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Peng, Y. Calpain Inhibitor. Encyclopedia. Available online: https://encyclopedia.pub/entry/61879 (accessed on 12 November 2026).
Peng Y. Calpain Inhibitor. Encyclopedia. Available at: https://encyclopedia.pub/entry/61879. Accessed November 12, 2026.
Peng, Yu. "Calpain Inhibitor" Encyclopedia, https://encyclopedia.pub/entry/61879 (accessed November 12, 2026).
Peng, Y. (2026, November 05). Calpain Inhibitor. In Encyclopedia. https://encyclopedia.pub/entry/61879
Peng, Yu. "Calpain Inhibitor." Encyclopedia. Web. 05 November, 2026.

Calpain Inhibitor

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A calpain inhibitor is a molecule that reduces the proteolytic activity of one or more members of the calpain family, particularly the calcium-activated cysteine proteases calpain-1 and calpain-2 [1]. Calpains cleave selected peptide bonds within cellular proteins, and their inhibition limits this processing rather than directly preventing protein synthesis [1][2]. Inhibitors include synthetic small molecules, peptide derivatives, and the endogenous regulatory protein calpastatin. Many small-molecule inhibitors interact with the catalytic cleft, where electrophilic groups can engage the active-site cysteine; individual compounds differ in reversibility and activity against other cysteine proteases [2]. Calpastatin uses a distinct recognition mechanism involving several contacts with calcium-activated calpain. Its inhibitory segment occupies the substrate-binding cleft while a loop passes around the catalytic cysteine, avoiding cleavage of the inhibitor itself [3][4]. Each of its four inhibitory repeats can engage a calpain molecule [4]. Inhibition therefore encompasses chemically diverse interactions that suppress substrate cleavage, with specificity varying among compounds and calpain isoforms [1][2].

calpain calpastatin cysteine protease proteolysis
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References

  1. Yasuko Ono; Takaomi C. Saido; Hiroyuki Sorimachi; Calpain research for drug discovery: challenges and potential. Nat. Rev. Drug Discov. 2016, 15, 854-876. [CrossRef]
  2. Darrel E. Goll; Valery F. Thompson; Hongqi Li; Wei Wei; Jinyang Cong; The Calpain System. Physiol. Rev. 2003, 83, 731-801. [CrossRef]
  3. Rachel A. Hanna; Robert L. Campbell; Peter L. Davies; Calcium-bound structure of calpain and its mechanism of inhibition by calpastatin. Nature 2008, 456, 409-412. [CrossRef]
  4. Tudor Moldoveanu; Kalle Gehring; Douglas R. Green; Concerted multi-pronged attack by calpastatin to occlude the catalytic cleft of heterodimeric calpains. Nature 2008, 456, 404-408. [CrossRef]
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Update Date: 05 Nov 2026
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