Zobrazeno 1 - 10
of 20
pro vyhledávání: '"Anthony J. Jurewicz"'
Autor:
Peter A. Jones, Ashley K. Wiseman, Helai P. Mohammad, Christopher S. Kershaw, Bryan W. King, Ian D. Waddell, Thau F. Ho, Stephen B. Baylin, Morris Muliaditan, Marcus Bantscheff, Elisabeth A. Minthorn, Thilo Werner, Alan P. Graves, Wendy A. Kellner, Phil Chapman, Mehul Patel, Anthony J. Jurewicz, Allan M. Jordan, Emma E. Fairweather, Rab K. Prinjha, Nino Campobasso, Anna Rutkowska, H. Christian Eberl, Ryan G. Kruger, Charles F. McHugh, Michael T. McCabe, Kristin M. Goldberg, Jon Paul Jaworski, Christopher L. Carpenter, Michael Steidel, Stuart Paul Romeril, Dirk A. Heerding, Lourdes Rueda, David T. Fosbenner, Amy N. Taylor, Jacques Briand, Shawn W. Foley, Arthur Groy, Andrew B. Benowitz, Xiaodong Cheng, Donald J. Ogilvie, Paola Grandi, Cunyu Zhang, Mei Li, Sarath Pathuri, Aidan G. Gilmartin, Christian S. Sherk, Juan I. Luengo, Mark Cockerill, Ali Raoof, Alexandra Stowell, Kathryn Keenan, Melissa B. Pappalardi, Makda Mebrahtu, Kristen Wong, Xing Zhang, Jessica L. Handler, Roger J. Butlin, John R. Horton, Susan Merrihew, Charlotte Burt, Dean E. McNulty
Publikováno v:
Nature Cancer. 2:1002-1017
DNA methylation, a key epigenetic driver of transcriptional silencing, is universally dysregulated in cancer. Reversal of DNA methylation by hypomethylating agents, such as the cytidine analogs decitabine or azacytidine, has demonstrated clinical ben
High-Throughput Screening and Triage Assays Identify Small Molecules Targeting c-MYC in Cancer Cells
Autor:
Jon-Paul Jaworski, Lisa A. Payne, Anna Waszkiewicz, Biju Mangatt, Anthony J. Jurewicz, Lorena A. Kallal, Jesus R. Medina, Pat Brady, Xin Zeng, Thomas J. Berrodin, Carolyn Doepner-Buser, Anthony Della Pietra
Publikováno v:
SLAS discovery : advancing life sciences RD. 26(2)
While c-MYC is well established as a proto-oncogene, its structure and function as a transcription factor have made c-MYC a difficult therapeutic target. To identify small-molecule inhibitors targeting c-MYC for anticancer therapy, we designed a high
Autor:
Jessica L. Schneck, Charlie Y. Mo, Zachary M Hostetler, Anthony J. Jurewicz, Paul M. Keller, Trevor Selwood, Amy Quinn, Andrew J. Pope, Matthew J. Culyba, Widdowson Katherine L, Rahul M. Kohli, Jeffrey M. Kubiak
Publikováno v:
ACS Infectious Diseases. 4:349-359
The RecA/LexA axis of the bacterial DNA damage (SOS) response is a promising, yet non-traditional drug target. The SOS response is initiated upon genotoxic stress, when RecA, a DNA damage sensor, induces LexA, the SOS repressor, to undergo autoproteo
Autor:
Mary Ann Hardwicke, Hong Lin, Karl F. Erhard, John D. Martin, Ren Xie, Kaushik Raha, Rosanna Tedesco, Jin Zeng, Yanqiu Qian, Patricia M. Kratz, Yong Jiang, Ted Cecconie, Stan F. Martens, Angela Smallwood, Patrick McDevitt, James F. Mack, Baoguang Zhao, Stephenie B. Chen, Anthony J. Jurewicz, Juan I. Luengo, Mark J. Schulz, Nino Campobasso, Catherine A. Oleykowski, Lawrence M. Szewczuk, Alan R. Rendina, Cynthia M. Rominger, Benjamin J. Schwartz, Leng Nickels, Junya Qu, Jacques Briand
Publikováno v:
ACS Medicinal Chemistry Letters. 7:217-222
A novel series of potent and selective hexokinase 2 (HK2) inhibitors, 2,6-disubstituted glucosamines, has been identified based on HTS hits, exemplified by compound 1. Inhibitor-bound crystal structures revealed that the HK2 enzyme could adopt an "in
Autor:
Catherine E. Peishoff, John R. White, Scott K. Thompson, Anthony J. Jurewicz, Daniel F. Veber, Judithann M. Lee
Publikováno v:
International Journal of Peptide and Protein Research. 47:214-218
In an effort to determine which regions of IL-8 are involved in interactions with its receptors, eight peptides were designed to correspond to distinct exposed regions of the IL-8 monomer, using the proton NMR-derived structure of the dimer as a basi
Autor:
Sara H. Thrall, Rosalie Matico, Michael Jaye, Paul M. Keller, Benjamin J. Schwartz, Timothy Rust, Dennis J. Murphy, Anthony J. Jurewicz, Krawiec John A, Mark R. Harpel, John J. Trill
Publikováno v:
SLAS Discovery. 13:468-475
Endothelial lipase (EL) is a 482-amino-acid protein from the triglyceride lipase gene family that uses a Ser-His-Asp triad for catalysis. Its expression in endothelial cells and preference for phospholipids rather than triglycerides are unique. Anima
Autor:
Kyung O. Johanson, Thau F. Ho, Anthony J. Jurewicz, Benjamin J. Schwartz, Jianhong Ma, Sara H. Thrall, Leng A. Lor, John D. Martin, Robert B. Kirkpatrick, Monique F. Murray, Hong Zhang
Publikováno v:
SLAS Discovery. 12:1050-1058
Tumor suppressor p53 is typically maintained at low levels in normal cells. In response to cellular stresses, such as DNA damage, p53 is stabilized and can stimulate responses leading to cell cycle arrest or apoptosis. Corresponding to its central ro
Autor:
Victoria J. Barrett, Feng Wang, Christopher Browning, Matthew J Lindon, Henry M. Sarau, James A. Fornwald, Andy J. Harker, Guido Hartmann, Jeffery K. Kerns, David P. Andrew, Graeme Irvine Stevenson, Ashley Paul Hancock, Victoria Vinader, Michael L. Moore, James J. Foley, Jian Jin, Parvathi Rao, Anthony J. Jurewicz, Helen E. Connor, Dwight M. Morrow, Kristen E. Belmonte, Yonghui Wang, Ralph A. Rivero, Cuc Nguyen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1722-1725
High-throughput screening of the corporate compound collection led to the discovery of a novel series of N-substituted-5-aryl-oxazolidinones as potent human CCR8 antagonists. The synthesis, structure-activity relationships, and optimization of the se
Autor:
Henry M. Sarau, John R. White, Lisa T. Christmann, Dashyant Dhanak, Anthony J. Jurewicz, Widdowson Katherine L, Richard M. Keenan, Judithann M. Lee, Michael G. Darcy
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:1441-1444
The discovery of a series of phenylalanine derived CCR3 antagonists is reported. Parallel, solution-phase library synthesis has been utilized to delineate the structure–activity relationship leading to the synthesis of highly potent, CCR3-selective
Autor:
Widdowson Katherine L, James J. Foley, Judithann M. Lee, James A. Fornwald, Michael G. Darcy, Lisa T. Christmann, George K. Chan, Dulcie B. Schmidt, Christina S. Imburgia, John R. White, Anthony J. Jurewicz, Dashyant Dhanak, Kimberly A. Dede, Henry M. Sarau
Publikováno v:
Journal of Biological Chemistry. 275:36626-36631
Eosinophils have been implicated in the pathogenesis of asthma and other allergic diseases. Several CC chemokines including eotaxin (CCL-11), eotaxin-2 (CCL-24), RANTES (CCL-5), and monocyte chemotactic protein-3 (MCP-3, CCL-7) and 4 (MCP-4, CCL-13)