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Literature summary extracted from

  • Kulkarni, S.; Reddy, K.B.; Esteva, F.J.; Moore, H.C.; Budd, G.T.; Tubbs, R.R.
    Calpain regulates sensitivity to trastuzumab and survival in HER2-positive breast cancer (2010), Oncogene, 29, 1339-1350.
    View publication on PubMed

Application

EC Number Application Comment Organism
3.4.22.52 medicine calpain1 is a therapeutic target in HER2-positive breast cancer Homo sapiens

Protein Variants

EC Number Protein Variants Comment Organism
3.4.22.52 H272A catalytically inactive Homo sapiens

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.52 calpeptin
-
 Homo sapiens
3.4.22.52 MDL28170 potent inhibitor of the active site of calpain1 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
3.4.22.52 Homo sapiens
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
3.4.22.52 breast cancer cell
-
 Homo sapiens
-
3.4.22.52 BT-474 cell
-
 Homo sapiens
-
3.4.22.52 SK-BR-3 cell
-
 Homo sapiens
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
3.4.22.52 human epithelial growth factor receptor 2 + H2O overexpression of calpain1 or activation of endogenous calpain during adhesion or trastuzumab treatment of trastuzumab-sensitive cells induces cleavage of cytoplasmic domains of human epithelial growth factor receptor 2/phospho-human epithelial growth factor receptor 2 protein Homo sapiens 75000 Da fragment + 42000 Da fragment
-
 ?

Synonyms

EC Number Synonyms Comment Organism
3.4.22.52 calpain1
-
 Homo sapiens

General Information

EC Number General Information Comment Organism
3.4.22.52 physiological function calpain regulates trastuzumab sensitivity and survival, and the deregulation of the activation of calpain promotes trastuzumab resistance, trastuzumab-resistant cells require calpain activity for survival and activation of AKT1 Homo sapiens