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27 April 2024 |
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Amelioration of vascular dysfunctions in diabetic rats by an oral PKC beta inhibitor | | H Ishii
; M R Jirousek
; D Koya
; C Takagi
; P Xia
; A Clermont
; S E Bursell
; T S Kern
; L M Ballas
; W F Heath
; L E Stramm
; E P Feener
; G L King
; | | Date: |
3 May 1996 | | Journal: | Science, 272 (5262), 728-31 | | 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. | | Source: | PubMed, pmid8614835 | | Services: | Forum | Review | Favorites | |
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