Literature summary for 3.4.22.52 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

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

Engineering

Protein Variants Comment Organism
H272A catalytically inactive Homo sapiens

Inhibitors

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

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

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

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
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

Synonyms Comment Organism
calpain1
-
Homo sapiens

General Information

General Information Comment Organism
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