נגישות
menu      
חיפוש מתקדם
תחביר
חפש...
הספר "אוצר וולקני"
אודות
תנאי שימוש
ניהול
קהילה:
אסיף מאגר המחקר החקלאי
פותח על ידי קלירמאש פתרונות בע"מ -
Protection of enkephalins from enzymatic degradation utilizing selective metal-chelating inhibitors
Year:
1983
Source of publication :
European Journal of Pharmacology
Authors :
אלטשטיין, מרים
;
.
Volume :
91
Co-Authors:
Altstein, M., Department of Neurobiology, The Weizmann Institute of Science, P.O.B. 26, Rehovot, 76100, Israel
Bachar, E., Department of Neurobiology, The Weizmann Institute of Science, P.O.B. 26, Rehovot, 76100, Israel
Vogel, Z., Department of Neurobiology, The Weizmann Institute of Science, P.O.B. 26, Rehovot, 76100, Israel
Blumberg, S., Department of Biophysics, The Weizmann Institute of Science, P.O.B. 26, Rehovot, 76100, Israel
Facilitators :
From page:
353
To page:
361
(
Total pages:
9
)
Abstract:
Metal ion-chelating agents inhibited enkephalin degradation by a rat striatal membrane-associated endopeptidase termed 'enkephalinase'. The combination of a hydrophobic dipeptidyl moiety and a transition metal-chelating moiety in the same molecule resulted in very efficient and selective inhibitors of enkephalinase. The mercaptoacetyl dipeptides (2-mercaptoacetyl-Leu-Phe and 2-mercaptoacetyl-Phe-Leu) and the N-phosphorylated dipeptides (phosphoryl-Leu-Phe and phosphoramidon) inhibited enkephalinase with IC50 values of 15, 70, 0.3 and 1 nM respectively, but were much less potent against the aminopeptidase and angiotensin converting enzyme, two other metalloenzymes implicated in the degradation of the enkephalins in brain. The inhibition of enkephalinase, using phosphoryl-Leu-Phe as a selective inhibitor, resulted in a 4 fold increase in the amount of enkephalin recovered following K+ depolarization of rat striatal slices. © 1983.
Note:
Related Files :
Animal
animal cell
dithiothreitol
mercaptoacetyldipeptide
mercaptoethanol
Metal-chelating reagents
phosphoramidon
synaptosome
עוד תגיות
תוכן קשור
More details
DOI :
10.1016/0014-2999(83)90158-9
Article number:
Affiliations:
Database:
סקופוס
Publication Type:
מאמר
;
.
Language:
אנגלית
Editors' remarks:
ID:
23695
Last updated date:
02/03/2022 17:27
Creation date:
17/04/2018 00:01
Scientific Publication
Protection of enkephalins from enzymatic degradation utilizing selective metal-chelating inhibitors
91
Altstein, M., Department of Neurobiology, The Weizmann Institute of Science, P.O.B. 26, Rehovot, 76100, Israel
Bachar, E., Department of Neurobiology, The Weizmann Institute of Science, P.O.B. 26, Rehovot, 76100, Israel
Vogel, Z., Department of Neurobiology, The Weizmann Institute of Science, P.O.B. 26, Rehovot, 76100, Israel
Blumberg, S., Department of Biophysics, The Weizmann Institute of Science, P.O.B. 26, Rehovot, 76100, Israel
Protection of enkephalins from enzymatic degradation utilizing selective metal-chelating inhibitors
Metal ion-chelating agents inhibited enkephalin degradation by a rat striatal membrane-associated endopeptidase termed 'enkephalinase'. The combination of a hydrophobic dipeptidyl moiety and a transition metal-chelating moiety in the same molecule resulted in very efficient and selective inhibitors of enkephalinase. The mercaptoacetyl dipeptides (2-mercaptoacetyl-Leu-Phe and 2-mercaptoacetyl-Phe-Leu) and the N-phosphorylated dipeptides (phosphoryl-Leu-Phe and phosphoramidon) inhibited enkephalinase with IC50 values of 15, 70, 0.3 and 1 nM respectively, but were much less potent against the aminopeptidase and angiotensin converting enzyme, two other metalloenzymes implicated in the degradation of the enkephalins in brain. The inhibition of enkephalinase, using phosphoryl-Leu-Phe as a selective inhibitor, resulted in a 4 fold increase in the amount of enkephalin recovered following K+ depolarization of rat striatal slices. © 1983.
Scientific Publication
You may also be interested in