Zobrazeno 1 - 10
of 188
pro vyhledávání: '"Elena Ho"'
Autor:
John Morser, Imadul Islam, Cornell Mallari, Elena Ho, Marc Adler, Kumar Emayan, Gary Phillips, Shendong Yuan, Marc Whitlow, Christopher W. West, David R. Light, Giovanna Gualtieri, Drew Sukovich, Ulrich Bothe, Zheng Chang, Kieu Chu, Judi Bryant, Deborah Chen, Caralee Schaefer, Brad O. Buckman
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 28:3372-3375
We report here the design and synthesis of a novel series of benzylamines that are potent and selective inhibitors of uPA with promising oral availability in rat. Further evaluation of one representative (ZK824859) of the new structural class showed
Autor:
Xiao Yan Zhao, Andreas Baumann, Thomas Schwarz, Joachim Schuhmacher, Babu Subramanyan, Chandra Patel, Maria Koellnberger, Kathy Tran, Elena Ho, Jian-Ming Gu, Timothy Myles
Publikováno v:
The AAPS Journal. 19:1186-1195
BAY 1093884 is a fully human monoclonal antibody against the tissue factor pathway inhibitor (TFPI) in development as prophylaxis in patients with hemophilia with or without inhibitors. In vitro, BAY 1093884 binds to human, mouse, and monkey TFPI. Th
Autor:
Elena Ho, Hironao Wakabayashi, Derek Sim, Katherine Tran, Philip J. Fay, Thomas Eugene Thompson, Perry Liu, Lilley Leong, Chandra Patel, Peter J. Kretschmer, J. E. Murphy
Publikováno v:
Blood. 125:392-398
An important negative regulator of factor VIIIa (FVIIIa) cofactor activity is A2 subunit dissociation. FVIII molecules with stabilized activity have been generated by elimination of charged residues at the A1-A2 and A2-A3 interfaces. These molecules
Publikováno v:
Biochemical and Biophysical Research Communications. 440:485-489
Addition of N-linked glycosylation sites has been shown to increase serum half-life and decrease clearance for proteins such as recombinant erythropoietin (EPO). However, factor IX (FIX) variants with additional N-linked glycans (“HG” variants) t
Autor:
Lilley Leong, Derek Sim, R. I. Feldman, L. Tang, H. Jiang, Elena Ho, F. Monteclaro, D. Schneider, J.-M. Gu, J. E. Murphy
Publikováno v:
Haemophilia. 19:539-545
PEGylation of B-domain deleted factor VIII (PEG-FVIII-BDD) prolongs the half-life of the molecule by approximately twofold in animals (Mei et al., Blood 2010; 116: 270). To investigate the role of von Willebrand factor (vWF) in the catabolism of PEG-
Autor:
Loki Natarajan, Michael H. Criqui, Julie O. Denenberg, Victor Aboyans, Lindsey A. Ho, Elena Ho
Publikováno v:
Journal of Vascular Surgery. 48(5):1197-1203
ObjectiveThe presence of a high ankle-brachial index (ABI) is related to stiff ankle arteries due to medial calcification. Recently, this condition has attracted new interest after reports of a worse cardiovascular prognosis, similar to a low ABI. We
Autor:
Richard I. Feldman, Gary Phillips, Marc Adler, Daguang Zhu, Elena Ho, Wheeseong Lee, Mark A. Polokoff, Hongyi Yu, Dao Lentz, Marc Whitlow, Arnaiz Damian O, Kochanny Monica, Babu Subramanyam, Imadul Islam, James M. Wu, Judi Bryant, Yuo-Ling Chou
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:3814-3818
HTS screening identified 1 with micromolar inhibitory activity against PDK1. Optimization of 1 afforded 4i (BX-517) which has single-digit nanomolar activity against PDK1 and excellent selectivity against PKA.
Autor:
Jih-Lie Tseng, David D. Davey, Mark A. Polokoff, Gary Phillips, Raju Mohan, Marc Whitlow, Shendong Yuan, Marc Adler, Robert G. Wei, Elena Ho, Wei Xu
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 17:2499-2504
A new series of 1-(1,3-benzodioxol-5-ylmethyl)-3-[4-(1H-Imidazol-1-yl)phenoxy]-piperidine analogs were designed and identified as potent and selective inhibitors of NO formation based both on the crystal structure of a murine iNOS Δ114 monomer domai
Autor:
Julie O. Denenberg, Richard R. Fabsitz, Matthew A. Allison, Anne B. Newman, Robert Langer, Elena Ho, Michael H. Criqui
Publikováno v:
American Journal of Preventive Medicine. 32:328-333
Background Individuals diagnosed with peripheral arterial disease (PAD) are at increased risk for future functional limitations as well as cardiovascular morbidity and mortality. The aim of this study was to estimate the age-, gender-, and ethnic-spe
Autor:
Dao Lentz, Marc Whitlow, Kenneth J. Shaw, Karna Lyn Sacchi, Sakata Steven T, Janette Walters, Kathy White, Joseph Post, Bin Ye, Wheeseong Lee, Kochanny Monica, Elena Ho, Amy Liang, Ron Vergona, Janice Ewing, Morrissey Michael M, Karanjawala Rushad E, Gary Phillips, Zuchun Zhao, Brian D. Griedel, Babu Subramanyam, Marc Adler
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:2127-2146
A series of thiophene-containing non-amidine factor Xa inhibitors is described. Simple methyl-substituted thiophene analogs were relatively weak inhibitors. However, introduction of hydrophilic substituents at C-4 or C-5 of the thiophene afforded inh