Search Results - "Gardell, S"

Enhanced Evoked Excitatory Transmitter Release in Experimental Neuropathy Requires Descending Facilitation by Gardell, L. R, Vanderah, T. W, Gardell, S. E, Wang, R, Ossipov, M. H, Lai, J, Porreca, F

“…Nerve injury-induced afferent discharge is thought to elicit spinal sensitization and consequent abnormal pain. Experimental neuropathic pain, however, also…”
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Photoactivated γ-secretase inhibitors directed to the active site covalently label presenilin 1 by Gardell, Stephen J, Li, Yue-Ming, Xu, Min, Lai, Ming-Tain, Huang, Qian, Castro, José L, DiMuzio-Mower, Jillian, Harrison, Timothy, Lellis, Colin, Nadin, Alan, Neduvelil, Joseph G, Register, R. Bruce, Sardana, Mohinder K, Shearman, Mark S, Smith, Adrian L, Shi, Xiao-Ping, Yin, Kuo-Chang, Shafer, Jules A

“…Cleavage of amyloid precursor protein (APP) by the β- and γ-secretases generates the amino and carboxy termini, respectively, of the Aβ amyloidogenic peptides…”
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Effect of tiplaxtinin (PAI‐039), an orally bioavailable PAI‐1 antagonist, in a rat model of thrombosis by HENNAN, J. K., MORGAN, G. A., SWILLO, R. E., ANTRILLI, T. M., MUGFORD, C., VLASUK, G. P., GARDELL, S. J., CRANDALL, D. L.

“…Objective: To assess the antithrombotic and profibrinolytic effects of tiplaxtinin (PAI‐039), an orally bioavailable antagonist of PAI‐1, in rat models of…”
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Effect of the small molecule plasminogen activator inhibitor‐1 (PAI‐1) inhibitor, PAI‐749, in clinical models of fibrinolysis by LUCKING, A. J., VISVANATHAN, A., PHILIPPOU, H., FRASER, S., GRANT, P. J., CONNOLLY, T. M., GARDELL, S. J., FEUERSTEIN, G. Z., FOX, K. A. A., BOOTH, N. A., NEWBY, D. E.

“…Background: The principal inhibitor of fibrinolysis in vivo is plasminogen activator inhibitor‐1 (PAI‐1). PAI‐749 is a small molecule inhibitor of PAI‐1 with…”
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Presenilin 1 Is Linked with γ -Secretase Activity in the Detergent Solubilized State by Li, Yue-Ming, Lai, Ming-Tain, Xu, Min, Huang, Qian, DiMuzio-Mower, Jillian, Sardana, Mohinder K., Shi, Xiao-Ping, Yin, Kuo-Chang, Shafer, Jules A., Gardell, Stephen J.

“…γ -Secretase is a membrane-associated protease that cleaves within the transmembrane region of amyloid precursor protein to generate the C termini of the two…”
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Presenilin-1 and presenilin-2 exhibit distinct yet overlapping gamma-secretase activities by Lai, Ming-Tain, Chen, Elizabeth, Crouthamel, Ming-Chih, DiMuzio-Mower, Jillian, Xu, Min, Huang, Qian, Price, Eric, Register, R Bruce, Shi, Xiao-Ping, Donoviel, Dorit B, Bernstein, Alan, Hazuda, Daria, Gardell, Stephen J, Li, Yue-Ming

“…Presenilin-1 (PS1) and presenilin 2 (PS2) are proposed to be transmembrane aspartyl proteases that cleave amyloid precursor protein and Notch. PS1- and…”
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The Pro Domain of β-Secretase Does Not Confer Strict Zymogen-like Properties but Does Assist Proper Folding of the Protease Domain by Shi, Xiao-Ping, Chen, Elizabeth, Yin, Kuo-Chang, Na, Sang, Garsky, Victor M., Lai, Ming-Tain, Li, Yue-Ming, Platchek, Michael, Register, R. Bruce, Sardana, Mohinder K., Tang, Mei-Jy, Thiebeau, James, Wood, Theresa, Shafer, Jules A., Gardell, Stephen J.

“…β-Secretase (BACE) is a membrane-bound aspartyl protease that cleaves the amyloid precursor protein to generate the N terminus of the amyloid β peptide. BACE…”
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Characterization of plasmin-mediated activation of plasma procarboxypeptidase B. Modulation by glycosaminoglycans by Mao, S S, Cooper, C M, Wood, T, Shafer, J A, Gardell, S J

“…Plasma carboxypeptidase B (PCB) is an exopeptidase that exerts an antifibrinolytic effect by releasing C-terminal Lys and Arg residues from partially degraded…”
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Potent Noncovalent Thrombin Inhibitors That Utilize the Unique Amino Acid d-Dicyclohexylalanine in the P3 Position. Implications on Oral Bioavailability and Antithrombotic Efficacy by Tucker, Thomas J, Lumma, William C, Lewis, S. Dale, Gardell, Stephen J, Lucas, Bobby J, Baskin, Elizabeth P, Woltmann, Richard, Lynch, Joseph J, Lyle, Elizabeth A, Appleby, Sandra D, Chen, I-Wu, Dancheck, Kimberley B, Vacca, Joseph P

“…In an effort to prepare orally bioavailable analogs of our previously reported thrombin inhibitor 1, we have synthesized a series of compounds that utilize the…”
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L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor by Sanderson, Philip E.J., Cutrona, Kellie J., Dorsey, Bruce D., Dyer, Dona L., McDonough, Colleen M., Naylor-Olsen, Adel M., Chen, I-Wu, Chen, Zhongguo, Cook, Jacquelynn J., Gardell, Stephen J., Krueger, Julie A., Lewis, S.Dale, Lin, Jiunn H., Lucas, Bobby J., Lyle, Elizabeth A., Lynch, Joseph J., Stranieri, Maria T., Vastag, Kari, Shafer, Jules A., Vacca, Joseph P.

“…Replacement of the amidinopiperidine P1 group of 3-benzylsulfonylamino-6-methyl-2-pyridinone acetamide thrombin inhibitor L-373,890 ( 2) with a mildly basic…”
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Isolation, characterization, and cDNA cloning of a vampire bat salivary plasminogen activator by Gardell, S J, Duong, L T, Diehl, R E, York, J D, Hare, T R, Register, R B, Jacobs, J W, Dixon, R A, Friedman, P A

“…Vampire bat saliva contains a plasminogen activator that presumably assists these hematophagous animals during feeding. Here, we report that the vampire bat…”
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Discovery of a Novel, Selective, and Orally Bioavailable Class of Thrombin Inhibitors Incorporating Aminopyridyl Moieties at the P1 Position by Feng, Dong-Mei, Gardell, Stephen J, Lewis, S. Dale, Bock, Mark G, Chen, Zhongguo, Freidinger, Roger M, Naylor-Olsen, Adel M, Ramjit, Harri G, Woltmann, Richard, Baskin, Elizabeth P, Lynch, Joseph J, Lucas, Robert, Shafer, Jules A, Dancheck, Kimberley B, Chen, I-Wu, Mao, Shi-Shan, Krueger, Julie A, Hare, Timothy R, Mulichak, Anne M, Vacca, Joseph P

“…A novel class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position has been discovered. Four of these thrombin inhibitors (13b,c,e and…”
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Assessment of thrombin inhibitor efficacy in a novel rabbit model of simultaneous arterial and venous thrombosis by Marsh Lyle, E, Lewis, S D, Lehman, E D, Gardell, S J, Motzel, S L, Lynch, Jr, J J

“…The importance of thrombin in arterial and venous thrombosis renders thrombin inhibition an important therapeutic target. Identification of novel inhibitors…”
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A novel rat carboxypeptidase, CPA2: characterization, molecular cloning, and evolutionary implications on substrate specificity in the carboxypeptidase gene family by Gardell, S J, Craik, C S, Clauser, E, Goldsmith, E J, Stewart, C B, Graf, M, Rutter, W J

“…A new member of the carboxypeptidase gene family, carboxypeptidase A2 (CPA2), has been identified from the predicted amino acid sequence of a rat pancreatic…”
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Design and Synthesis of a Series of Potent and Orally Bioavailable Noncovalent Thrombin Inhibitors That Utilize Nonbasic Groups in the P1 Position by Tucker, Thomas J, Brady, Stephen F, Lumma, William C, Lewis, S. Dale, Gardell, Stephen J, Naylor-Olsen, Adel M, Yan, Youwei, Sisko, Jack T, Stauffer, Kenneth J, Lucas, Bobby J, Lynch, Joseph J, Cook, Jacquelynn J, Stranieri, Maria T, Holahan, Marie A, Lyle, Elizabeth A, Baskin, Elizabeth P, Chen, I-Wu, Dancheck, Kimberly B, Krueger, Julie A, Cooper, Carolyn M, Vacca, Joseph P

“…As part of an ongoing effort to prepare therapeutically useful orally active thrombin inhibitors, we have synthesized a series of compounds that utilize…”
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Efficacious, Orally Bioavailable Thrombin Inhibitors Based on 3-Aminopyridinone or 3-Aminopyrazinone Acetamide Peptidomimetic Templates by Sanderson, Philip E. J, Lyle, Terry A, Cutrona, Kellie J, Dyer, Dona L, Dorsey, Bruce D, McDonough, Colleen M, Naylor-Olsen, Adel M, Chen, I-Wu, Chen, Zhongguo, Cook, Jacquelynn J, Cooper, Carolyn M, Gardell, Stephen J, Hare, Timothy R, Krueger, Julie A, Lewis, S. Dale, Lin, Jiunn H, Lucas, Bobby J, Lyle, Elizabeth A, Lynch, Joseph J, Stranieri, Maria T, Vastag, Kari, Yan, Youwei, Shafer, Jules A, Vacca, Joseph P

“…We have addressed the key deficiency of noncovalent pyridinone acetamide thrombin inhibitor L-374,087 (1), namely, its modest half-lives in animals, by making…”
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The core proteins of large and small interstitial proteoglycans from various connective tissues form distinct subgroups by Heinegård, D, Björne-Persson, A, Cöster, L, Franzén, A, Gardell, S, Malmström, A, Paulsson, M, Sandfalk, R, Vogel, K

“…Large and small proteoglycans were separately isolated from a number of connective tissues and compared to determine the extent of structural similarity. This…”
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Comparison of the bleeding potential of vampire bat salivary plasminogen activator versus tissue plasminogen activator in an experimental rabbit model by MONTONEY, M, GARDELL, S. J, MARDER, V. J

“…Vampire bat salivary plasminogen activator (Bat-PA) has significantly greater fibrin specificity than any of the fibrinolytic agents currently in clinical use…”
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C6 Modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption by Isaacs, Richard C.A., Cutrona, Kellie J., Newton, Christina L., Sanderson, Philip E.J., Solinsky, Mark G., Baskin, Elizabeth P., Chen, I-Wu, Cooper, Carolyn M., Cook, Jacquelynn J., Gardell, Stephen J., Lewis, S.Dale, Lucas, Robert J., Lyle, Elizabeth A., Lynch, Joseph J., Naylor-Olsen, Adel M., Stranieri, Maria T., Vastag, Kari, Vacca, Joseph P.

“…1 (L-374,087) is a potent, selective, efficacious, and orally bioavailable thrombin inhibitor that contains a core 3-amino-2-pyridinone moiety. Replacement of…”
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Vampire bat salivary plasminogen activator exhibits a strict and fastidious requirement for polymeric fibrin as its cofactor, unlike human tissue-type plasminogen activator. A kinetic analysis by BERGUM, P. W, GARDELL, S. J

“…The vampire bat salivary plasminogen activator (BatPA) is virtually inactive toward Glu-plasminogen in the absence of a fibrin-like cofactor, unlike human…”
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