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Proprotein convertase subtilisin/kexin type 2 (PCSK2) is a serine protease enzyme belonging to the proprotein convertase family. It is primarily expressed in neuroendocrine tissues and is responsible for proteolytically processing prohormones and neuropeptide precursors, such as the conversion of proglucagon to glucagon and proinsulin to insulin intermediates. PCSK2 activity is essential for the production of mature, bioactive peptide hormones involved in metabolic regulation and neuroendocrine signaling. The enzyme requires interaction with the regulatory protein 7B2 for proper activation. Genetic variants of PCSK2 are associated with altered glucose homeostasis and increased risk of metabolic disorders, including diabetes and obesity. Immunohistochemical detection of PCSK2 is clinically useful in determining the origin of certain neuroendocrine tumors, notably midgut, pulmonary, and adrenal neoplasms[1][2][3][5][7].
Drugs could theoretically modulate the enzymatic activity of PCSK2 to alter prohormone processing (e.g., by inhibition or enhancement of PCSK2's serine endopeptidase activity), but no clinically approved drugs specifically targeting PCSK2 are currently known[5][2].
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