Proprotein convertase subtilisin/kexin type 9 (PCSK9) binds to low density lipoprotein receptor (LDLR) through the LDLR epidermal growth factor-like repeat A (EGF-A) domain and induces receptor internalization and degradation. PCSK9 has emerged as a novel therapeutic target for hypercholesterolemia. Clinical studies with PCSK9 inhibiting antibodies have demonstrated strong LDL-c lowering effects, but other therapeutic approaches using small molecule inhibitors for targeting PCSK9 functions may offer supplementary therapeutic options. The aim of our study was to evaluate the effect of synthetic EGF-A analogs on mutated (D374Y) PCSK9-D374Y mediated LDLR degradation in vitro.
Scrimali, C., Spina, R., Ingrassia, V., Brucato, F., Altieri, G., Noto, D., et al. (2020). PCSK9-D374Y MEDIATED LDL-R DEGRADATION CAN BE FUNCTIONALLY INHIBITED BY EGF-A AND TRUNCATED EGF-A PEPTIDES. AN IN VITRO STUDY. ATHEROSCLEROSIS, 315, 258-258.
PCSK9-D374Y MEDIATED LDL-R DEGRADATION CAN BE FUNCTIONALLY INHIBITED BY EGF-A AND TRUNCATED EGF-A PEPTIDES. AN IN VITRO STUDY
Scrimali, C;Spina, R;Ingrassia, V;Brucato, F;Altieri, GI;Noto, D;Misiano, G;Giammanco, A;Fayer, F;Barbagallo, CM;Ganci, A;Cefalu, AB;Averna, M
2020-01-01
Abstract
Proprotein convertase subtilisin/kexin type 9 (PCSK9) binds to low density lipoprotein receptor (LDLR) through the LDLR epidermal growth factor-like repeat A (EGF-A) domain and induces receptor internalization and degradation. PCSK9 has emerged as a novel therapeutic target for hypercholesterolemia. Clinical studies with PCSK9 inhibiting antibodies have demonstrated strong LDL-c lowering effects, but other therapeutic approaches using small molecule inhibitors for targeting PCSK9 functions may offer supplementary therapeutic options. The aim of our study was to evaluate the effect of synthetic EGF-A analogs on mutated (D374Y) PCSK9-D374Y mediated LDLR degradation in vitro.
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