Search Results - "Tapparelli, Carlo"
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Synthetic low-molecular weight thrombin inhibitors: molecular design and pharmacological profile
Published in Trends in pharmacological sciences (Regular ed.) (01-10-1993)“…Thrombin is a multifunctional protein: in addition to its role in coagulation, thrombin has important biological effects on platelets, endothelial and smooth…”
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High level expression of human apolipoprotein A-I in transgenic rats raises total serum high density lipoprotein cholesterol and lowers rat apolipoprotein A-I
Published in Transgenic research (01-05-1992)“…To examine the consequences of increased apolipoprotein A-I production on cholesterol and lipoprotein metabolism, we have produced two lines of transgenic…”
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Characterization of the P2‘ and P3‘ Specificities of Thrombin Using Fluorescence-Quenched Substrates and Mapping of the Subsites by Mutagenesis
Published in Biochemistry (Easton) (04-06-1996)“…The importance of substrate residues P2‘ and P3‘ on thrombin catalysis has been investigated by comparing the hydrolysis of a series of fluorescence-quenched…”
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Design, synthesis and biological evaluation of selective boron-containing thrombin inhibitors
Published in Bioorganic & medicinal chemistry (01-07-1999)“…Based on the structural comparison of the S-1 pocket in different trypsin-like serine proteases, a series of Boc-D-trimethylsilylalanine-proline-boro-X…”
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Selective boron-Containing thrombin inhibitors—X-ray analysis reveals surprising binding mode
Published in Bioorganic & medicinal chemistry (01-09-2000)“…Based on the structural comparison of the S1 pocket in different trypsin-like serine proteases, a series of Boc- d-trimethylsilylalanine-proline-boro-X…”
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Thrombin inhibitors as antithrombotic agents: the importance of rapid inhibition
Published in Journal of enzyme inhibition (1995)“…For use as an antithrombotic agent, a thrombin inhibitor must be potent and specific, i.e., it should not significantly inhibit the proteases of the…”
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Beta-amino acid derivatives as orally active non-peptide fibrinogen receptor antagonists
Published in Bioorganic & medicinal chemistry letters (18-03-1997)“…The omithine sulfonamide 1 was identified by random screening as weak fibrinogen receptor antagonist. Homologation of the carboxylic acid function and further…”
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In vitro and in vivo characterization of a neutral boron-containing thrombin inhibitor
Published in The Journal of biological chemistry (05-03-1993)“…Peptide boronic acid derivatives have proven to be very potent inhibitors of serine proteases with boroarginine derivatives being particularly potent thrombin…”
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Platelet aggregation and fibrinogen binding in human, rhesus monkey, guinea-pig, hamster and rat blood: activation by ADP and a thrombin receptor peptide and inhibition by glycoprotein IIb/IIIa antagonists
Published in Thrombosis and haemostasis (01-09-1993)“…Platelet aggregation and fibrinogen binding in whole blood, induced either by ADP or by a 14 amino acid peptide mimicking an N-terminal region of the platelet…”
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Structure and function of thrombin receptors
Published in Trends in pharmacological sciences (Regular ed.) (01-12-1993)Get more information
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Antithrombotic activity in vivo of SDZ 217-766, a low-molecular weight thrombin inhibitor in comparison to heparin
Published in Thrombosis and haemostasis (01-04-1995)“…Antithrombotic potency of SDZ 217-766, a potent inhibitor of thrombin and other trypsin-like serine proteases, was studied in comparison with heparin in rat…”
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Inhibition of exocytosis by intracellularly applied antibodies against a chromaffin granule-binding protein
Published in Nature (London) (29-06-1989)“…Exocytotic secretion requires the interaction and fusion of secretory vesicles with the plasma membrane. This process could be mediated by specific recognition…”
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Pharmacological studies on frozen stored canine saphenous veins and basilar arteries
Published in Naunyn-Schmiedeberg's archives of pharmacology (1986)“…Canine saphenous veins were either placed in Krebs-Henseleit solution and stored for 24 h at +4 degrees C, or immersed in FCS (fetal calf serum) containing 1.8…”
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Release of platelet Met-enkephalin, but not serotonin, in migraine. A platelet response unique to migraine patients?
Published in Journal of the neurological sciences (01-10-1989)“…Plasma-induced release of platelet-serotonin and Met-enkephalin was studied by incubating platelets from migraineurs, tension headache patients and healthy…”
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Comparison of the actions of serotoninergic agents on human saphenous veins and platelets
Published in European journal of pharmacology (13-05-1986)“…Changes in tension of helical strips from human saphenous veins and reversible aggregation of human platelets were recorded in vitro. Comparison of the…”
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Methylergometrine, an active metabolite of methysergide
Published in Cephalalgia (01-03-1986)“…In conscious dogs methysergide (MS) caused constriction of the saphenous vein at about 3000 times lower doses than methylergometrine (MT) when infused locally,…”
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Detergents inhibit exocytosis in PC 12 cells: evidence for an effect on ion fluxes
Published in Journal of cellular biochemistry (01-04-1987)“…Membrane events in exocytosis were studied by examining the effect of different detergents on the K+-stimulated release of noradrenaline in the secretory cell…”
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Hemodynamic, antivasoconstrictor, and antiatherosclerotic effects of calcium antagonists in animal models of atherosclerosis
Published in Journal of cardiovascular pharmacology (1990)“…Calcium antagonists retard the development of atherosclerosis in cholesterol-fed rabbits and modestly enhance regression after their return to a normal diet…”
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Inhibition of exocytosis by intracellularly applied antibodies against a chromaffin granule-binding protein
Published in Nature (London) (27-07-1989)Get full text
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