Literature DB >> 3899113

Binding of the bidentate inhibitor [3H]HACBO-Gly to the rat brain neutral endopeptidase "enkephalinase".

G Waksman, R Bouboutou, J Devin, R Besselievre, M C Fournie-Zaluski, B P Roques.   

Abstract

The synthesis and binding properties to rat brain tissue of the enkephalinase inhibitor [3H] N-[(R,S)-3-hydroxyaminocarbonyl-2-benzyl-1-oxopropyl]-glycine ([3H]HACBO-Gly, 45 Ci/mmole) is reported. [3H]HACBO-Gly binding to membranes from various rat brain tissue is saturable (KD = 0.4 +/- 0.05 nM) and linearly related to the amount of tissue. Non specific binding is less than 15% of total binding at the KD concentration. The regional distribution of [3H]HACBO-Gly binding and enkephalinase activity are closely correlated with highest levels in striatum and substantia nigra. The efficiency of inhibitors of various peptidases (thiorphan, captopril, bestatin ...) to inhibit [3H]HACBO-Gly binding or enkephalinase activity are similar. These results indicate that [3H]HACBO-Gly binds selectively to enkephalinase. This compound should help to clarify the localization of the enzyme in the CNS.

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Year:  1985        PMID： 3899113     DOI： 10.1016/0006-291x(85)91797-8

Source DB:  PubMed          Journal:  Biochem Biophys Res Commun        ISSN： 0006-291X            Impact factor:   3.575


  8 in total

1.  Autoradiographic comparison of the distribution of the neutral endopeptidase "enkephalinase" and of mu and delta opioid receptors in rat brain.

Authors:  G Waksman; E Hamel; M C Fournié-Zaluski; B P Roques
Journal:  Proc Natl Acad Sci U S A       Date:  1986-03       Impact factor: 11.205

2.  Pre- and post-natal ontogeny of neutral endopeptidase 24-11 ('enkephalinase') studied by in vitro autoradiography in the rat.

Authors:  I Dutriez; N Salès; M C Fournié-Zaluski; B P Roques
Journal:  Experientia       Date:  1992-03-15

3.  Dual inhibition of angiotensin-converting enzyme and neutral endopeptidase by the orally active inhibitor mixanpril: a potential therapeutic approach in hypertension.

Authors:  M C Fournié-Zaluski; W Gonzalez; S Turcaud; I Pham; B P Roques; J B Michel
Journal:  Proc Natl Acad Sci U S A       Date:  1994-04-26       Impact factor: 11.205

4.  Development of [125I]RB104, a potent inhibitor of neutral endopeptidase 24.11, and its use in detecting nanogram quantities of the enzyme by "inhibitor gel electrophoresis".

Authors:  M C Fournié-Zaluski; J M Soleilhac; S Turcaud; R Laï-Kuen; P Crine; A Beaumont; B P Roques
Journal:  Proc Natl Acad Sci U S A       Date:  1992-07-15       Impact factor: 11.205

5.  Identification and characterization of a neutral endopeptidase activity in Aplysia californica.

Authors:  W Bawab; R S Aloyz; P Crine; B P Roques; L DesGroseillers
Journal:  Biochem J       Date:  1993-12-01       Impact factor: 3.857

6.  Identification and characterization of aminopeptidases from Aplysia californica.

Authors:  W Bawab; E Querido; P Crine; L DesGroseillers
Journal:  Biochem J       Date:  1992-09-15       Impact factor: 3.857

7.  Cloning and expression in Bacillus subtilis of the npr gene from Bacillus thermoproteolyticus Rokko coding for the thermostable metalloprotease thermolysin.

Authors:  M J O'Donohue; B P Roques; A Beaumont
Journal:  Biochem J       Date:  1994-06-01       Impact factor: 3.857

8.  Neuronal localization of the neutral endopeptidase 'enkephalinase' in rat brain revealed by lesions and autoradiography.

Authors:  G Waksman; E Hamel; P Delay-Goyet; B P Roques
Journal:  EMBO J       Date:  1986-12-01       Impact factor: 11.598
  8 in total

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