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Gardell, Stephen J, PhD
Overview
Publications
Most Recent Publications
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2024Genetic drivers of human plasma metabolites that determine mortality in heart failure patients with reduced ejection fraction. FRONTIERS IN CARDIOVASCULAR MEDICINE. 11.Full Text via DOI: 10.3389/fcvm.2024.1409340 PMID: 39045004
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2024The TAS1R2 G-protein-coupled receptor is an ambient glucose sensor in skeletal muscle that regulates NAD homeostasis and mitochondrial capacity. NATURE COMMUNICATIONS. 15.Full Text via DOI: 10.1038/s41467-024-49100-8 PMID: 38851747
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2023Comprehensive interrogation of human skeletal muscle reveals a dissociation between insulin resistance and mitochondrial capacity. AMERICAN JOURNAL OF PHYSIOLOGY-ENDOCRINOLOGY AND METABOLISM. 325:E291-E302.Full Text via DOI: 10.1152/ajpendo.00143.2023 PMID: 37584609
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2023Circulating Metabolomic Profile Predicts Change In Ejection Fraction In Heart Failure Patients. JOURNAL OF CARDIAC FAILURE. 569-569.
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2023Source of nicotinamide governs its metabolic fate in cultured cells, mice, and humans. CELL REPORTS. 42.Full Text via DOI: 10.1016/j.celrep.2023.112218 PMID: 36897780
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2023Exercise and ageing impact the kynurenine/tryptophan pathway and acylcarnitine metabolite pools in skeletal muscle of older adults. JOURNAL OF PHYSIOLOGY-LONDON.Full Text via DOI: 10.1113/JP284142 PMID: 36814134
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2022NAD(+) and human muscle health. NATURE AGING. 195-196.Full Text via DOI: 10.1038/s43587-022-00192-1 PMID: 37118373
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2021A Metabolomic Signature of Glucagon Action in Healthy Individuals With Overweight/Obesity. JOURNAL OF THE ENDOCRINE SOCIETY. 5.Full Text via DOI: 10.1210/jendso/bvab118 PMID: 34337278
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2021Discovery of 1-[2-(1-methyl-1H-pyrazol-5-yl)-[1,2,4]triazolo[1,5-a] pyridin-6-yl]-3-(pyridin-4-ylmethyl)urea as a potent NAMPT (nicotinamide phosphoribosyltransferase) activator with attenuated CYP inhibition. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. 43.Full Text via DOI: 10.1016/j.bmcl.2021.128048 PMID: 33887438
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2021Optimization of a urea-containing series of nicotinamide phosphoribosyltransferase (NAMPT) activators. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. 41.Full Text via DOI: 10.1016/j.bmcl.2021.128007 PMID: 33798699
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2021Metabolic adaptation characterizes short-term resistance to weight loss induced by a low-calorie diet in overweight/obese individuals.. The American journal of clinical nutrition. 267-280.Full Text via DOI: 10.1093/ajcn/nqab027 PMID: 33826697
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2019Boosting NAD(+) with a small molecule that activates NAMPT. NATURE COMMUNICATIONS. 10.Full Text via DOI: 10.1038/s41467-019-11078-z PMID: 31324777
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2019Measurement of Pyridine Nucleotides in Biological Samples Using LC-MS/MS. METABOLOMICS: METHODS AND PROTOCOLS. 1996:61-73.Full Text via DOI: 10.1007/978-1-4939-9488-5_7 PMID: 31127548
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2019Metabolomics Analyses of Muscle Atrophy Induced by Hind Limb Unloading. METABOLOMICS: METHODS AND PROTOCOLS. 1996:297-309.Full Text via DOI: 10.1007/978-1-4939-9488-5_22 PMID: 31127563
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2018Impaired Mitochondrial Energetics Characterize Poor Early Recovery of Muscle Mass Following Hind Limb Unloading in Old Mice. JOURNALS OF GERONTOLOGY SERIES A-BIOLOGICAL SCIENCES AND MEDICAL SCIENCES. 73:1313-1322.Full Text via DOI: 10.1093/gerona/gly051 PMID: 29562317
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2018Elevated Nicotinamide Phosphoribosyl Transferase in Skeletal Muscle Augments Exercise Performance and Mitochondrial Respiratory Capacity Following Exercise Training. FRONTIERS IN PHYSIOLOGY. 9.Full Text via DOI: 10.3389/fphys.2018.00704 PMID: 29942262
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2018Skeletal muscle overexpression of nicotinamide phosphoribosyl transferase in mice coupled with voluntary exercise augments exercise endurance. MOLECULAR METABOLISM. 7:1-11.Full Text via DOI: 10.1016/j.molmet.2017.10.012 PMID: 29146412
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2017Targeted Metabolomic Profiling of Plasma and Survival in Heart Failure Patients. JACC-HEART FAILURE. 5:823-832.Full Text via DOI: 10.1016/j.jchf.2017.07.009 PMID: 29096792
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2016Use of Ion Chromatography/Mass Spectrometry for Targeted Metabolite Profiling of Polar Organic Acids. ANALYTICAL CHEMISTRY. 88:11799-11803.Full Text via DOI: 10.1021/acs.analchem.6b03435 PMID: 27782384
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2016Presence of arachidonoyl-carnitine is associated with adverse cardiometabolic responses in hypertensive patients treated with atenolol. METABOLOMICS. 12.Full Text via DOI: 10.1007/s11306-016-1098-2 PMID: 28217401
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2016The Failing Heart Relies on Ketone Bodies as a Fuel. CIRCULATION. 133:698-705.Full Text via DOI: 10.1161/CIRCULATIONAHA.115.017355 PMID: 26819376
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2013Rotenone induces reductive stress and triacylglycerol deposition in C2C12 cells. INTERNATIONAL JOURNAL OF BIOCHEMISTRY & CELL BIOLOGY. 45:2749-2755.Full Text via DOI: 10.1016/j.biocel.2013.09.011 PMID: 24104397
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2010Cardiovascular Drug Discovery in the Academic Setting: Building Infrastructure, Harnessing Strengths, and Seeking Synergies. JOURNAL OF CARDIOVASCULAR TRANSLATIONAL RESEARCH. 3:431-437.Full Text via DOI: 10.1007/s12265-010-9204-8 PMID: 20625868
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2010Effect of the small molecule plasminogen activator inhibitor-1 (PAI-1) inhibitor, PAI-749, in clinical models of fibrinolysis. JOURNAL OF THROMBOSIS AND HAEMOSTASIS. 8:1333-1339.Full Text via DOI: 10.1111/j.1538-7836.2010.03872.x PMID: 20345708
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2009LXR ligand lowers LDL cholesterol in primates, is lipid neutral in hamster, and reduces atherosclerosis in mouse. JOURNAL OF LIPID RESEARCH. 50:2358-2370.Full Text via DOI: 10.1194/jlr.M900037-JLR200 PMID: 19318684
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2009Selective Kv1.5 Blockers: Development of (R)-1-(Methylsulfonylamino)-3-[2-(4-methoxyphenyl)ethyl]-4-(4-methoxyphenyl)-2-imidazolidinone (KVI-020/WYE-160020) as a Potential Treatment for Atrial Arrhythmia. JOURNAL OF MEDICINAL CHEMISTRY. 52:6531-6534.Full Text via DOI: 10.1021/jm901042m PMID: 19888755
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2009GAP-134 ([2S,4R]-1-[2-Aminoacetyl]-4-Benzamidopyrrolidine-2-Carboxylic Acid) Prevents Spontaneous Ventricular Arrhythmias and Reduces Infarct Size During Myocardial Ischemia/Reperfusion Injury in Open-Chest Dogs. JOURNAL OF CARDIOVASCULAR PHARMACOLOGY AND THERAPEUTICS. 14:207-214.Full Text via DOI: 10.1177/1074248409340779 PMID: 19721133
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2009Activation of farnesoid X receptor prevents atherosclerotic lesion formation in LDLR-/- and apoE(-/-) mice. JOURNAL OF LIPID RESEARCH. 50:1090-1100.Full Text via DOI: 10.1194/jlr.M800619-JLR200 PMID: 19174369
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2009The Gap Junction Modifier, GAP-134 [(2S,4R)-1-(2-Aminoacetyl)-4-benzamido-pyrrolidine-2-carboxylic Acid], Improves Conduction and Reduces Atrial Fibrillation/Flutter in the Canine Sterile Pericarditis Model. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS. 329:1127-1133.Full Text via DOI: 10.1124/jpet.108.150102 PMID: 19252062
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2009A synthetic farnesoid X receptor (FXR) agonist promotes cholesterol lowering in models of dyslipidemia. AMERICAN JOURNAL OF PHYSIOLOGY-GASTROINTESTINAL AND LIVER PHYSIOLOGY. 296:G543-G552.Full Text via DOI: 10.1152/ajpgi.90585.2008 PMID: 19136377
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2008Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride Synthesis. JOURNAL OF MEDICINAL CHEMISTRY. 51:7161-7168.Full Text via DOI: 10.1021/jm800799q PMID: 18973288
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2008Effect of tiplaxtinin (PAI-039), an orally bioavailable PAI-1 antagonist, in a rat model of thrombosis. JOURNAL OF THROMBOSIS AND HAEMOSTASIS. 6:1558-1564.Full Text via DOI: 10.1111/j.1538-7836.2008.03063.x PMID: 18624980
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2008Enhanced clearance of A beta in brain by sustaining the plasmin proteolysis cascade. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA. 105:8754-8759.Full Text via DOI: 10.1073/pnas.0710823105 PMID: 18559859
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2007Small-molecule ghrelin receptor antagonists improve glucose tolerance, suppress appetite, and promote weight loss. ENDOCRINOLOGY. 148:5175-5185.Full Text via DOI: 10.1210/en.2007-0239 PMID: 17656463
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2007Quinazolinone derivatives as orally available ghrelin receptor antagonists for the treatment of diabetes and obesity. JOURNAL OF MEDICINAL CHEMISTRY. 50:5202-5216.Full Text via DOI: 10.1021/jm070071+ PMID: 17887659
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2007Neutralization of plasminogen activator inhibitor I (PAI-1) by the synthetic antagonist PAI-749 via a dual mechanism of action. MOLECULAR PHARMACOLOGY. 72:897-906.Full Text via DOI: 10.1124/mol.107.037010 PMID: 17622579
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2006A presenilin-independent aspartyl protease prefers the gamma-42 site cleavage. JOURNAL OF NEUROCHEMISTRY. 96:118-125.Full Text via DOI: 10.1111/j.1471-4159.2005.03528.x PMID: 16300640
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2005P-2 pyridine N-oxide thrombin inhibitors: a novel peptidomimetic scaffold. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. 15:2771-2775.Full Text via DOI: 10.1016/j.bmcl.2005.03.110 PMID: 15911253
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2003Electrochemiluminescence assay for basic carboxypeptidases: inhibition of basic carboxypeptidases and activation of thrombin-activatable fibrinolysis inhibitor. ANALYTICAL BIOCHEMISTRY. 319:159-170.Full Text via DOI: 10.1016/S0003-2697(03)00252-5 PMID: 12842119
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2003Presenilin-1 and presenilin-2 exhibit distinct yet overlapping gamma-secretase activities. JOURNAL OF BIOLOGICAL CHEMISTRY. 278:22475-22481.Full Text via DOI: 10.1074/jbc.M300974200 PMID: 12684521
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2003Miniaturizable homogenous time-resolved fluorescence assay for carboxypeptidase B activity. ANALYTICAL BIOCHEMISTRY. 317:94-98.Full Text via DOI: 10.1016/S0003-2697(03)00048-4 PMID: 12729605
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2003Pharmacokinetic optimization of 3-amino-6-chloropyrazinone acetamide thrombin inhibitors. Implementation of P3 pyridine N-oxides to deliver an orally bioavailable series containing P1N-benzylamides. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. 13:1353-1357.Full Text via DOI: 10.1016/S0960-894X(03)00099-4 PMID: 12657281
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2003Metabolism-directed optimization of 3-aminopyrazinone acetamide thrombin inhibitors. Development of an orally bioavailable series containing P1 and P3 pyridines. JOURNAL OF MEDICINAL CHEMISTRY. 46:461-473.Full Text via DOI: 10.1021/jm020311f PMID: 12570369
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2002gamma-Secretase: characterization and implication for Alzheimer disease therapy. NEUROBIOLOGY OF AGING. 23:1023-1030.PMID: 12470798
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2001The Pro domain of beta-secretase does not confer strict zymogen-like properties but does assist proper folding of the protease domain. JOURNAL OF BIOLOGICAL CHEMISTRY. 276:10366-10373.PMID: 11266439
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2001A beta pp secretases are co-expressed with A beta pp in the pancreatic islets. JOURNAL OF ALZHEIMERS DISEASE. 3:393-396.Full Text via DOI: 10.3233/JAD-2001-3405 PMID: 12214042
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2000Photoactivated gamma-secretase inhibitors directed to the active site covalently label presenilin 1. NATURE. 405:689-694.PMID: 10864326
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2000Presenilin 1 is linked with gamma-secretase activity in the detergent solubilized state. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA. 97:6138-6143.PMID: 10801983
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1999Characterization of plasmin-mediated activation of plasma procarboxypeptidase B - Modulation by glycosaminoglycans. JOURNAL OF BIOLOGICAL CHEMISTRY. 274:35046-35052.PMID: 10574983
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1999Antithrombotic efficacy of thrombin inhibitor L-374,087: Intravenous activity in a primate model of venous thrombus extension and oral activity in a canine model of primary venous and coronary artery thrombosis. JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS. 289:503-510.PMID: 10087043
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1998Efficacious, orally bioavailable thrombin inhibitors based on 3-aminopyridinone or 3-aminopyrazinone acetamide peptidomimetic templates. JOURNAL OF MEDICINAL CHEMISTRY. 41:4466-4474.PMID: 9804686
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1998Design and synthesis of a series of potent and orally bioavailable noncovalent thrombin inhibitors that utilize nonbasic groups in the P1 position. JOURNAL OF MEDICINAL CHEMISTRY. 41:3210-3219.PMID: 9703466
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1998C6 modification of the pyridinone core of thrombin inhibitor L-374,087 as a means of enhancing its oral absorption. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. 8:1719-1724.PMID: 9873422
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1998L-374,087, an efficacious, orally bioavailable, pyridinone acetamide thrombin inhibitor. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. 8:817-822.PMID: 9871547
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1998Assessment of thrombin inhibitor efficacy in a novel rabbit model of simultaneous arterial and venous thrombosis. THROMBOSIS AND HAEMOSTASIS. 79:656-662.PMID: 9531058
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1998Characterization of the two-step pathway for inhibition of thrombin by alpha-ketoamide transition state analogs. JOURNAL OF BIOLOGICAL CHEMISTRY. 273:4843-4854.PMID: 9478925
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1998Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): Coapplication of structure-based design and rapid multiple analogue synthesis on solid support. JOURNAL OF MEDICINAL CHEMISTRY. 41:401-406.PMID: 9464370
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1998Novel anticoagulants based an direct inhibition of thrombin and factor Xa. CORONARY ARTERY DISEASE. 9:75-81.PMID: 9647407
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1997Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position. JOURNAL OF MEDICINAL CHEMISTRY. 40:3726-3733.PMID: 9371237
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1997Synthesis of a series of potent and orally bioavailable thrombin inhibitors that utilize 3,3-disubstituted propionic acid derivatives in the P-3 position. JOURNAL OF MEDICINAL CHEMISTRY. 40:3687-3693.PMID: 9357536
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1997Potent noncovalent thrombin inhibitors that utilize the unique amino acid D-dicyclohexylalanine in the P3 position. Implications on oral bioavailability and antithrombotic efficacy. JOURNAL OF MEDICINAL CHEMISTRY. 40:1565-1569.PMID: 9171866
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1995
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1995VAMPIRE BAT SALIVARY PLASMINOGEN-ACTIVATOR EVOKES MINIMAL BLEEDING RELATIVE TO TISSUE-TYPE PLASMINOGEN-ACTIVATOR AS ASSESSED BY A RABBIT CUTICLE BLEEDING-TIME MODEL. THROMBOSIS AND HAEMOSTASIS. 73:478-483.PMID: 7545321
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1995HUMAN ERYTHROLEUKEMIC (HEL) CELLS EXPRESS A PLATELET P2T-LIKE ADP RECEPTOR. THROMBOSIS RESEARCH. 77:235-247.PMID: 7740516
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1993THE SEARCH FOR THE IDEAL THROMBOLYTIC AGENT - MAXIMIZE THE BENEFIT AND MINIMIZE THE RISK. TOXICOLOGIC PATHOLOGY. 21:190-198.PMID: 8210941
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1993VAMPIRE BAT SALIVARY PLASMINOGEN-ACTIVATOR. PROTEOLYTIC ENZYMES IN COAGULATION, FIBRINOLYSIS, AND COMPLEMENT ACTIVATION, PART B. 233-249.PMID: 8271956
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1992HEPARIN ENHANCES ACTIVE SITE-DEPENDENT BINDING OF TISSUE-TYPE PLASMINOGEN-ACTIVATOR TO ENDOTHELIAL-CELLS. BLOOD. 80:1486-1495.PMID: 1520875
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1992VAMPIRE 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. JOURNAL OF BIOLOGICAL CHEMISTRY. 267:17726-17731.PMID: 1387641
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1992VAMPIRE BAT SALIVARY PLASMINOGEN-ACTIVATOR PROMOTES ROBUST LYSIS OF PLASMA CLOTS IN A PLASMA MILIEU WITHOUT CAUSING FLUID PHASE PLASMINOGEN ACTIVATION. THROMBOSIS AND HAEMOSTASIS. 68:165-169.PMID: 1412162
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1992VAMPIRE BAT SALIVARY PLASMINOGEN-ACTIVATOR PROMOTES RAPID AND SUSTAINED REPERFUSION WITHOUT CONCOMITANT SYSTEMIC PLASMINOGEN ACTIVATION IN A CANINE MODEL OF ARTERIAL THROMBOSIS. ARTERIOSCLEROSIS AND THROMBOSIS. 12:212-221.PMID: 1371932
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1991
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1991COMBINATORIAL MUTAGENESIS OF THE REACTIVE SITE REGION IN PLASMINOGEN-ACTIVATOR INHIBITOR-I. JOURNAL OF BIOLOGICAL CHEMISTRY. 266:8495-8500.PMID: 2022663
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1990THE PHARMACOKINETICS OF PLASMINOGEN-ACTIVATOR INHIBITOR-1 IN THE RABBIT. BLOOD. 76:1514-1520.PMID: 2207327
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1990PURIFICATION AND CHARACTERIZATION OF HUMAN PLASMINOGEN-ACTIVATOR INHIBITOR TYPE-I EXPRESSED IN SACCHAROMYCES-CEREVISIAE. ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS. 278:467-474.PMID: 2183723
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1989ISOLATION, CHARACTERIZATION, AND CDNA CLONING OF A VAMPIRE BAT SALIVARY PLASMINOGEN-ACTIVATOR. JOURNAL OF BIOLOGICAL CHEMISTRY. 264:17947-17952.PMID: 2509450
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1968BIOSYNTHESIS OF GLYCOSAMINOGLYCANS (MUCOPOLYSACCHARIDES) IN HUMAN LEUKOCYTES. BIOCHIMICA ET BIOPHYSICA ACTA. 165:309-&.PMID: 4243121
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1967ANALYSIS OF AORTIC GLYCOSAMINOGLYCANS FROM VARIOUS ANIMAL SPECIES BY CPC-CELLULOSE COLUMN PROCEDURES. JOURNAL OF ATHEROSCLEROSIS RESEARCH. 7:283-&.PMID: 6036101
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1965AN ION-EXCHANGE COLUMN CHROMATOGRAPHIC METHOD FOR SEPARATION AND QUANTITATIVE ANALYSIS OF NEUTRAL MONOSACCHARIDES. ANALYTICAL BIOCHEMISTRY. 13:177-&.PMID: 5863677
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- Stephen J Gardell, PhD