Zobrazeno 1 - 10
of 68
pro vyhledávání: '"Elizabeth A. Lunney"'
Publikováno v:
Journal of Computer-Aided Molecular Design. 28:13-23
Protein kinases are the second most prominent group of drug targets, after G-protein-coupled receptors. Despite their distinct inhibition mechanisms, the majority of kinase inhibitors engage the conserved hydrogen bond interactions with the backbone
Autor:
Paul Galatsis, John R. Rubin, Robert V. Talanian, Bradley William Caprathe, Kenneth Dale Brady, Catherine R. Kostlan, Sheehan Susan M, Anthony Thomas, Charles J. Stankovic, Elizabeth A. Lunney, William Glen Harter, Kristin Linn, John Gilmore, Hamish Allen
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:5184-5190
Succinic acid amides have been found to be effective P2-P3 scaffold replacements for peptidic ICE inhibitors. Heteroarylalkyl fragments occupying the P4 position provided access to compounds with nM affinities. Utilization of an acylal prodrug moiety
Autor:
Joseph Wu, Michael J. Greig, Wade Diehl, Alan G. Marshall, Xiu Yu, Hui-Min Zhang, Mark R. Emmett, Ketan S. Gajiwala, Elizabeth A. Lunney
Publikováno v:
Protein Science. 19:703-715
Mutations of the receptor tyrosine kinase KIT are linked to certain cancers such as gastrointestinal stromal tumors (GISTs). Biophysical, biochemical, and structural studies have provided insight into the molecular basis of resistance to the KIT inhi
Autor:
Ellen M. Dobrusin, Elizabeth A. Lunney, William A. Denny, Edward N. Baker, Andrew M. Thompson, R. John Booth, Brian D. Palmer, John Quin, Alan J. Kraker, Christopher J. Squire, Ivan Ivanovic, Daniel F. Ortwine, Ho H. Lee, Jeff B. Smaill, James M. J. Dickson, Alexander James Bridges
Publikováno v:
European Journal of Medicinal Chemistry. 43:1276-1296
A series of N-6 substituted 9-hydroxy-4-phenylpyrrolo[3,4-c]carbazole-1,3(2H,6H)-diones were prepared from N-substituted (5-methoxyphenyl)ethenylindoles. The target compounds were tested for their ability to inhibit the G2/M cell cycle checkpoint kin
Publikováno v:
Bioorganicmedicinal chemistry. 23(19)
Protein kinases constitute a major class of intracellular signaling molecules, and describe some of the most prominent drug targets. Kinase inhibitors commonly employ small chemical scaffolds that form hydrogen bonds with the kinase hinge residues co
Autor:
Dong Liming, Xinjun Hou, Elizabeth A. Lunney, Corinne E. Augelli-Szafran, Deal Judith G, Christopher F. Bigge, Darin Vanderpool, Raymond Andrew Hudack, Nancy Sue Barta, Bradley William Caprathe, Chuangxing Guo, Steve Bender, Richard E. Showalter, Lorraine Kathleen Fay, Arindam Chatterjee
Publikováno v:
Journal of Medicinal Chemistry. 49:1202-1206
Since the discovery that FK-506 promotes neurite outgrowth, considerable attention has been focused on the development of potent nonimmunosuppressive ligands for FK-506 binding proteins (FKBPs). Such neuroimmunophilin agents have been reported to sho
Autor:
John R. Rubin, Nigel Walker, Kenneth Dale Brady, Winnie W. Wong, Mark S. Plummer, Christine Humblet, Charles J. Stankovic, Aurash B Shahripour, Connolly Michael Kevin, Robert V. Talanian, Elizabeth A. Lunney, Hamish Allen, Tomi K. Sawyer
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 11:2779-2782
A series of compounds was designed and prepared as inhibitors of interleukin-1β converting enzyme (ICE), also known as caspase-1. These inhibitors, which employ a diphenyl ether sulfonamide, were designed to improve potency by forming favorable inte
Autor:
Bradley D. Tait, Susan Elizabeth Hagen, Michael Lovdahl, Eric Andrew Zeikus, Carolyn Nouhan, Joanne Brodfuehrer, Donald Hupe, Christopher Andrew Gajda, John M. Domagala, Greg Zeikus, Elizabeth A. Lunney, Steve Vanderroest, Alexander Pavlovsky, Andrej Urumov, James Saunders, Stephen J. Gracheck, Eric Wise, Tod P. Holler
Publikováno v:
Journal of Medicinal Chemistry. 44:2319-2332
Due largely to the emergence of multi-drug-resistant HIV strains, the development of new HIV protease inhibitors remains a high priority for the pharmaceutical industry. Toward this end, we previously identified a 4-hydroxy-5,6-dihydropyrone lead com
Autor:
Christie G. Brouillette, Patrick I. McConnell, Patrick Michael Ann Arbor La Ann Arbor O'brien, Matthew H. Parker, Craig Banotai, William T. Mueller, Daniel F. Ortwine, Elizabeth A. Lunney
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2427-2430
Isothermal titration calorimetry was used to analyze the binding of an enantiomeric pair of inhibitors to the stromelysin-1 catalytic domain. Differences in binding affinity are attributable to different conformational entropy penalties suffered upon
Autor:
Elizabeth A. Lunney, Robert L. Rosati, Dennis J. Hoover, Ian J. Tickle, Mohammed O. Badasso, Christine Humblet, T. Dreyer, Jonathan B. Cooper, Nora Cronin
Publikováno v:
Journal of Molecular Biology. 303:745-760
Saccharopepsin is a vacuolar aspartic proteinase involved in activation of a number of hydrolases. The enzyme has great structural homology to mammalian aspartic proteinases including human renin and we have used it as a model system to study the bin