Optimization of 4-Amino-2-Pyridone Inhibitors of Proprotein Convertase Subtilisin/Kexin Type 9: Integrating Structure-Activity and Structure-Metabolism Relationships. [PDF]
ChemMedChemGreen chemistry‐based late‐stage functionalization (LSF) of the anti‐proprotein convertase subtilisin/kexin type 9 (PCSK9) early lead compound 5c led to optimized analogs with improved metabolic stability/PCSK9 IC50 ratio. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a key drug target for the treatment of different hypercholesterolemia ...
Giannessi L +12 more
europepmc +2 more sources
Internalized PCSK9 dissociates from recycling LDL receptors in PCSK9-resistant SV-589 fibroblasts
Journal of Lipid Research, 2014 Secreted PCSK9 binds to cell surface LDL receptor (LDLR) and directs the receptor for lysosomal degradation. PCSK9 is potent at inducing LDLR degradation in cultured liver-derived cells, but it is considerably less active in immortalized fibroblasts.
My-Anh Nguyen +2 more
doaj +1 more source
Polymorphic Variant rs11206510 in PCSK9 and Risk of Coronary Artery Disease in Bulgarians
Acta Medica Bulgarica, 2023 The aim of this study was to investigate the potential association of rs11206510 in PCSK9 gene with coronary artery disease (CAD) and myocardial infarction (MI) in Bulgarians.
Tzveova R. +7 more
doaj +1 more source
Frontiers in Medicine, 2022 BackgroundProprotein convertase subtilisin/kexin type 9 (PCSK9) is a serine protease that is a mediator of the immune response to sepsis. PCSK9 is also highly expressed in pneumocytes and pulmonary endothelial cells.
Thomas S. Metkus +5 more
doaj +1 more source
Renal Failure, 2020 Background Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a major post-transcriptional regulator of low-density lipoprotein receptor degradation. Recently, PCSK9 was shown to be overexpressed by liver cells in rats with proteinuria.
Huaying Shen +5 more
doaj +1 more source
SEC24A deficiency lowers plasma cholesterol through reduced PCSK9 secretion. [PDF]
, 2013 The secretory pathway of eukaryotic cells packages cargo proteins into COPII-coated vesicles for transport from the endoplasmic reticulum (ER) to the Golgi.
Adams, Elizabeth +17 more
core +1 more source
Proteolytic cleavage of antigen extends the durability of an anti-PCSK9 monoclonal antibody[S]
Journal of Lipid Research, 2015 Lilly PCSK9 antibody LY3015014 (LY) is a monoclonal antibody (mAb) that neutralizes proprotein convertase subtilisin-kexin type 9 (PCSK9). LY decreases LDL cholesterol in monkeys and, unlike other PCSK9 mAbs, does not cause an accumulation of intact ...
Krista M. Schroeder +7 more
doaj +1 more source
Unpacking and understanding the impact of proprotein convertase subtilisin/kexin type 9 inhibitors on apolipoprotein B metabolism [PDF]
, 2017 No abstract ...
Packard, Chris J.
core +1 more source
Research Models for Studying Vascular Calcification [PDF]
, 2020 Calcification of the vessel wall contributes to high cardiovascular morbidity and mortality. Vascular calcification (VC) is a systemic disease with multifaceted contributing and inhibiting factors in an actively regulated process.
Babic, Milen +4 more
core +1 more source
Effect of a novel nutraceutical combination on serum lipoprotein functional profile and circulating PCSK9 [PDF]
, 2017 BACKGROUND: A beneficial effect on cardiovascular risk may be obtained by improving lipid-related serum lipoprotein functions such as high-density lipoproteins (HDLs) cholesterol efflux capacity (CEC) and serum cholesterol loading capacity (CLC) and by ...
Adorni, Maria Pia +7 more
core +3 more sources