones, Ariele Viacava Follis, Hui Qiu, Andreas Goutopoulos, Daigen Xu, Sherer Brian A
Publikováno v:
ChemMedChem. 14:217-223
Bruton's tyrosine kinase (Btk) is an attractive target for the treatment of a wide array of B-cell malignancies and autoimmune diseases. Small-molecule covalent irreversible Btk inhibitors targeting Cys481 have been developed for the treatment of suc
Autor:
Thabo Mpotje, Daigen Xu, Thomas Spangenberg, Frank Brombacher, Kai Fu, Justin Komguep Nono, Lerato Hlaka, Paballo Mosala, Severin Donald Kamdem, Nada Abdel Aziz, Georgianna Varrone
Publikováno v:
Scientific Reports
Scientific Reports, Vol 10, Iss 1, Pp 1-12 (2020)
Scientific Reports, Vol 10, Iss 1, Pp 1-12 (2020)
Tissue fibrosis underlies the majority of human mortality to date with close to half of all reported deaths having a fibrotic etiology. The progression of fibrosis is very complex and reputed irreversible once established. Although some preventive op
Autor:
Meera Ramanujam, Daigen Xu, Soo Min, John Woods, Jennifer Postelnek, Julia Ayala, Kai-Yeung Lau, Holly Hilton, Julie Hang, Yong Kim, Julie DeMartino, Rosario Garrido, Mario Giron, Stella Stefanova, Satwant K. Narula, Nena Dimaano, Toni Whittard, Natalie D. Keirstead, Alka Patel, Jacob LaStant, Paola Mina-Osorio
Publikováno v:
Arthritis & Rheumatism. 65:2380-2391
Objective Bruton's tyrosine kinase (BTK) plays a critical role in B cell development and function. We recently described a selective BTK inhibitor, RN486, that blocks B cell receptor (BCR) and Fcγ receptor signaling and is efficacious in animal mode
Autor:
Julie DeMartino, Ronald J. Hill, Jay S. Fine, Alison O'Mahony, Jennifer Postelnek, Cheng Liao, Dinesh Srinivasan, Michael Bradshaw, Anita Levin, Daigen Xu, Yong Kim, Satwant K. Narula, Achal Pashine, Dong-Qing Hu, John Woods, Jonathan Hsu, Minh Diem Vu, Yan Lou, Jun Zhang, Timothy D. Owens
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 341:90-103
Genetic mutation and pharmacological inhibition of Bruton9s tyrosine kinase (Btk) both have been shown to prevent the development of collagen-induced arthritis (CIA) in mice, providing a rationale for the development of Btk inhibitors for treating rh
Autor:
Yin Wu, Shinji L. Okitsu, Jared Head, Roland Grenningloh, Federica Morandi, Andrew Bender, Ursula Koehler, Melinda Genest, Eileen Samy, Yi-Ying Chen, Hui Tian, Richard D. Caldwell, Albertina Pereira, Daigen Xu, Lesley Liu-Bujalski, Kai Fu
Publikováno v:
Clinical immunology (Orlando, Fla.). 164
Bruton's tyrosine kinase (Btk) is expressed in a variety of immune cells and previous work has demonstrated that blocking Btk is a promising strategy for treating autoimmune diseases. Herein, we utilized a tool Btk inhibitor, M7583, to determine the
Autor:
Alex G. Therien, Carl Berthelette, Mark Wrona, Michael J. Boyd, Jean-François Lévesque, Rino Stocco, Daigen Xu, Yongxin Han, Danielle Denis, Steve Rowland, Marie-Claude Mathieu, John Colucci, Patsy Clark, Jean-François Chiasson
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:484-487
A novel series of EP(4) ligands, based on a benzyl indoline scaffold, has been discovered. It was found that agonism and antagonism in this series can be easily modulated by minor modifications on the benzyl group. The pharmacokinetic, metabolic and
Autor:
Richard Frenette, Jocelyne Guay, Christine Brideau, Evelyn Martins, Marc Gagnon, Denis Riendeau, Joseph A. Mancini, Andre Giroux, Bernard Cote, Louise Boulet, David Claveau, Diane Ethier, Frédéric Massé, Richard Friesen, Daigen Xu, Anh Chau, Nathalie Méthot, Joel Rubin, Yves Ducharme, Hongping Yu, Sébastien Guiral
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:5837-5841
Phenanthrene imidazoles 26 and 44 have been identified as novel potent, selective and orally active mPGES-1 inhibitors. These inhibitors are significantly more potent than the previously reported chlorophenanthrene imidazole 1 (MF63) with a human who
Autor:
Daigen Xu, Maria Antonietta Davoli, Steven Xanthoudakis, Jimmy Fourtounis, John Tam, George S. Robertson, Gordon Y.K. Ng, Donald W. Nicholson
Publikováno v:
Neuroscience. 115:125-136
In the present study, we evaluated the time-course of caspase-3 activation, and the evolution of cell death following focal cerebral ischemia produced by transient middle cerebral artery occlusion in rats. Ischemia-induced active caspase-3 immunoreac
Autor:
Mingyan Zhou, Andreas Kuglstatter, Preeti Yadava, Aruna Railkar, Johannes C. Hermann, Stephan Kirchner, Ying Peng, Linghao Niu, Christine Lukacs, Eric Chiao, Calvin Yee, Fernando Padilla, Daigen Xu, Matthew C. Lucas, Cheng Liao, Michelle Slade, David Michael Goldstein, Michael Soth, Pei-Yuan Hsu, Niala Bhagirath, John Menke, Joshua Kennedy-Smith, Liudmila Polonchuk
Publikováno v:
Journal of medicinal chemistry. 57(6)
Inhibition of spleen tyrosine kinase has attracted much attention as a mechanism for the treatment of cancers and autoimmune diseases such as asthma, rheumatoid arthritis, and systemic lupus erythematous. We report the structure-guided optimization o
Autor:
Sophie Roy, Jacqueline L. Vanderluit, Matthew T. W. Simpson, Jason G. MacLaurin, David S. Park, George S. Robertson, Donald W. Nicholson, Kerry L. Ferguson, Daigen Xu, Maria Antonietta Davoli, Ruth S. Slack
Publikováno v:
The Journal of Neuroscience. 21:7089-7098
The retinoblastoma tumor suppressor protein, pRb, is a key regulator of cell cycle and has been implicated in the terminal differentiation of neuronal cells. Mice nullizygous for pRb die by embryonic day 14.5 from hematopoietic and neurological defec