Zobrazeno 1 - 10
of 32
pro vyhledávání: '"Nicole Caspers"'
Autor:
Seungil Han, Martin E. Dowty, Ralph P. Robinson, Steven E. Heasley, Peter T. Symanowicz, Jason Jussif, Thomas M. Harris, Neelu Kaila, Lu Wang, Matthew Frank Brown, Jeffrey M. Casavant, Nicole Caspers, Sarah H. Griffin, Mark J. Mitton-Fry, Martin Hegen, Johnson Timothy Allan, Tenbrink Ruth E, Mary Ellen Banker, Jonathan Langille, Mihir D. Parikh, Tsung H. Lin, Arindrajit Basak, Jean-Baptiste Telliez, James D. Clark, Strohbach Joseph Walter, Eric P. Arnold, Ray Unwalla, Li Li, Brian A. Duclos, Xin Yang, Mark Edward Flanagan, John David Trzupek, Michael L. Vazquez, Soojin Kwon, Ashley Edward Fenwick
Publikováno v:
Journal of Medicinal Chemistry. 61:1130-1152
Janus kinases (JAKs) are intracellular tyrosine kinases that mediate the signaling of numerous cytokines and growth factors involved in the regulation of immunity, inflammation, and hematopoiesis. As JAK1 pairs with JAK2, JAK3, and TYK2, a JAK1-selec
Autor:
Ravi G. Kurumbail, Eric Johnson, Nicole Caspers, Timothy A. Subashi, Michael L. Vazquez, Francis Rajamohan, Lise R. Hoth, Neelu Kaila, Kieran F. Geoghegan, Ciarán N. Cronin, Seungil Han
Publikováno v:
Acta Crystallographica Section F Structural Biology Communications. 72:840-845
Crystals of phosphorylated JAK1 kinase domain were initially generated in complex with nucleotide (ADP) and magnesium. The tightly bound Mg2+-ADP at the ATP-binding site proved recalcitrant to ligand displacement. Addition of a molar excess of EDTA h
Autor:
Jane M. Withka, Daniel W. Kung, Russell A. Miller, Matthew S. Dowling, Aaron C. Smith, Angela Wolford, Heather Eng, Janice A. Brown, Jun Xiao, Kris A. Borzilleri, Ravi G. Kurumbail, David J. Edmonds, Jessica Ward, Amit S. Kalgutkar, Colin R. Rose, Tim F. Ryder, Meihua Tu, Dilinie P. Fernando, Emily Cokorinos, David Hepworth, James A. Landro, Kimberly O. Cameron, Matthew F. Calabrese, Christopher T. Salatto, Francis Rajamohan, Andre Shavnya, Markus Boehm, Yuxia Mao, Allan R. Reyes, Richard K. Frisbie, Nicole Caspers, Edward L. Conn, Samit Kumar Bhattacharya
Publikováno v:
Journal of Medicinal Chemistry. 59:8068-8081
Adenosine monophosphate-activated protein kinase (AMPK) is a protein kinase involved in maintaining energy homeostasis within cells. On the basis of human genetic association data, AMPK activators were pursued for the treatment of diabetic nephropath
Autor:
Michael David Rogers, Jeffery N. Carroll, Mark A. Massa, Jeffrey Hitchcock, Peter G. Ruminski, Michelle A. Schmidt, Bruce C. Hamper, Strohbach Joseph Walter, Huey S. Shieh, Laurence O. Whiteley, Katherine E. Palmquist, Joe T. Collins, Grace E. Munie, Hanau Cathleen E, H. Peter Kleine, Mark E. Schnute, T. Sunyer, Nicole Caspers, John E. Baldus, Theresa R. Fletcher, Joseph J. McDonald, Silvia Portolan, Jeffrey A. Scholten, Dean Messing, Margaret L. Grapperhaus, Brandon Collins
Publikováno v:
Journal of Medicinal Chemistry. 59:313-327
Matrix metalloproteinase-13 (MMP-13) is a zinc-dependent protease responsible for the cleavage of type II collagen, the major structural protein of articular cartilage. Degradation of this cartilage matrix leads to the development of osteoarthritis.
Autor:
Brian Juba, Robert Hughes, Mihir D. Parikh, Erin McCarthy, John I. Trujillo, John Robert Springer, Li Xing, Venkataraman Thanabal, Kyung-Hee Kim, Arthur J. Wittwer, Daniel P. Walker, Dean Messing, Nancy L. Wood, Margaret L. Grapperhaus, Nicole Caspers, Zhao-Kui Wan, John Douhan, Shashi Mohan, Mark E. Schnute, Seungil Han, Stephen E. Benoit, Jeffrey F. Ohren, Ingrid P. Buchler, Shaun R. Selness, Thomas N. O'Connell, Jane M. Withka, Michelle Schmidt, Joy S. Miyashiro, Christoph W. Zapf, Nelson Huang, Erica Liu, Rajeev Hotchandani
Publikováno v:
ACS medicinal chemistry letters. 10(1)
[Image: see text] Potent covalent inhibitors of Bruton’s tyrosine kinase (BTK) based on an aminopyrazole carboxamide scaffold have been identified. Compared to acrylamide-based covalent reactive groups leading to irreversible protein adducts, cyana
Autor:
Martin Hegen, David C. Wood, Patrik Rhönnstad, Felix Vajdos, Atli Thorarensen, Mark E. Schnute, Timothy Braden, Kimberly Crouse, Maria Sjöberg, John I. Trujillo, Ravi G. Kurumbail, Bolette Husman, Konrad F. Koehler, Mattias Wennerstål, Tomas Bonn, Joakim Löfstedt, Eva Backström-Rydin, Bo Carlsson, Aron Sundell, Ming Z. Chen, Steven E. Heasley, John David Trzupek, Annika Goos-Nilsson, Carol A. Menard, Peter Harris, James R. Kiefer, Martin Bengtsson, Leon P. Collis, Michael J. Prinsen, Philippe Nuhant, Jennifer Alley, Scott A. Long, Alexander E. Hromockyj, Andrew C. Flick, Johnny Sandberg, Christoph W. Zapf, Edouard Zamaratski, Xiao Hu, Lee Napierata, Björn Kauppi, Nicole Caspers, Kimberly F. Fennell, Robert E. Kyne, Gabriel Berstein, Neelu Kaila, Lars Kruger, Wei Li, Li Xing, Ray Unwalla, Elisabet Kallin, Matthew J. Pelc, Susan Fish, James Robert Blinn, Hjalmar Gullberg, Marvin J. Meyers, Scot Richard Mente, Chulho Choi, Falgun Shah, Mathias Färnegårdh, Dean Messing, Peter G. Jones, Yajuan Zhao, Alexandria P. Taylor, Maria Sandström, Charles W. Bolten, Daniel Nöteberg, Robin A. Weinberg, Tomasz Janosik, John D. Knafels, Anna Wilhelmsson
Publikováno v:
Journal of medicinal chemistry. 61(23)
The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to reduce production
Autor:
Kimberly O. Cameron, Kevin J. Filipski, Jana Polivkova, Matthew S. Dowling, Andre Shavnya, Gary Erik Aspnes, David Christopher Ebner, Allan R. Reyes, Qifang Li, Michael Herr, Jun Xiao, Jessica Ward, Shawn Cabral, Heather Eng, Sophie Y. Lavergne, Ravi G. Kurumbail, Jane M. Withka, Samit Kumar Bhattacharya, Dilinie P. Fernando, Meihua Tu, Edward L. Conn, Bo Feng, Janice A. Brown, Daniel W. Kung, Francis Rajamohan, Esther C.Y. Lee, Russell A. Miller, Emily Cokorinos, Christopher T. Salatto, Nicole Caspers, Nathan E. Genung, Jane Panteleev, Benjamin A. Thuma, Matthew F. Calabrese, Sumathy Mathialagan, Aaron C. Smith, Kris A. Borzilleri, David J. Edmonds, Amit S. Kalgutkar
Publikováno v:
Journal of medicinal chemistry. 61(6)
Optimization of the pharmacokinetic (PK) properties of a series of activators of adenosine monophosphate-activated protein kinase (AMPK) is described. Derivatives of the previously described 5-aryl-indole-3-carboxylic acid clinical candidate (1) were
Autor:
Seungil Han, Aaron C. Smith, Melissa S. Harris, Timothy A. Subashi, Shawn Cabral, Lise R. Hoth, Nicole Caspers, Francis Rajamohan, Philip A. Carpino, Parag Sahasrabudhe, Ravi G. Kurumbail, Hong Wang, Jessica Ward, Edward L. Conn, Kris A. Borzilleri, James A. Landro, Jane M. Withka, Janice A. Brown, Russell A. Miller, Kimberly O. Cameron, Allyn T. Londregan, Richard K. Frisbie, Xiayang Qiu, Matthew F. Calabrese, Allan R. Reyes, Rachelle Magyar, Kieran F. Geoghegan
Publikováno v:
Structure. 22:1161-1172
SummaryAMP-activated protein kinase (AMPK) is a principal metabolic regulator affecting growth and response to cellular stress. Comprised of catalytic and regulatory subunits, each present in multiple forms, AMPK is best described as a family of rela
Autor:
Jeremy T. Starr, Veerabahu Shanmugasundaram, Sandra P. McCurdy, Michael D. Huband, Lisa Aschenbrenner, Brian S. Gerstenberger, Eric B. McElroy, M. Megan Lemmon, Mark R. Rauckhorst, Seungil Han, Andrew P. Tomaras, Ye Che, Nicole Caspers, Jennifer A. Young, Richard P. Zaniewski, John D. Knafels, Matthew Frank Brown, Chao Li
Publikováno v:
Journal of Medicinal Chemistry. 57:3845-3855
Multidrug-resistant Gram-negative pathogens are an emerging threat to human health, and addressing this challenge will require development of new antibacterial agents. This can be achieved through an improved molecular understanding of drug-target in
Autor:
Kieran F. Geoghegan, Seungil Han, Veerabahu Shanmugasundaram, Richard P. Zaniewski, Nicole Caspers, Andrew P. Tomaras, Brian M. Lacey, Xidong Feng
Publikováno v:
Journal of the American Chemical Society. 133:20536-20545
Multi-drug-resistant forms of the Gram-negative pathogen Acinetobacter baumannii are an emerging threat to human health and further complicate the general problem of treating serious bacterial infections. Meeting this challenge requires an improved u