Zobrazeno 1 - 7
of 7
pro vyhledávání: '"Shelby Crawford"'
Autor:
Krystal Herman, Jonathan M. Blevitt, Homayon Banie, Mandana Tootoonchi, Murray McKinnon, Glenda Castro, Yan Zhang, Rosa Luna, Tadimeti S. Rao, Anton Bittner, Anne M. Fourie, Jiao Song, Xuejun Liu, Maxwell D. Cummings, Marciano Sablad, Xiaohu Deng, Rose A. Dandridge, Wai-Ping Fung-Leung, Natasha Rozenkrants, Marina I. Nelen, Pejman Soroosh, Steven W. Sutton, Jiejun Wu, Marcos E. Milla, Kacey L. Sachen, Steven Nguyen, Xia V. Yang, Shelby Crawford, Aimee De Leon-Tabaldo, Siquan Sun, Changlu Liu, Jingxue Yu, Xiaohua Xue, Jingjin Gao, Neelakandha S. Mani, Karen Ngo, Chester Kuei
Publikováno v:
Proceedings of the National Academy of Sciences. 111:12163-12168
The RAR-related orphan receptor gamma t (RORγt) is a nuclear receptor required for generating IL-17-producing CD4(+) Th17 T cells, which are essential in host defense and may play key pathogenic roles in autoimmune diseases. Oxysterols elicit profou
Autor:
Virginia M. Tanis, Dan Pippel, Cheryl A. Grice, Shelby Crawford, Jason P. Riley, Navin Rao, Karlsson Lars, Brad M. Savall, Christa C. Chrovian, Aimee Rose de Leon, Xiaohua Xue, Alejandro Santillan, Anne M. Fourie, Jimmy T. Liang, Xiaohu Deng, Jonathan M. Blevitt, Aaron M. Kearney, Arlene L. Young, Alice Lee-Dutra, Krystal Herman, Wendy Eccles, Rosa Luna, Jamila N. Booker
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 23:811-815
Leukotrienes (LT's) are known to play a physiological role in inflammatory immune response. Leukotriene A(4) hydrolase (LTA(4)H) is a cystolic enzyme that stereospecifically catalyzes the transformation of LTA(4) to LTB(4). LTB(4) is a known pro-infl
Autor:
Jonathan M. Blevitt, Arlene L. Young, Xiaohua Xue, Genesis M. Bacani, Aimee Rose de Leon, Alejandro Santillan, Adrienne M. Landry-Bayle, Aaron M. Kearney, John J. M. Wiener, Laurent Gomez, Anne M. Fourie, Jason P. Riley, Krystal Herman, Christa C. Chrovian, Cheryl A. Grice, Shelby Crawford, Jay Nelson, Alice Lee-Dutra, Virginia M. Tanis
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:7504-7511
Previously, benzthiazole containing LTA4H inhibitors were discovered that were potent (1–3), but were associated with the potential for a hERG liability. Utilizing medicinal chemistry first principles (e.g., introducing rigidity, lowering c Log D)
Checkpoint Kinase Inhibitors: SAR and Radioprotective Properties of a Series of 2-Arylbenzimidazoles
Autor:
Anders Brunmark, Danielle K. Neff, Shelby Crawford, Lars Karlsson, Kelly J. McClure, Alice Lee, J. Guy Breitenbucher, Chennagiri R. Pandit, Frank U. Axe, Kristen L. Arienti, Jon Blevitt, Liming Huang
Publikováno v:
Journal of Medicinal Chemistry. 48:1873-1885
The discovery of a series of novel, potent, and highly selective inhibitors of the DNA damage control kinase chk2 is disclosed. Here we report the first SAR study around inhibitors of this kinase. High-throughput screening of purified human chk2 led
Autor:
Virginia M, Tanis, Genesis M, Bacani, Jonathan M, Blevitt, Christa C, Chrovian, Shelby, Crawford, Aimee, De Leon, Anne M, Fourie, Laurent, Gomez, Cheryl A, Grice, Krystal, Herman, Aaron M, Kearney, Adrienne M, Landry-Bayle, Alice, Lee-Dutra, Jay, Nelson, Jason P, Riley, Alejandro, Santillán, John J M, Wiener, Xiaohua, Xue, Arlene L, Young
Publikováno v:
Bioorganicmedicinal chemistry letters. 22(24)
Previously, benzthiazole containing LTA(4)H inhibitors were discovered that were potent (1-3), but were associated with the potential for a hERG liability. Utilizing medicinal chemistry first principles (e.g., introducing rigidity, lowering cLogD) a
Autor:
Fourie Anne M, Scott D. Bembenek, Jonathan M. Blevitt, Wolin Ronald L, Jason P. Riley, Daniel Belajic, Jianmei Wei, James P. Edwards, Paul J. Dunford, Lars Karlsson, Shelby Crawford, Anders Brunmark
Publikováno v:
Molecular cancer therapeutics. 7(3)
B-RAF mutations have been identified in the majority of melanoma and a large fraction of colorectal and papillary thyroid carcinoma. Drug discovery efforts targeting mutated B-RAF have yielded several interesting molecules, and currently, three compo
Autor:
Jonathan M. Blevitt, Lars Karlsson, Scott D. Bembenek, Anders Brunmark, Katherine A. Lundeen, Jianmei Wei, James P. Edwards, Shelby Crawford, Wolin Ronald L
Publikováno v:
Bioorganicmedicinal chemistry letters. 18(9)
Computer aided modeling guided the design of a series of diarylimidazole compounds (11–22) intended to interact with both the ATP and adjacent allosteric binding domains of B-RAF kinase. Their ability to inhibit the function of B-RAF kinase and int