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Crystal structure of PCSK9 (28]PCSK9 is a member of the peptidase S8 family. [27]: Family & Domains The solved structure of PCSK9 reveals four major components in the pre-processed protein: the signal peptide (residues 1-30); the N-terminal prodomain (residues 31–152); the catalytic domain (residues 153–425); and the C-terminal domain (residues 426–692), which is further divided into ...
VERVE-101 and VERVE-102 are an experimental gene therapy developed by Verve Therapeutics that targets the PCSK9 gene and is intended to reduce blood cholesterol levels. It works on the same protein as the cholesterol-lowering drugs known as PCSK9 inhibitors but, unlike them, is permanent. It works via base editing, a form of CRISPR gene editing.
Molar mass. 145 077.18 g·mol −1. Bococizumab (USAN; [1] development code RN316[2]) is a drug that was in development by Pfizer targeting PCSK9 to reduce LDL cholesterol. [3] Pfizer withdrew the drug from development in November 2016, determining that it was "not likely to provide value to patients, physicians or shareholders." [4]
PCSK9 inhibitors may be used for patients who have been unable to lower their cholesterol enough using statins. In this case, a PCSK9 inhibitor would be prescribed alongside a statin.
Evolocumab is a fully human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9). PCSK9 is a protein that targets LDL receptors for degradation; its inhibition thereby enhances the liver's ability to remove LDL-C, often colloquially referred to as "bad" cholesterol, from the blood. [7] [8]
PCSK9 inhibitors. A new category of drug candidates for treating high cholesterol by inhibiting the PCSK9 protein. First approval (by EU) mid 2015.
The proprotein convertase, PCSK9, is a liver-produced and -secreted serine protease whose binding and action on LDL receptors results in their increased lysosomal degradation in hepatocytes, a consequence of which is an increase in the level of circulating LDL cholesterol (and inhibition of which, the decrease in this level). [10]
Molar mass. 145 983.80 g·mol −1. Alirocumab, sold under the brand name Praluent, is a medication used as a second-line treatment for high cholesterol for adults whose cholesterol is not controlled by diet and statin treatment. It is a human monoclonal antibody that belongs to a novel class of anti-cholesterol drugs, known as PCSK9 inhibitors ...
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