Search Results - "Savage, Paula"
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The importance of male underwear in cases of alleged sexual assault
Published in Journal of forensic sciences (01-07-2024)“…The potential evidential value of male underwear in cases of alleged sexual assault is often overlooked. Male underwear can be a critical item in the…”
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Isoindolines: A new series of potent and selective endothelin-A receptor antagonists
Published in Bioorganic & medicinal chemistry letters (09-07-2001)“…1,3-Disubstituted isoindolines have been discovered as a new class of potent functional ET A selective receptor antagonists through pharmacophore analysis of…”
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Design and Synthesis of Potent, Selective Inhibitors of Endothelin-Converting Enzyme
Published in Journal of medicinal chemistry (23-04-1998)“…Endothelin-1 is the most potent peptidic vasoconstrictor discovered to date. The final step of posttranslational processing of this peptide is the conversion…”
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Potent non-peptidic dual inhibitors of endothelin-converting enzyme and neutral endopeptidase 24.11
Published in Bioorganic & medicinal chemistry letters (22-04-1997)“…Structural modifications of CGS 26303, a non-peptidic α-aminophosphonate dual ECE/NEP inhibitor lead, were performed to maximize inhibition of recombinant…”
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Early thymus and activation-regulated chemokine (TARC) reduction and response following panobinostat treatment in patients with relapsed/refractory Hodgkin lymphoma following autologous stem cell transplant
Published in Leukemia & lymphoma (01-05-2014)“…Abstract In a phase 2 trial of panobinostat in 129 patients with relapsed or refractory Hodgkin lymphoma, exploratory analyses of chemokines and cytokines were…”
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Identification and partial purification of a thiol endothelin-converting enzyme from porcine aortic endothelial cells
Published in Journal of biochemistry (Tokyo) (01-03-1992)“…Endothelin is a potent peptide vasoconstrictor. The final step in the processing of endothelin has been postulated to be the cleavage of the Trp21-Val22…”
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Potent and Selective Non-Peptidic Inhibitors of Endothelin-Converting Enzyme-1 with Sustained Duration of Action
Published in Journal of medicinal chemistry (10-02-2000)“…Potent and selective non-peptidic inhibitors of human endothelin-converting enzyme-1 (ECE-1) have been designed as potential modulators of endothelin (ET-1)…”
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Safety, Pharmacokinetics (PK), Metabolism, and Mass Balance of [14C]-AMN107, a Novel Aminopyrimidine Inhibitor of Bcr-Abl Tyrosine Kinase, in Healthy Subjects
Published in Blood (16-11-2005)“…Background: AMN107, a selective and potent inhibitor of Bcr-Abl tyrosine kinase signaling, has demonstrated activity against imatinib resistant forms of…”
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Upregulation of endothelin-1 binding in tissues of salt-loaded stroke-prone spontaneously hypertensive rats
Published in Canadian journal of physiology and pharmacology (01-05-2002)“…Upon maintained on a 1% NaCl drinking solution beginning at 7 weeks of age, the stroke-prone spontaneously hypertensive rat (SHRsp) developed severe…”
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CGS 35601 and its Orally Active Prodrug CGS 37808 as Triple Inhibitors of Endothelin-converting Enzyme-1, Neutral Endopeptidase 24.11, and Angiotensin-converting Enzyme
Published in Journal of cardiovascular pharmacology (01-11-2004)“…CGS 35601 is a potent triple inhibitor of endothelinconverting enzyme-1, neutral endopeptidase 24.11, and angiotensinconverting enzyme. It inhibited the…”
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CGS 34226, a thiol-based dual inhibitor of endothelin converting enzyme-1 and neutral endopeptidase 24.11
Published in Clinical science (1979) (01-08-2002)“…Endothelins (ETs) are potent vasoconstrictors and have been implicated in the pathogenesis of various cardiovascular and renal diseases. In contrast, atrial…”
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Synthesis and biological activity of potent heterocyclic thiol-based inhibitors of endothelin-converting enzyme-1
Published in Bioorganic & medicinal chemistry letters (04-11-2002)“…Directed screening of metalloprotease inhibitors identified CGS 30084 ( 1) as a potent inhibitor of endothelin-converting enzyme-1 (ECE-1) in vitro (IC 50=77…”
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Effects of the ECE/NEP inhibitor CGS 34225 on the big ET-1-induced pressor response and plasma atrial natriuretic peptide concentration in conscious rats
Published in Clinical science (1979) (01-08-2002)“…CGS 34226 is a thiol-containing, potent dual inhibitor of endothelin converting enzyme-1 (ECE-1) and neutral endopeptidase 24.11 (NEP) with IC(50) values of 11…”
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Oral administration of an inhibitor of endothelin-converting enzyme attenuates cerebral vasospasm following experimental subarachnoid haemorrhage in rabbits
Published in Clinical science (1979) (01-08-2002)“…Increasing evidence has implicated endothelin-1 (ET-1), a potent vasoconstrictive peptide, in the pathophysiology of cerebral vasospasm after subarachnoid…”
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Expression, purification and characterization of the monomeric and dimeric forms of soluble bovine endothelin converting enzyme-1a
Published in Clinical science (1979) (01-08-2002)“…In this study, the catalytic domain of bovine endothelin converting enzyme-1a (ECE-1a) was cloned into a baculovirus transfer vector behind the human alkaline…”
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Activation of BK Ca channel via endothelin ET A receptors in porcine coronary artery smooth muscle cells
Published in European journal of pharmacology (1997)“…It has been demonstrated previously that endothelin-1 stimulates the Ca 2+-activated K + (BK Ca) channel activity in porcine coronary artery smooth muscle…”
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Design and Synthesis of a Potent and Selective Endothelin-Converting Enzyme Inhibitor, CGS 35066
Published in Journal of cardiovascular pharmacology (2000)“…CGS 26303 has previously been shown to inhibit human endothelin converting enzyme-1 (ECE-1) with an IC50 of 410 nM and to be efficacious in several animal…”
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Design and synthesis of potent thiol-based inhibitors of endothelin converting enzyme-1
Published in Bioorganic & medicinal chemistry letters (04-09-2000)“…Through directed screening of compounds prepared as metalloprotease inhibitors a compound, CGS 30084, that had potent endothelin converting enzyme-1 (ECE-1) in…”
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Cgs 34043: A non-peptidic, potent and long-acting dual inhibitor of endothelin converting enzyme-1 and neutral endopeptidase 24.11
Published in Life sciences (1973) (2000)“…Endothelin-1 (ET-1) is a potent vasoconstrictor. Its biosynthesis is catalyzed by endothelin converting enzyme (ECE). In contrast, atrial natriuretic peptide…”
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