Zobrazeno 1 - 10
of 48
pro vyhledávání: '"William J. Metzler"'
Autor:
William J. Metzler, Luciano Mueller, Yaqun Zhang, Mian Gao, Nicolas Szapiel, Mark R. Witmer, David Hedin, Deepa Calambur, Dianlin Xie, Hui Wei, Frank Marsilio, Andrew E Douglas, Ping Zhang
Publikováno v:
Journal of Biomolecular NMR. 68:237-247
An improved expression protocol is proposed for amino acid type-specific [13C], [15N]-isotope labeling of proteins in baculovirus-infected (BV) insect cell cultures. This new protocol modifies the methods published by Gossert et al. (J Biomol NMR 51(
Autor:
Litao Zhang, William J. Metzler, Shana L. Posy, Robert M. Borzilleri, Yuval Blat, Brigitte Devaux, Charu Chaudhry, Randy Talbott, Chunhong Yan, Yong Zhang, Jonathan H. Davis, Ming Lei, Henry Shen
Publikováno v:
Analytical Biochemistry. 497:8-17
XIAP (X-chromosome-linked inhibitor of apoptosis protein) is a central apoptosis regulator that blocks cell death by inhibiting caspase-3, caspase-7, and caspase-9 via binding interactions with the XIAP BIR2 and BIR3 domains (where BIR is baculovirus
Publikováno v:
Applied Biophysics for Drug Discovery
Externí odkaz:
https://explore.openaire.eu/search/publication?articleId=doi_________::c456c27f487063f2e6484a1dbd2ffbfe
https://doi.org/10.1002/9781119099512.ch8
https://doi.org/10.1002/9781119099512.ch8
Autor:
John E. Macor, Ramesh Padmanabha, Jere E. Meredith, Jeremy H. Toyn, William J. Metzler, Andrew J. Tebben, Jodi K. Muckelbauer, Charles F. Albright, Lynda S. Cook, Lorin A. Thompson, Samuel Gerritz, Michael J. Sofia, Michael A. Poss, Shirong Zhu, Lawrence G. Iben, Daniel M. Camac, Kimberley A. Lentz, Shuhao Shi, Andrew C. Good, Weixu Zhai, Catherine R. Burton
Publikováno v:
Journal of Medicinal Chemistry. 55:9208-9223
This report describes the discovery and optimization of a BACE-1 inhibitor series containing an unusual acyl guanidine chemotype that was originally synthesized as part of a 6041-membered solid-phase library. The synthesis of multiple follow-up solid
Autor:
David R. Langley, Brian Carpenter, Valentina Goldfarb, William J. Metzler, Susan E. Kiefer, Walter Kostich, Mian Gao, Kevin Kish, Ryan Westphal, Patricia A. McDonnell, Steven Sheriff, James William Bryson
Publikováno v:
Acta Crystallographica Section F Structural Biology and Crystallization Communications. 67:768-774
Protein tyrosine phosphatase γ is a membrane-bound receptor and is designated RPTPγ. RPTPγ and two mutants, RPTPγ(V948I, S970T) and RPTPγ(C858S, S970T), were recombinantly expressed and purified for X-ray crystallographic studies. The purified e
Autor:
Luciano Mueller, Dietmar A. Seiffert, Ruth R. Wexler, Anzhi Wei, John A. Newitt, Jeffrey M. Bozarth, Alexandra H. Nirschl, Paul E. Morin, Xiao Wen, Daniel L. Cheney, James K. Tamura, Alan R. Rendina, William J. Metzler, Nicholas R. Wurtz, E. Scott Priestley
Publikováno v:
Journal of medicinal chemistry. 58(6)
A multidisciplinary, fragment-based screening approach involving protein ensemble docking and biochemical and NMR assays is described. This approach led to the discovery of several structurally diverse, neutral surrogates for cationic factor VIIa P1
Autor:
William J. Metzler, Keith L. Constantine, Stephen R. Johnson, Patricia A. McDonnell, Thomas J. Caulfield, David R. Magnin, Richard B. Sulsky, Jeffrey A. Robl, Luciano Mueller, Valentina Goldfarb, David S. Taylor, Bennett T. Farmer, Rex A. Parker, Leonard P. Adam
Publikováno v:
Journal of Medicinal Chemistry. 49:5013-5017
The NMR structure is presented for compound 1 (BMS-480404) (Ki = 33 (+/-2) nM) bound to keratinocyte fatty acid-binding protein. This article describes interactions between a high affinity drug-like compound and a member of the fatty acid-binding pro
Autor:
Young B. Kim, Mark S. Kirby, Lawrence G. Hamann, William J. Metzler, Carolyn A. Weigelt, Jovita Marcinkeviciene, Lisa M. Kopcho
Publikováno v:
Archives of Biochemistry and Biophysics. 445:9-18
Dipeptidyl peptidase-IV (DPP-IV) is a serine protease with a signature Asp-His-Ser motif at the active site. Our pH data suggest that Gly-Pro-pNA cleavage catalyzed by DPP-IV is facilitated by an ionization of a residue with a p K of 7.2 ± 0.1. By a
Autor:
Bruce M. Rankin, William J. Pitts, William J. Metzler, Kenneth J. Leavitt, Andrew T. Pudzianowski, Wayne Vaccaro, Richard Liu, Patricia A. McDonnell, Joseph Barbosa, Soong-Hoon Kim
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1101-1106
Computer aided drug design led to a new class of spiro-barbiturates (e.g., 4a, MMP-13 K(i)=4.7 nM) that are potent inhibitors of MMP-13.
Autor:
William J. Metzler, Robert A. Copeland, Jovita Marcinkeviciene, Mark R. Witmer, Larisa Toulokhonova
Publikováno v:
Journal of Biological Chemistry. 278:4582-4589
The steady-state kinetic mechanism of β-amyloid precursor protein-cleaving enzyme (BACE)-catalyzed proteolytic cleavage was evaluated using product and statine- (Stat(V)) or hydroxyethylene-containing (OM99-2) peptide inhibition data, solvent kineti