Zobrazeno 1 - 10
of 69
pro vyhledávání: '"Joseph J. McDonald"'
Autor:
Mary E Matyskiela, Thomas Clayton, Philip P Chamberlain, Aaron Carpenter, Mark Rolfe, Barbra Pagarigan, Joseph J. McDonald, Gang Lu, Eileen Tran, Christopher Mayne, Lawrence G Hamann, Xinde Zheng
Publikováno v:
Nature Structural & Molecular Biology. 27:319-322
Thalidomide-dependent degradation of the embryonic transcription factor SALL4 by the CRL4CRBN E3 ubiquitin ligase is a plausible major driver of thalidomide teratogenicity. The structure of the second zinc finger of SALL4 in complex with pomalidomide
Autor:
JOHN Malona, CLAUDIO CHUAQUI, BORIS M. SELETSKY, LISA BEEBE, SUSAN CANTIN, DANIEL VAN KALKEN, KELLY FAHNOE, ZHIGANG WANG, BETH BROWNING, HILARY SZABO, LOUISE A. KOOPMAN, TAMAS ORAVECZ, JOSEPH J. MCDONALD, FRANCISCO RAMIREZ-VALLE, RAJULA GAUR, KOFI A. MENSAH, MICHAEL THOMAS, JAMIE N. CONNARN, HAIQING HU, MATTHEW D. ALEXANDER, ALAN F. CORIN
Publikováno v:
Translational research : the journal of laboratory and clinical medicine. 249
As an anti-inflammatory strategy, MAPK-activated protein kinase-2 (MK2) inhibition can potentially avoid the clinical failures seen for direct p38 inhibitors, especially tachyphylaxis. CC-99677, a selective targeted covalent MK2 inhibitor, employs a
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:
David J. Richard, Julie Lee, Alessandro Moretto, Seungil Han, Kristin Janz, Neelu Kaila, Mark Ryan, Cristina Aevazelis, Lori Fitz, Jeanne Chang, Zhao-Kui Wan, Atli Thorarensen, Joseph J. McDonald, Christoph Martin Dehnhardt, Frank Lovering, Nikolaos Papaioannou, William M. Moore
Publikováno v:
ChemMedChem. 11:217-233
There has been significant interest in spleen tyrosine kinase (Syk) owing to its role in a number of disease states, including autoimmunity, inflammation, and cancer. Ongoing therapeutic programs have resulted in several compounds that are now in cli
Publikováno v:
Journal of chemical theory and computation. 12(4)
Epidermal growth factor receptor (EGFR) inhibitors interrupt EGFR-dependent cellular signaling pathways that lead to accelerated tumor growth and proliferation. Mutation of a threonine in the inhibitor binding pocket, known as the "gatekeeper", to me
Publikováno v:
Biophysical Journal. 110(3)
Small molecular inhibitors of receptor kinases suppress cellular signaling pathways mediated by the proteins that lead to malignant cell growth and division. We have studied molecular interactions between epidermal grow factor receptor (EGFR) and the
Autor:
Julie Lee, Paul Alan Glossop, Atli Thorarensen, Yogesh A. Sabnis, Christopher Phillips, Lori Fitz, Frank Lovering, Andrew F. Bent, Ravi G. Kurumbail, Gavin A. Whitlock, Jeanne S. Chang, Seungil Han, Joseph J. McDonald, Mark Ryan
Publikováno v:
Chemical Biology & Drug Design. 80:657-664
Spleen tyrosine kinase is a non-receptor tyrosine kinase, overactivation of which is thought to contribute to autoimmune diseases as well as allergy and asthma. Protein kinases have a highly conserved ATP binding site, thus making challenging the des
Autor:
Jeffery N. Carroll, Craig Swearingen, Decrescenzo Gary A, Rico Joseph G, Theresa R. Fletcher, Daniel P. Becker, Joseph J. McDonald, Susan L. Hockerman, Grace E. Munie, Stephen A. Kolodziej, Boehm Terri L, Debbie A. Mischke, Nathan W. Stehle
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3557-3560
A series of phenyl piperidine alpha-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13, are dual-sparing
Autor:
Daniel P. Becker, Theresa R. Fletcher, Debbie A. Mischke, Joseph J. McDonald, Stephen A. Kolodziej, Nathan W. Stehle, Susan L. Hockerman, Grace E. Munie, Craig Swearingen, Decrescenzo Gary A
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:3561-3564
A series of N-aryl isonipecotamide alpha-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13.
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.