Calpain-1 catalytic subunit (CANP1 (or CAPN1))

Calpain-1 catalytic subunit is the large, catalytic unit of the calcium-activated, nonlysosomal cysteine protease calpain-1, encoded by the CAPN1 gene in humans[1][5]. It forms a heterodimer with a regulatory subunit (CAPNS1), and this complex performs regulated, limited proteolysis of target proteins involved in cytoskeletal remodeling, cell migration, apoptosis, and intracellular signal transduction[1][5][8]. Activation occurs in response to increased intracellular calcium levels, and its dysregulation is associated with pathological processes including cancer progression, metastasis, neurodegenerative disorders, cardiac injury, and inflammatory responses[2][3][7][8]. Despite its potential as a therapeutic target, no specific calpain-1 inhibitor is clinically approved, mainly due to the enzyme’s broad physiological roles and challenges in developing selective inhibitors[3][4][5].

Other names

CANP1CAPN1muCANPCell proliferation-inducing gene 30 proteinMicromolar-calpain

Inhibition of calpain-1 catalytic activity (active site inhibition or allosteric inhibition blocking dimerization and calcium activation), modulation of downstream proteolytic pathways