Introduction: PKC-βII 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-βII is difficult and yet to be achieved successfully.
Areas covered: This review discusses the studies carried out in various aspects of PKC-βII. The biological aspects, crystal structure data, structure–activity relationship study (SAR) and in silico studies related to PKC-βII such as homology modeling, molecular docking, molecular dynamics, quantitative structure–activity relationship (QSAR) studies and pharmacophore modeling etc. are summarized.
Expert opinion: PKC-βII 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-βII is valuable.