Tags

Type your tag names separated by a space and hit enter

Ruboxistaurin, a protein kinase C beta inhibitor, as an emerging treatment for diabetes microvascular complications.
Ann Pharmacother. 2005 Oct; 39(10):1693-9.AP

Abstract

OBJECTIVE

To review current clinical data regarding the pharmacologic actions of ruboxistaurin (LY333531) mesylate, an inhibitor of protein kinase C (PKC) beta, and its role to potentially reduce the development and/or the progression of diabetic microvascular complications.

DATA SOURCES

Primary literature was obtained via a MEDLINE search (1966-August 2004) and through review of pertinent abstracts and presentations at major medical meetings.

STUDY SELECTION AND DATA EXTRACTION

Literature relevant to PKC physiology, the pharmacokinetics of ruboxistaurin, and data evaluating the use of ruboxistaurin in treating diabetic microvascular complications in human and relevant animal models was reviewed.

DATA SYNTHESIS

PKC is part of a group of intracellular signaling molecules activated in response to various specific hormonal, neuronal, and growth factor stimuli. Hyperglycemia leads to PKC beta 1 and 2 isoform activation, which experimentally has been shown to contribute to the development and progression of diabetic microvascular complications (retinopathy, nephropathy, neuropathy) through various biochemical mechanisms. Animal and/or human studies using ruboxistaurin mesylate, a novel, highly selective inhibitor of PKC beta, have shown delay in the progression and, in some cases, reversal of diabetic retinopathy, nephropathy, and neuropathy.

CONCLUSIONS

Ruboxistaurin mesylate, by inhibiting excessive activation of certain PKC isoforms, has the potential to reduce the burden of microvascular complications for patients with diabetes.

Authors+Show Affiliations

Department of Medicine, Duke University Medical Center, Durham, NC 27705-0493, USA.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article
Review

Language

eng

PubMed ID

16160002

Citation

Joy, Scott V., et al. "Ruboxistaurin, a Protein Kinase C Beta Inhibitor, as an Emerging Treatment for Diabetes Microvascular Complications." The Annals of Pharmacotherapy, vol. 39, no. 10, 2005, pp. 1693-9.
Joy SV, Scates AC, Bearelly S, et al. Ruboxistaurin, a protein kinase C beta inhibitor, as an emerging treatment for diabetes microvascular complications. Ann Pharmacother. 2005;39(10):1693-9.
Joy, S. V., Scates, A. C., Bearelly, S., Dar, M., Taulien, C. A., Goebel, J. A., & Cooney, M. J. (2005). Ruboxistaurin, a protein kinase C beta inhibitor, as an emerging treatment for diabetes microvascular complications. The Annals of Pharmacotherapy, 39(10), 1693-9.
Joy SV, et al. Ruboxistaurin, a Protein Kinase C Beta Inhibitor, as an Emerging Treatment for Diabetes Microvascular Complications. Ann Pharmacother. 2005;39(10):1693-9. PubMed PMID: 16160002.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Ruboxistaurin, a protein kinase C beta inhibitor, as an emerging treatment for diabetes microvascular complications. AU - Joy,Scott V, AU - Scates,Ann C, AU - Bearelly,Srilaxmi, AU - Dar,Moahad, AU - Taulien,Christina A, AU - Goebel,Jason A, AU - Cooney,Michael J, Y1 - 2005/09/13/ PY - 2005/9/15/pubmed PY - 2006/1/7/medline PY - 2005/9/15/entrez SP - 1693 EP - 9 JF - The Annals of pharmacotherapy JO - Ann Pharmacother VL - 39 IS - 10 N2 - OBJECTIVE: To review current clinical data regarding the pharmacologic actions of ruboxistaurin (LY333531) mesylate, an inhibitor of protein kinase C (PKC) beta, and its role to potentially reduce the development and/or the progression of diabetic microvascular complications. DATA SOURCES: Primary literature was obtained via a MEDLINE search (1966-August 2004) and through review of pertinent abstracts and presentations at major medical meetings. STUDY SELECTION AND DATA EXTRACTION: Literature relevant to PKC physiology, the pharmacokinetics of ruboxistaurin, and data evaluating the use of ruboxistaurin in treating diabetic microvascular complications in human and relevant animal models was reviewed. DATA SYNTHESIS: PKC is part of a group of intracellular signaling molecules activated in response to various specific hormonal, neuronal, and growth factor stimuli. Hyperglycemia leads to PKC beta 1 and 2 isoform activation, which experimentally has been shown to contribute to the development and progression of diabetic microvascular complications (retinopathy, nephropathy, neuropathy) through various biochemical mechanisms. Animal and/or human studies using ruboxistaurin mesylate, a novel, highly selective inhibitor of PKC beta, have shown delay in the progression and, in some cases, reversal of diabetic retinopathy, nephropathy, and neuropathy. CONCLUSIONS: Ruboxistaurin mesylate, by inhibiting excessive activation of certain PKC isoforms, has the potential to reduce the burden of microvascular complications for patients with diabetes. SN - 1060-0280 UR - https://www.unboundmedicine.com/medline/citation/16160002/Ruboxistaurin_a_protein_kinase_C_beta_inhibitor_as_an_emerging_treatment_for_diabetes_microvascular_complications_ L2 - http://journals.sagepub.com/doi/full/10.1345/aph.1E572?url_ver=Z39.88-2003&rfr_id=ori:rid:crossref.org&rfr_dat=cr_pub=pubmed DB - PRIME DP - Unbound Medicine ER -