Zobrazeno 1 - 9
of 9
pro vyhledávání: '"Erik Gjerstad"'
Autor:
Paul A. Sprengeler, James W. Janc, Michael J. Green, Bradley A. Katz, Vincent W.-F. Tai, Jeffrey R. Spencer, Joseph D. Ho, Mary E. McGrath, Michael Graupe, Robb Yee, Erik Gjerstad, Angeles Estiarte, Chang-Sun Lee, Chandru Venkataramani, Yang Liu, Isabelle Lehoux, Hirschbein Bernard L, John R. Somoza, David Sperandio, Liang Liu
Publikováno v:
Biochemistry. 45:5964-5973
Improved peptide-based inhibitors of human beta tryptase were discovered using information gleaned from tripeptide library screening and structure-guided design methods, including fragment screening. Our efforts sought to improve this class of inhibi
Autor:
Erik Gjerstad, James W. Janc, John R. Somoza, Christine Luong, Bradley A. Katz, Erik Verner, Mary E. McGrath, Kyle Mortara, Jie Tang, Hedy Chan, Steven R. Williams, Richard L. Mackman, Wendy B. Young, Paul A. Sprengeler, Joseph D. Ho
Publikováno v:
Journal of Molecular Biology. 344:527-547
A site-directed mutant of the serine protease urokinase-type plasminogen activator (uPA), was produced to assess the contribution of the Ser190 side-chain to the affinity and selectivity of lead uPA inhibitors in the absence of other differences pres
Autor:
Siobhan M Loftus, James E. Sheppeck, Luke J. Gosink, Erik Gjerstad, Alexi R Zubiria, Jeffrey B Wheatley, James W. Janc, Heidi Kar
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 10:2639-2642
A statistically exhaustive, 8800 compound tripeptidal amidomethylcoumarin library was synthesized as discreet compounds using solid-phase combinatorial chemistry. A subset of the compounds was purified by HPLC and tested in a high-throughput fluorome
Publikováno v:
Journal of biomolecular screening. 17(6)
Early assessment of absorption, distribution, metabolism, and excretion (ADME) properties of drug candidates has become an essential component of modern drug discovery. ADME characterization is important in identifying compounds early that are likely
Autor:
James T. Palmer, Ling Leung, Mark Rice, Robert M. Rydzewski, Erik Gjerstad, Leland C. Ii Burrill, James W. Janc, Ram Tahilramani, Kathryn E. Bass, Rohan Mendonca, Lin Pan
Publikováno v:
Journal of medicinal chemistry. 49(10)
Beginning with the peptide sequence Cbz-Ile-Glu(OtBu)-Ala-Leu found in PSI (3), a series of vinyl sulfones (VS) were synthesized for evaluation as inhibitors of the chymotrypsin-like activity of the 20S proteasome. Variations at the key P3 position c
Autor:
Kieron E. Wesson, Ronnel Cabuslay, Erik Gjerstad, Jennifer R. Riggs, William D. Shrader, Robin Stephens, Michael J. Green, Margaret Nguyen, Ellen M. Leahy, Wendy B. Young, Aleksandr Kolesnikov, Paul A. Sprengeler, Huiyong Hu, Ellen Sanford
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(17)
The 4-amino-5-azaindole as an amidino-benzimidazole replacement is described. A series of potent and selective analogs were discovered and showed desirable ex vivo efficacy as measured by PT.
Autor:
Hedy Chan, Erik Gjerstad, Jun Sampang, Jing Yuan, James W. Janc, Jeri Beltman, Margaret Nguyen, James M. Clark
Publikováno v:
Protein expression and purification. 49(1)
Tryptases are trypsin-like serine proteases whose expression is restricted to cells of hematopoietic origin, notably mast cells. gamma-Tryptase, a recently described member of the family also known as transmembrane tryptase (TMT), is a membrane-bound
Autor:
Aleksandr Kolesnikov, Ellen M. Leahy, James W. Janc, Joyce Mordenti, Wendy B. Young, Paul A. Sprengeler, Erik Gjerstad, William D. Shrader, Roopa Rai, Huiyong Hu, Steven M. Torkelson, Bradley A. Katz, Liang Liu
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(8)
Efforts to improve the potency and pharmacokinetic properties of small molecule factor VIIa inhibitors are described. Small structural modifications to existing leads allow the modulation of half-life and clearance, potentially making these compounds