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Literature summary for 2.3.2.13 extracted from

  • Satpathy, M.; Shao, M.; Emerson, R.; Donner, D.B.; Matei, D.
    Tissue transglutaminase regulates matrix metalloproteinase-2 in ovarian cancer by modulating cAMP-response element-binding protein activity (2009), J. Biol. Chem., 284, 15390-15399.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
KCC009 dihydroisoxazole TG2 inhibitor Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-2780 cell
-
Homo sapiens
-
IGROV-1 cell
-
Homo sapiens
-
MDA-MB-436 cell
-
Homo sapiens
-
OV-90 cell
-
Homo sapiens
-
PC-3 cell
-
Homo sapiens
-
SKOV-3 cell
-
Homo sapiens
-

General Information

General Information Comment Organism
physiological function TG2 regulates the expression and function of matrix metalloproteinase MMP-2. TG2 knockdown down-regulates MMP-2 protein and mRNA expression in SKOV-3, IGROV-1, MDA-MB-436, and PC-3 cancer cells. TG2 knockdown or inhibition of TG2 activity using KCC009 decreases MMP-2 gelatinase activity in cancer cells. MMP-2 expression and function are regulated by TG2 at transcriptional level. Binding of CREB to the MMP-2 promoter is diminished in cells that express decreased TG2 levels. TG2 knockdown decreases CREB phosphorylation, and CREB knockdown decreases MMP-2 expression. The effect of TG2 on CREB activity and MMP-2 transcription is mediated by TG2-dependent degradation of protein phosphatase PP2A-alpha. PP2A-alpha complexes with and is targeted for degradation by TG2 Homo sapiens