Proprotein convertase subtilisin/kexin type 9: A new target molecule for gene therapy |
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Authors: | Anna Banaszewska Michal Piechota Robert Plewa |
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Institution: | Department of Animal Physiology and Development, Adam Mickiewicz University, 89 Umultowska St., 61-614, Poznan, Poland. |
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Abstract: | Proprotein convertase subtilisin/kexin type 9 (PCSK9) has emerged as a novel target for controlling plasma levels of low-density
lipoprotein cholesterol (LDL-C) and decreasing the risk of cardiovascular diseases. At present it is clear that the major
classes of commonly prescribed lipid-lowering medications increase serum PCSK9 levels and fail to protect a significant percentage
of patients from cardiovascular events. Therefore development of new LDL-C lowering medications that either do not increase
circulating PCSK9 levels or work through inhibition of PCSK9 expression and protease activity is a highly desirable approach
to overcome hypercholesterolemia. Since there are several agents which are being evaluated in human preclinical and clinical
trials, this review summarizes current therapeutic strategies targeting PCSK9, including specific antibodies, antisense oligonucleotides,
small interfering RNAs (siRNAs) and other small-molecule inhibitors. |
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