PMID: 7529108Sep 1, 1994Paper

Generation by the phosphoramidon-sensitive peptidases, endopeptidase-24.11 and thermolysin, of endothelin-1 and c-terminal fragment from big endothelin-1

British Journal of Pharmacology
L J MurphyA J Turner

Abstract

1. Phosphoramidon, a potent inhibitor of endopeptidase-24.11 (E-24.11) and thermolysin, has been shown to reduce the hypertensive effect of exogenous big endothelin-1 (big ET-1) in rats. To examine whether E-24.11 or thermolysin convert big ET-1 to endothelin-1 (ET-1) and C-terminal fragment (CTF), the effects on porcine and human big ET-1 of each of the purified enzymes were compared in vitro. 2. For E-24.11, the relative rates of hydrolysis were ET-1 > CTF > big ET-1. The relative half-lives for hydrolysis of 3 nmol of each peptide by 200 ng enzyme were: big ET-1 > 24 h; ET-1, 37 min; CTF, 57 min. For comparison, the half-life for hydrolysis of substance P under similar conditions was 2.1 min. 3. For thermolysin the relative rates of hydrolysis were found to be big ET-1 > CTF > ET-1. The relative half-lives for hydrolysis of 3 nmol peptide by 50 ng enzyme were: big ET-1, 25 min; ET-1, 56 min; CTF, 47 min. 4. Because the low rate of conversion of big ET-1 to ET-1 by E-24.11 did not yield sufficient ET-1 for h.p.l.c. quantification a RIA specific for ET-1(16-21) was used to study further the hydrolysis of big ET-1 by E-24.11. Incubation of big ET-1 (0.2-2 nmol) with E-24.11 (4-400 ng) generated ET-1 levels of between 1.7 and 33...Continue Reading

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Citations

Feb 27, 2001·BioEssays : News and Reviews in Molecular, Cellular and Developmental Biology·A J TurnerD Coates
Jan 19, 2013·Pflügers Archiv : European journal of physiology·Sanjaya KuruppuA Ian Smith
Jan 16, 2002·Current Hypertension Reports·Thomas QuaschningThomas F Lüscher
Jan 1, 1995·British Journal of Pharmacology·J C Yu, A P Davenport
Feb 18, 2011·Expert Opinion on Investigational Drugs·Florim Cuculi, Paul Erne
Sep 13, 2014·International Journal of Cardiology·Massimo Volpe
Jan 26, 2013·The Journal of Sexual Medicine·Harrina E RahardjoMarkus A Kuczyk
Jun 21, 2011·European Journal of Cell Biology·Heiko MeyerAchim Paululat
May 18, 2004·Journal of Clinical Pharmacology·Marc PfisterJeffrey S Barrett
Dec 18, 2003·British Journal of Clinical Pharmacology·Matthew I WorthleyStephen G Worthley
Jan 26, 1996·Biochemical Pharmacology·A J Turner, L J Murphy
May 20, 2014·Pharmacology & Therapeutics·Thomas G von LuederHenry Krum
Aug 6, 2016·Journal of the American College of Cardiology·Antoni Bayes-GenisA Mark Richards
Jun 11, 1999·Japanese Journal of Pharmacology·A DendorferP Dominiak
Sep 30, 1996·FEBS Letters·H PetoB A Wallace
Jun 8, 2001·Journal of Cardiovascular Pharmacology·F EnseleitT F Lüscher
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Mar 27, 1998·Biochemical Pharmacology·F D RussellA P Davenport
Oct 25, 2001·Journal of the American Society of Nephrology : JASN·Thomas QuaschningThomas F Lüscher

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