Amelioration of vascular dysfunctions in diabetic rats by an oral PKC beta inhibitor.
Science
; 272(5262): 728-31, 1996 May 03.
Article
in En
| MEDLINE
| ID: mdl-8614835
ABSTRACT
The vascular complications of diabetes mellitus have been correlated with enhanced activation of protein kinase C (PKC). LY333531, a specific inhibitor of the beta isoform of PKC, was synthesized and was shown to be a competitive reversible inhibitor of PKC beta 1 and beta 2, with a half-maximal inhibitory constant of approximately 5 nM; this value was one-fiftieth of that for other PKC isoenzymes and one-thousandth of that for non-PKC kinases. When administered orally, LY333531 ameliorated the glomerular filtration rate, albumin excretion rate, and retinal circulation in diabetic rats in a dose-responsive manner, in parallel with its inhibition of PKC activities.
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Collection:
01-internacional
Database:
MEDLINE
Main subject:
Protein Kinase C
/
Diabetes Mellitus, Experimental
/
Diabetic Angiopathies
/
Enzyme Inhibitors
/
Indoles
/
Isoenzymes
/
Maleimides
Type of study:
Etiology_studies
Language:
En
Journal:
Science
Year:
1996
Document type:
Article