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Biochem Biophys Res Commun ; 492(1): 103-108, 2017 10 07.
Artigo em Inglês | MEDLINE | ID: mdl-28802576

RESUMO

Statins are the first-line treatment for hypercholesterolemic patients. Herein, the effects of three statins on complex formation between proprotein convertase subtilisin-kexin 9 (PCSK9) and the low density lipoprotein receptor (LDLR), a critical step for the PCSK9-dependent degradation of LDLR in the lysosome, were examined. Human hepatocyte-like C3A cells grown in control (containing 10% fetal bovine serum) or MITO+ (supplemented with BD™ MITO + serum extender) medium were also treated with atorvastatin (Atorv), lovastatin (Lov), or pravastatin (Prav) for 24 h. RNA and protein expression studies and determinations of PCSK9/LDLR complex formation were performed. As expected, the statins increased the expression of PCSK9 and LDLR independently of the medium employed. Interestingly, Atov and Lov caused increases in PCSK9/LDLR complex formation, whereas Prav decreased complex formation when compared to cells treated without drugs. These results may explain why Prav works better for statin intolerant patients than other statins such as Atorv and Lov.


Assuntos
Atorvastatina/farmacologia , Lovastatina/farmacologia , Inibidores de PCSK9 , Pravastatina/farmacologia , Pró-Proteína Convertase 9/biossíntese , Receptores de LDL/antagonistas & inibidores , Receptores de LDL/biossíntese , Células Cultivadas , Humanos , Relação Estrutura-Atividade
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