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Hypercholesterolemia: The role of PCSK9
Archives of Biochemistry and Biophysics, 2017Heart disease ends the life of more people than any other disease in the United States. High levels of low density lipoprotein (LDL)-cholesterol cause heart diseases by increasing the formation of atherosclerotic plaques. Proprotein convertase subtilisin/kexin-9 (PCSK9) indirectly regulates plasma LDL levels by controlling the LDL receptor expression ...
Quantil M. Melendez +3 more
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An oral antisense oligonucleotide for PCSK9 inhibition
Science Translational Medicine, 2021A highly potent, chemically modified PCSK9 antisense oligonucleotide formulated with a permeation enhancer was developed for oral administration. An oral ASO to lower LDL Strategies to decrease low-density lipoprotein (LDL) cholesterol could help treat ...
P. Gennemark +27 more
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Current Opinion in Lipidology, 2013
To summarize the therapeutic strategies to inhibit PCSK9 and to describe the main results obtained in phase I and II trials with monoclonal antibodies targeting PCSK9.Among the various approaches for PCSK9 inhibition, human data are only available for inhibition of PCSK9 binding to LDL receptor by monoclonal antibodies.
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To summarize the therapeutic strategies to inhibit PCSK9 and to describe the main results obtained in phase I and II trials with monoclonal antibodies targeting PCSK9.Among the various approaches for PCSK9 inhibition, human data are only available for inhibition of PCSK9 binding to LDL receptor by monoclonal antibodies.
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The role of PCSK9 in NAFLD/NASH and therapeutic implications of PCSK9 inhibition
Expert Review of Clinical Pharmacology, 2022There are inconsistent findings regarding the effect of lipid-lowering agents on nonalcoholic fatty liver disease (NAFLD). Proprotein Convertase Subtilisin/Kexin type 9 (PCSK9) is an important player in cholesterol homeostasis and intracellular lipogenesis, and PCSK9 inhibitors (PCSK9-i) have been found to be efficient for pharmacological management of
Amir Abbas Momtazi-Borojeni +3 more
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The promises of PCSK9 inhibition
Current Opinion in Lipidology, 2013In the past 10 years, the LDL receptor inhibitor proprotein convertase subtilisin kexin type 9 (PCSK9) has emerged as a validated target for lowering plasma LDL cholesterol levels. Here we review the most recent reports on PCSK9 out of a total of 500 publications published in print or online before March 2013 and indexed on PubMed.All published in 2012,
Florian Guilbaud +5 more
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Clinica Chimica Acta, 2015
Proprotein convertase subtilisin/kexin type 9 (PCSK9), a newly-recognized protein, plays a key role in regulating cholesterol homeostasis. PCSK9 reduces hepatic low-density lipoprotein receptors (LDLRs) thereby increasing LDL-cholesterol (LDL-C). Recently, biologic and genetic research proposed several approaches to inhibit or reduce PCSK9 to improve ...
Chuan-Jue Cui, Sha Li, Jian-Jun Li
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Proprotein convertase subtilisin/kexin type 9 (PCSK9), a newly-recognized protein, plays a key role in regulating cholesterol homeostasis. PCSK9 reduces hepatic low-density lipoprotein receptors (LDLRs) thereby increasing LDL-cholesterol (LDL-C). Recently, biologic and genetic research proposed several approaches to inhibit or reduce PCSK9 to improve ...
Chuan-Jue Cui, Sha Li, Jian-Jun Li
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The role of the C-terminal domain of PCSK9 and SEC24 isoforms in PCSK9 secretion
Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 2020Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a secretory protein that promotes low-density lipoprotein receptor (LDLR) degradation and thereby regulating plasma levels of LDL cholesterol. Previous studies have revealed the role of the C-terminal domain (CTD) of PCSK9 in its secretion, however, how CTD regulates PCSK9 secretion is not ...
Yishi Shen +5 more
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Herz, 2016 The 2 or 4‑week subcutaneous therapy with the recently approved antibodies alirocumab and evolocumab for inhibition of proprotein convertase subtilisin-kexin type 9 (PCSK9) reduces low-density lipoprotein cholesterol (LDL-C) in addition to statins and ezetimibe by 50-60 %. The therapy is well-tolerated.
Christian Werner +2 more
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Biochimica et Biophysica Acta (BBA) - Molecular and Cell Biology of Lipids, 2008
Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a critical role in cholesterol metabolism by controlling the levels of low density lipoprotein (LDL) particles that circulate in the bloodstream. Several gain-of-function and loss-of-function mutations in the PCSK9 gene, that occur naturally, have been identified and linked to ...
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Proprotein convertase subtilisin/kexin type 9 (PCSK9) plays a critical role in cholesterol metabolism by controlling the levels of low density lipoprotein (LDL) particles that circulate in the bloodstream. Several gain-of-function and loss-of-function mutations in the PCSK9 gene, that occur naturally, have been identified and linked to ...
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In vivo CRISPR base editing of PCSK9 durably lowers cholesterol in primates
Nature, 2021K. Musunuru +41 more
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