Protein kinase C beta inhibitors: a new therapeutic target for diabetic nephropathy and vascular complications.

Abstract

Diabetic nephropathy (DN) has emerged as the major causative pathology in patients entering end-stage renal disease (ESRD) worldwide and it is responsible for 30-40% of all ESRD cases. Treatments for DN are centered on control of hyperglycemia and blood pressure control. However, current therapeutic regimens have not yet provided satisfactory prevention from the onset of DN. Protein kinase C (PKC) is an intracellular signaling molecule and activation of it plays an important role in the development of diabetic complications. In numerous experimental and clinical studies, inhibition of PKC (LY333531) has been shown to delay/halt the progression of diabetic complications. Presently, the drug is submitted in USA-FDA for new drug application in moderate to severe diabetic retinopathy. This review selectively discusses the role of PKC in DN and therapeutic effects produced by PKC inhibitors in DN. The role of PKC inhibitor in other diabetic complications is also discussed.

• Authors: S Budhiraja, J Singh
• Journal: Fundamental & clinical pharmacology (Fundam Clin Pharmacol) Vol. 22 Issue 3 Pg. 231-40 (Jun 2008) ISSN: 1472-8206 [Electronic] England
• PMID: 18485142 (Publication Type: Journal Article, Review)

Chemical References

• Isoenzymes
• Protein Kinase Inhibitors
• Protein Kinase C
• Protein Kinase C beta

Topics

• Animals
• Diabetic Nephropathies (drug therapy, enzymology)
• Diabetic Retinopathy (drug therapy, enzymology)
• Humans
• Hyperglycemia (drug therapy, enzymology)
• Isoenzymes (antagonists & inhibitors, metabolism)
• Protein Kinase C (antagonists & inhibitors, metabolism)
• Protein Kinase C beta
• Protein Kinase Inhibitors (pharmacology, therapeutic use)