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Combined neutral endopeptidase inhibitors

Expert Opinion on Investigational Drugs, 2011
The renin-angiotensin-aldosterone system (RAAS) plays an important role in the pathophysiology of hypertension and heart failure. ACE inhibitors, angiotensin receptor II blockers (AT-II blockers) and aldosterone antagonists have been used to tackle the RAAS in the past but combined ACE and neutral endopeptidase (NEP) inhibitors have been shown to be ...
Cuculi, Florim, Erne, Paul
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Neutral endopeptidase and alcohol consumption, experiments in neutral endopeptidase-deficient mice

European Journal of Pharmacology, 2000
Alcohol consumption was investigated in mice which were rendered deficient in the peptide-degrading enzyme neutral endopeptidase (EC 3.4.24.11) (NEP-/-) by gene targeting and compared to alcohol consumption in corresponding wild type mice (NEP+/+). Mice were offered a free choice to drink tap water or 10% alcohol. The NEP-/- mice consumed significantly
W, Siems   +8 more
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Intracardiac expression of neutral endopeptidase

Molecular and Cellular Biochemistry, 2002
Neutral endopeptidase (NEP), a proteolytic enzyme, is known to degrade several peptides which control cardiovascular homeostasis. This is a preliminary study of the pattern of the intracardiac regional expression of the NEP gene in the normal heart, and the age-related changes in this expression in the cardiac regions.
V, Raizada   +3 more
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Neutral endopeptidase is a myristoylated protein

Molecular and Cellular Biochemistry, 2009
Neutral endopeptidase (NEP) is a cell-surface peptidase normally expressed by prostate epithelial cells and lost in ~50% of primary prostate cancers. NEP directly associates with multiple proteins at the cell surface including Ezrin/Radixin/Moesin (ERM) proteins and the PTEN tumor suppressor protein.
Rong, Zheng   +6 more
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Neutral Endopeptidase Inhibitors and Endothelin Antagonists

Cardiology Clinics, 2008
The current treatment paradigm for heart failure revolves around the central theory of neurohormonal antagonism. With the success of angiotensin-converting-enzyme inhibition, beta-blockade, and aldosterone antagonism in heart failure, alternative areas of the hormonal cascade have been targeted for potential benefits.
Srinivas, Iyengar, William T, Abraham
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Dicarboxylic Acid Dipeptide Neutral Endopeptidase Inhibitors

Journal of Medicinal Chemistry, 1995
The synthesis of three series of dicarboxylic acid dipeptide neutral endopeptidase 24.11 (NEP) inhibitors is described. In particular, the amino butyramide 21a exhibited potent NEP inhibitory activity (IC50 = 5.0 nM) in vitro and in vivo. Blood levels of 21a were determined using an ex vivo method by measuring plasma inhibitory activity in conscious ...
G M, Ksander   +7 more
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Neutral Endopeptidase Modulates Septic Shocka

Annals of the New York Academy of Sciences, 1996
Neutral endopeptidase (NEP; EC 3.4.24.11) is a type-2 cell-surface metalloproteinase known by a variety of eponyms, including enkephalinase, common acute lymphoblastic leukemia antigen (CALLA), and CD10. Identified substrates are largely neural or humoral oligopeptide agonists, and the enzyme functions to terminate signaling by degrading the ligand ...
B, Lu   +5 more
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Vasopeptidase Inhibitors, Neutral Endopeptidase Inhibitors, and Dual Inhibitors of Angiotensin-Converting Enzyme and Neutral Endopeptidase

Heart Disease, 2001
Vasopeptidase inhibitors represent a new class of cardiovascular drugs. They function as a combined angiotensin-converting enzyme (ACE) inhibitor and neutral endopeptidase (NEP) inhibitor, the latter of which potentiates the actions of atrial natriuretic peptide (ANP) by minimizing its degradation in the circulation.
J, Nawarskas, V, Rajan, W H, Frishman
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