Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a genetically validated target for hypercholesterolemia. PCSK9 binds to the low-density lipoprotein receptor (LDLR) and facilitates its lysosomal degradation reducing cell surface LDLR levels thereby increasing circulating levels of low-density lipoprotein cholesterol (LDL-C).There are two approved human monoclonal antibodies that bind to PCSK9 and inhibit interaction with the LDLR. Both of these antibodies bind to the epitope of PCSK9 that is adjacent to the region required for LDLR interaction. The current presentation will describe both peptidic and fragment-derived small molecule approaches that are designed to inhibit the interaction of PCSK9 with LDLR.

Small molecule and peptidic ligands as PCSK9-LDLR inhibitors

254th National Meeting (2017)

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