The DOI matches its Crossref record.
Amelioration of Vascular Dysfunctions in Diabetic Rats by an Oral PKC β Inhibitor
Abstract
The vascular complications of diabetes mellitus have been correlated with enhanced activation of protein kinase C (PKC). LY333531, a specific inhibitor of the β isoform of PKC, was synthesized and was shown to be a competitive reversible inhibitor of PKC β 1 and β 2 , with a half-maximal inhibitory constant of ∼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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Citations
Cited by
Biochemistry and molecular cell biology of diabetic complications
Brownlee, M. (2001) · Nature · doi:10.1038/414813a · Cited by 9,107
The Pathobiology of Diabetic Complications
Brownlee, M. (2005) · Diabetes · doi:10.2337/diabetes.54.6.1615 · Cited by 5,339
Normalizing mitochondrial superoxide production blocks three pathways of hyperglycaemic damage
Nishikawa, T., Edelstein, D., Du, X. L., Yamagishi, S.-I., Matsumura, T., Kaneda, Y., Yorek, M. A., Beebe, D., Oates, P. J., Hammes, H.-P., et al. (2000) · Nature · doi:10.1038/35008121 · Cited by 4,277
Mechanisms of Diabetic Complications
Forbes, J. M., & Cooper, M. E. (2013) · Physiological Reviews · doi:10.1152/physrev.00045.2011 · Cited by 2,890
Oxidative Stress and Stress-Activated Signaling Pathways: A Unifying Hypothesis of Type 2 Diabetes
Evans, J. L., Goldfine, I. D., Maddux, B. A., & Grodsky, G. M. (2002) · Endocrine Reviews · doi:10.1210/er.2001-0039 · Cited by 2,232
Metadata
- Authors
- Ishii, H., Jirousek, M. R., Koya, D., Takagi, C., Xia, P., Clermont, A., Bursell, S.-E., Kern, T. S., Ballas, L. M., Heath, W. F., Stramm, L. E., Feener, E. P., & King, G. L.
- Venue
- Science
- Published
- 1996-05-03
- Volume
- 272
- Issue
- 5262
- Pages
- 728-731
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W1966419887
- Cited by
- 1,103
- References
- 0
- FWCI
- 56.36
- Type
- journal article
- Language
- en
- Open access
- closed
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- Ishii, H., Jirousek, M. R., Koya, D., Takagi, C., Xia, P., Clermont, A., Bursell, S.-E., Kern, T. S., Ballas, L. M., Heath, W. F., Stramm, L. E., Feener, E. P., & King, G. L. (1996). Amelioration of Vascular Dysfunctions in Diabetic Rats by an Oral PKC β Inhibitor. Science. https://doi.org/10.1126/science.272.5262.728
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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).
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