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Drug intelligence / Profile preview
calpeptin
- Development stage
- Preclinical
- Modality
- Small Molecules
- Administration
- Intraparenchymal, In Vitro
01
Overview
Calpeptin is a potent, cell-permeable inhibitor of calpains, specifically targeting calpain 1 (μ-calpain) and calpain 2 (m-calpain). While primarily characterized as a cysteine protease inhibitor, it is widely utilized in cell biology research as an indirect activator of the RhoA/ROCK signaling pathway. This activation occurs because calpeptin inhibits the calpain-mediated cleavage of proteins that regulate RhoA, thereby promoting RhoA activity and its downstream effector, Rho-associated protein kinase (ROCK). Research has demonstrated that calpeptin-induced ROCK activity can regulate the Hippo signaling pathway by increasing the nuclear localization of Yap and the expression of Yap-regulated genes. It has been investigated in preclinical models for its role in mitigating radiation-induced salivary gland dysfunction (hyposalivation) and other conditions involving cytoskeletal remodeling and cellular polarity.
- Other names
- Benzyloxycarbonyl-L-leucyl-L-norleucinalCbz-Leu-nLe-CHO
02
Targets
CAPN (Schistosoma calpain large subunit family)CTSL (Cathepsin L)ROCK1 (Rho-associated coiled-coil containing protein kinase 1)Mpro (3C-like proteinase of SARS-CoV-2)
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