Ruboxistaurin.
Ruboxistaurin is a potent and specific inhibitor of the beta isoform of protein kinase C. Overactivation of protein kinase C has been demonstrated in patients with type 2 diabetes, and is postulated to play a major role in the pathogenesis of diabetic microvascular complications, which include diabetic retinopathy, neuropathy and nephropathy. The role of protein kinase C in promoting tissue injury in patients with diabetes, and the pharmacologic and clinical studies illustrating the potential of ruboxistaurin to reduce the burden of diabetic microvascular complications will be discussed in this article.
Taulien
Christina A
CA
Department of Medicine, Duke University Medical Center, Durham, North Carolina 27705-0493, USA. joy00002@mc.duke.edu
Joy
Scott V
SV
D000818:Animals; D002986:Clinical Trials as Topic; D003928:Diabetic Nephropathies / Q000188:drug therapy*; D003929:Diabetic Neuropathies / Q000188:drug therapy*; D003930:Diabetic Retinopathy / Q000188:drug therapy*; D004791:Enzyme Inhibitors / Q000494:pharmacology / Q000627:therapeutic use; D006801:Humans; D007211:Indoles / Q000494:pharmacology / Q000627:therapeutic use; D008301:Maleimides / Q000494:pharmacology / Q000627:therapeutic use; D011493:Protein Kinase C / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D007211:Indoles; D008301:Maleimides; C099154:ruboxistaurin; D011493:Protein Kinase C