Approach

Rationale

The discovery of the proprotein convertase subtilisin-kexin 9 (PCSK9) in 2003, and its subsequent rapid emergence as a therapeutic target, is today transforming the treatment of cardiovascular disease.  Just as the introduction of ‘statins’ in the 1980’s has significantly reduced mortality ...

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Biology

Like other proprotein convertases (PCs), PCSK9 undergoes an autocatalytic cleavage of its inhibitory prodomain in the endoplasmic reticulum (ER).  This results in a heterodimer of the prosegment and the rest of the mature protein, that is proteolytically inactive and allows the protein ...

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