Search Results - "Elrod, Kyle C"
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Factor VIIa inhibitors: Chemical optimization, preclinical pharmacokinetics, pharmacodynamics, and efficacy in an arterial baboon thrombosis model
Published in Bioorganic & medicinal chemistry letters (01-04-2006)“…Highly selective and potent factor VIIa–tissue factor (fVIIa · TF) complex inhibitors were generated through structure-based design. The pharmacokinetic…”
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Lactoferrin, a potent tryptase inhibitor, abolishes late-phase airway responses in allergic sheep
Published in American journal of respiratory and critical care medicine (01-08-1997)“…Tryptase, a serine protease released exclusively from activated mast cells, has been implicated as a potential causative agent in asthma. Enzymatically active…”
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High-Throughput Screening of Enzyme Inhibitors: Simultaneous Determination of Tight-Binding Inhibition Constants and Enzyme Concentration
Published in Analytical biochemistry (01-11-2000)“…Active site titration by a reversible tight-binding inhibitor normally depends on prior knowledge of the inhibition constant. Conversely, the determination of…”
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Potent bivalent inhibition of human tryptase-beta by a synthetic inhibitor
Published in Biological chemistry (01-12-2003)“…Human tryptase-beta (HTbeta) is a unique serine protease exhibiting a frame-like tetramer structure with four active sites directed toward a central pore…”
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High-Throughput Screening of Enzyme Inhibitors: Automatic Determination of Tight-Binding Inhibition Constants
Published in Analytical biochemistry (15-05-2000)“…Determination of tight-binding inhibition constants by nonlinear least-squares regression requires sufficiently good initial estimates of the best-fit values…”
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Small molecule inhibitors of plasma kallikrein
Published in Bioorganic & medicinal chemistry letters (01-04-2006)“…Plasma kallikrein is a serine protease that is involved in pathways of inflammation, complement fixation, coagulation, and fibrinolysis. Herein, we describe…”
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A Novel Approach to Serine Protease Inhibition: Kinetic Characterization of Inhibitors Whose Potencies and Selectivities Are Dramatically Enhanced by Zinc(II)
Published in Biochemistry (Easton) (25-04-2000)“…Serine proteases play a role in a variety of disease states and thus are attractive targets for therapeutic intervention. We report the kinetic…”
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Metal mediated protease inhibition: design and synthesis of inhibitors of the human cytomegalovirus (hCMV) protease
Published in Bioorganic & medicinal chemistry letters (16-10-2000)“…A versatile synthetic route to a novel series of bis-imidazolemethanes designed to inhibit the hCMV protease has been developed and a series of potential metal…”
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Expression, purification, crystallization and preliminary X-ray diffraction studies of human cathepsin F complexed with an irreversible vinyl sulfone inhibitor
Published in Acta crystallographica. Section D, Biological crystallography. (01-12-2002)“…Cathepsin F is a cysteine protease believed to be involved in the antigen‐presenting process of the class II major histocompatibility complex (MHC‐II) in…”
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Neutrophil Myeloperoxidase Is a Potent and Selective Inhibitor of Mast Cell Tryptase
Published in Archives of biochemistry and biophysics (01-06-1999)“…Myeloperoxidase (MPO) is an important component of the neutrophil response to microbial infection. In this paper we report an additional activity of MPO, the…”
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Expression and Characterization of Recombinant Mast Cell Tryptase
Published in Protein expression and purification (01-04-1999)“…Tryptase, a serine protease, is the major protein component in mast cells. In an animal model of asthma, tryptase has been established as an important mediator…”
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