Joshua Lee

Correction to “Discovery Process of Enlicitide, a Highly Engineered Macrocyclic Peptide Therapeutic, Through Issue Driven Fragment-Based Synthetic Assembly and SAR”

Hubert Josien, Anilkumar G. Nair, Fa‐Xiang Ding, Yan Guo et autres

Discovery Process of Enlicitide, a Highly Engineered Macrocyclic Peptide Therapeutic, through Issue-Driven Fragment-Based Synthetic Assembly and SAR

Hubert Josien, Anilkumar G. Nair, Fa‐Xiang Ding, Yan Guo et autres

Abstract Herein, we report the discovery process of enlicitide (MK-0616, compound 18), an orally active macrocyclic peptide therapeutic against PCSK9 for LDL-C reduction. To overcome development bottlenecks in a prior lead (compound 1a) in a timely manner (sulfur oxidation liability, low solubility, …

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Biocatalytic cascades enable manufacture of the macrocyclic peptide enlicitide

Artis Klapars, Anna Fryszkowska, Stephanie Galanie, Omer Ad et autres

Historically, many compelling therapeutic targets have been accessible only by injectable biologic drugs. Macrocyclic peptides, such as the proprotein convertase subtilisin/kexin type 9 inhibitor enlicitide for the treatment of atherosclerotic cardiovascular disease, are beginning to unlock these targets to orally administered therapies …

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