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Drug intelligence / Profile preview
Pep2-8 (PEP 2-8) is a synthetic 13-amino acid linear peptide that acts as a competitive inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9). Originally identified from phage-displayed peptide libraries by Genentech, Pep2-8 binds to PCSK9 with a KD of 0.7 μM, mimicking the EGF(A) domain of the low-density lipoprotein receptor (LDLR) and preventing PCSK9 from binding to LDLR. This inhibition restores LDLR surface levels and LDL particle uptake. In preclinical research, Pep2-8 has been investigated for its potential to protect kidneys from ischemia-reperfusion injury during hypothermic mechanical perfusion prior to transplantation, as well as for mitigating sepsis-induced endothelial dysfunction.
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