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[摘要]：Introduction: PKC-beta II is a conventional isoform of PKC. It is overexpressed in hyperglycemic conditions and is known to trigger various diabetic complications, mainly cardiovascular complications and to a certain extent nephropathy, neuropathy, retinopathy etc. Selective inhibition of this enzyme will be one of the favorable approaches to treat diabetes-mellitus-related complications. Due to high sequence similarities among PKC isoforms, selective inhibition of PKC-beta II is difficult and yet to be achieved successfully. Areas covered: This review discusses the studies carried out in various aspects of PKC-beta II. The biological aspects, crystal structure data, structure-activity relationship study (SAR) and in silico studies related to PKC-beta II such as homology modeling, molecular docking, molecular dynamics, quantitative structure-activity relationship (QSAR) studies and pharmacophore modeling etc. are summarized. Expert opinion: PKC-beta II is a potential target for treating diabetes-related complications. Selective inhibitors of this enzyme are under clinical trials but to date, success has not been achieved. Thus, extensive research is essential in this direction; the contribution of in silico tools in designing and optimizing selective inhibitors of PKC-beta II is valuable. |
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