Zobrazeno 1 - 10
of 19
pro vyhledávání: '"Marta C. Abad"'
Autor:
Fiona Madden, Kevin Clark, Marta C. Abad, Jingjie Mo, Caitlin O'Mahony Hartnett, Nikky Le, Barry McCarthy, Jim O'Mahony, Luke A. Gibbons, Francis Maslanka, Christopher Rode, Rosemary Rea, Kerry Robinson, Carl Rafferty, Ronan Hayes
Publikováno v:
Biotechnology Progress. 38
The Quality by Design (QbD) approach to the production of therapeutic monoclonal antibodies (mAbs) emphasizes an understanding of the production process ensuring product quality is maintained throughout. Current methods for measuring Critical Quality
Autor:
Lawrence C. Kuo, Gee-Hong Kuo, Weimei Sun, Fengbing Song, Zhihua Sui, Amy Xiang, Alan C. Gibbs, Marta C. Abad, Xuqing Zhang
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:4762-4767
A series of indazoles have been discovered as KHK inhibitors from a pyrazole hit identified through fragment-based drug discovery (FBDD). The optimization process guided by both X-ray crystallography and solution activity resulted in lead-like compou
Autor:
Kiev S. Ly, John M. Keith, Carsten Schubert, Jiejun Wu, Michael A. Letavic, Ann J. Barbier, Sandy J. Wilson, Marta C. Abad, Brian Lord, Heather McAllister, Kirsten L. Miller, Nicholas I. Carruthers, Emily M. Stocking, D.J. Tognarelli, Jill A. Jablonowski, Timothy W. Lovenberg, Leslie A. Gomez, Pascal Bonaventure, Jamin D. Boggs, Jennifer M. Miller
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:1047-1051
A series of novel 4-aryl-1,2,3,4-tetrahydroisoquinoline-based histamine H(3) ligands that also have serotonin reuptake transporter inhibitor activity is described. The synthesis, in vitro biological data, and select pharmacokinetic data for these nov
Autor:
Francis J. Castellino, James H. Geiger, Raghuvir K. Arni, Marta C. Abad, Davida K. Grella, Alexander Tulinsky
Publikováno v:
Journal of Molecular Biology. 318:1009-1017
Angiogenesis inhibitors have gained much public attention recently as anti-cancer agents and several are currently in clinical trials, including angiostatin (Phase I, Thomas Jefferson University Hospital, Philadelphia, PA). We report here the bowl-sh
Publikováno v:
Acta Crystallographica Section D Biological Crystallography. 58:359-361
Branching enzyme catalyzes the formation of the branch points in glycogen and starch by cleavage of the alpha-1,4 link and its subsequent transfer to the alpha-1,6 position. This paper reports the crystallization and preliminary structural studies of
Autor:
Alan C. Gibbs, John A. Masucci, Bruce E. Maryanoff, Diane K. Luci, Marta C. Abad, Ioanna Petrounia, David F. McComsey, William J. Jones, John O’Neill, Stephen C. Yabut, Alfonzo D. Jordan
Publikováno v:
ACS medicinal chemistry letters. 2(7)
Attenuation of fructose metabolism by the inhibition of ketohexokinase (KHK; fructokinase) should reduce body weight, free fatty acids, and triglycerides, thereby offering a novel approach to treat diabetes and obesity in response to modern diets. We
Publikováno v:
Methods in enzymology. 493
We describe here a method using protein crystallography as the sole detection tool for fragment-based lead discovery. The methodology consists of iterative design, synthesis, and X-ray crystallographic screening of three libraries of compounds. Targe
Autor:
John G. Geisler, Lily Lee Searle, Hossein Askari, Debyendu De, John O’Neill, Michael Kemmerer, James M Lenhard, Jianying Liu, Ling Lin, Xizhen Zhu, Marta C. Abad, Jyotsna Kasturi, Micheal Gaul, Raymond J. Patch, Dionisios Rentzeperis, Mark R. Player, Alexander Kim
Publikováno v:
Journal of medicinal chemistry. 54(3)
Estrogen-related receptor α (ERRα) is an orphan nuclear receptor that has been functionally implicated in the regulation of energy homeostasis. Herein is described the development of diaryl ether based thiazolidenediones, which function as selectiv
Autor:
Zhihua Sui, Marta C. Abad, Francis A. Lewandowski, Xuqing Zhang, Geoffrey T. Struble, Weimei Sun, Alan C. Gibbs, Lawrence C. Kuo, Brett A. Tounge
Publikováno v:
Journal of medicinal chemistry. 53(22)
A fragment-based drug design paradigm has been successfully applied in the discovery of lead series of ketohexokinase inhibitors. The paradigm consists of three iterations of design, synthesis, and X-ray crystallographic screening to progress low mol
Autor:
Shariff Bayoumy, Bruce E. Maryanoff, Lawrence de Garavilla, Jukka Kervinen, Marta C. Abad, Carl Crysler, Michael N. Greco, Ingrid Deckman, John C. Spurlino
Publikováno v:
Biochemical pharmacology. 80(7)
Chymases (EC 3.4.21.39) are mast cell serine proteinases that are variably expressed in different species and, in most cases, display either chymotryptic or elastolytic substrate specificity. Given that chymase inhibitors have emerged as potential th