Zobrazeno 1 - 10
of 118
pro vyhledávání: '"A. G. Tomasselli"'
Autor:
Huey-Sheng Shieh, Grace E. Munie, Nicole Caspers, Alfredo G. Tomasselli, James R. Kiefer, Karl J. Mathis, Arthur J. Wittwer, Micky D. Tortorella, Scott S. Woodard, Mark E. Schnute, Jennifer M. Williams, Anne-Marie Malfait
Publikováno v:
Protein Science. 20:735-744
A ((1S,2R)-2-hydroxy-2,3-dihydro-1H-inden-1-yl) succinamide derivative (here referred to as Compound 12) shows significant activity toward many matrix metalloproteinases (MMPs), including MMP-2, MMP-8, MMP-9, and MMP-13. Modeling studies had predicte
Autor:
James R. Kiefer, Joseph W. Leone, Alfredo G. Tomasselli, Robin A. Weinberg, Akshay Patny, H. David Fischer, Cynthia D. Sommers, Jennifer A. Gormley, Timothy E. Benson, Horng-Chih Huang, E.J. Jacobsen, Jacqueline E. Day, Thomas L. Emmons, Jill Chrencik, Iris K. Leung, Jeffrey L. Hirsch, Tenbrink Ruth E, Jennifer M. Williams, Brian Korniski, Troii Hall
Publikováno v:
Journal of Molecular Biology. 400:413-433
Janus kinases (JAKs) are critical regulators of cytokine pathways and attractive targets of therapeutic value in both inflammatory and myeloproliferative diseases. Although the crystal structures of active JAK1 and JAK2 kinase domains have been repor
Autor:
Thomas L. Emmons, Alfredo G. Tomasselli, Robin A. Weinberg, H. David Fischer, Jill Chrencik, Brian Korniski, Jacqueline E. Day, Stacy Brown, Joseph W. Leone, Ann D. Wrightstone, Cynthia D. Sommers, Jeffrey L. Hirsch, Arthur J. Wittwer, Troii Hall, Jennifer A. Gormley
Publikováno v:
Biochemical and Biophysical Research Communications. 396:543-548
The Janus kinase family consists of four members: JAK-1, -2, -3 and TYK-2. While JAK-2 and JAK-3 have been well characterized biochemically, there is little data on TYK-2. Recent work suggests that TYK-2 may play a critical role in the development of
Autor:
Thomas L. Emmons, James R. Kiefer, Joseph W. Leone, John F. Schindler, Melissa S. Harris, Jacqueline E. Day, Siradanahalli Guru, Alfredo G. Tomasselli, Robin A. Weinberg, Sandra Lightle, H. David Fischer, Jeffrey L. Hirsch, Jill Chrencik, Jennifer A. Gormley, Jennifer M. Williams, Matthew J. Saabye, Troii Hall
Publikováno v:
Protein Expression and Purification. 69:54-63
Janus-associated kinases (JAKs) play critical roles in cytokine signaling, and have emerged as viable therapeutic targets in inflammation and oncology related diseases. To date, targeting JAK proteins with highly selective inhibitor compounds have re
Autor:
Beverly A. Reitz, Joseph W. Leone, Michael J. Bienkowski, Daniel F. Curran, Karl J. Mathis, Thomas L. Emmons, Jacqueline E. Day, Mary E. Shuck, Mark C. Walker, Alfredo G. Tomasselli, H. David Fischer
Publikováno v:
Protein Expression and Purification. 65:133-139
Soluble guanylate cyclase (sGC) has been purified from 100 L cell culture infected by baculovirus using the newer and highly effective titerless infected-cells preservation and scale-up (TIPS) method. Successive passage of the enzyme through DEAE, Ni
Autor:
Beverly A. Reitz, Thomas L. Emmons, Alfredo G. Tomasselli, H. David Fischer, Michael J. Bienkowski, S. Edward Lee, David Wasilko, Karl J. Mathis, Kim Jonelle Stutzman-Engwall
Publikováno v:
Protein Expression and Purification. 65:122-132
Compounds capable of stimulating soluble guanylate cyclase (sGC) activity might become important new tools to treat hypertension. While rational design of these drugs would be aided by elucidation of the sGC three-dimensional structure and molecular
Autor:
A. M. Mildner, R. L. Heinrikson, H. D. Fischer, J. M. Lull, Thomas L. Emmons, Alfredo G. Tomasselli, J. W. Leone
Publikováno v:
Protein & Peptide Letters. 16:121-131
Evidence for a key role of beta-amyloid (Abeta) in Alzheimer's disease has led to considerable interest in potential therapeutic strategies targeting enzymes involved in processing the amyloid precursor protein (APP). Beta-site APP Cleaving Enzyme (B
Autor:
A. Tomasselli, D. Paddock, T. Emmons, A. Mildner, J. Leone, J. Lull, J. Cialdella, D. Prince, H. Fischer, R. Heinrikson, T. Benson, A. G. Tomasselli, D. J. Paddock, T. L. Emmons, A. M. Mildner, J. W. Leone, J. M. Lull, J. I. Cialdella, D. B. Prince, H. D. Fischer, R. L. Heinrikson, T. E. Benson
Publikováno v:
Protein & Peptide Letters. 15:131-143
BACE (beta-site APP cleaving enzyme) or beta-secretase, the enzyme responsible for processing APP to give the N-terminal portion of the Abeta peptide, is a membrane bound aspartyl protease consisting of an ectodomain catalytic unit, a C-terminal tran
Autor:
Timothy E. Benson, Michael J. Bienkowski, Tenbrink Ruth E, Alice Laborde, D. Bryan Prince, Joseph B. Moon, Steven W. Kortum, Thomas L. Emmons, Alfredo G. Tomasselli, Donna J. Paddock
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3378-3383
The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.
Autor:
John N. Freskos, Yvette M. Fobian, Timothy E. Benson, Michael J. Bienkowski, David L. Brown, Thomas L. Emmons, Robert Heintz, Alice Laborde, Joseph J. McDonald, Brent V. Mischke, John M. Molyneaux, Joseph B. Moon, Patrick B. Mullins, D. Bryan Prince, Donna J. Paddock, Alfredo G. Tomasselli, Gregory Winterrowd
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:73-77
We describe a novel series of potent inhibitors of human beta-secretase. These compounds possess the hydroxyethyl amine transition state isostere. A 2.5A crystal structure of inhibitor 32 bound to BACE is provided.