Inhibitors | Comment | Organism | Structure |
---|---|---|---|
KCC009 | dihydroisoxazole TG2 inhibitor | Homo sapiens |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | - |
- |
- |
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 | 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 |