Application | Comment | Organism |
---|---|---|
pharmacology | enzyme inhibitor (1'R,5'S,6'S)-2-(3',5'-dibromo-1',6'-dihydroxy-4'-oxocyclohex-2'-enyl) acetonitrile is a potential therapeutic agent for fibrotic disease and cancer treatment | Homo sapiens |
Cloned (Comment) | Organism |
---|---|
gene ALK5, transient recombinant expression of FLAG-tagged enzyme mutant T202D in HEKT293 cells | Homo sapiens |
Protein Variants | Comment | Organism |
---|---|---|
T202D | site-directed mutagenesis | Homo sapiens |
Inhibitors | Comment | Organism | Structure |
---|---|---|---|
(1'R,5'S,6'S)-2-(3',5'-dibromo-1',6'-dihydroxy-4'-oxocyclohex-2'-enyl) acetonitrile | the small dibromotyrosine derivative purified from Pseudoceratina sp. suppresses TGF-beta responsiveness by inhibiting TGF-beta type I receptor serine/threonine kinase activity. The compound inhibits the TGF-beta-stimulated transcriptional activations of 3TP-Lux and decreases phosphorylated Smad2/3 levels and the nuclear translocation of Smad2/3 increased by TGF-beta. The compound inhibits TGF-beta-induced EMT and wound healing of A-549 cells and is a potential therapeutic agent for fibrotic disease and cancer treatment. The compound has no effects on TGF-beta receptor synthesis but attenuates TGF-beta-induced transcriptional activation in Mv1Lu cells and TGF-beta-induced expression of fibronectin and PAI-1 in A549 and NMuMG cells and TGF-beta-induced cell migration | Homo sapiens |
Metals/Ions | Comment | Organism | Structure |
---|---|---|---|
Mg2+ | required | Homo sapiens |
Natural Substrates | Organism | Comment (Nat. Sub.) | Natural Products | Comment (Nat. Pro.) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + Smad2 | Homo sapiens | - |
ADP + phosphorylated Smad2 | - |
? | |
ATP + Smad3 | Homo sapiens | - |
ADP + phosphorylated Smad3 | - |
? |
Organism | UniProt | Comment | Textmining |
---|---|---|---|
Homo sapiens | P36897 | - |
- |
Source Tissue | Comment | Organism | Textmining |
---|---|---|---|
A-549 cell | - |
Homo sapiens | - |
epithelial cell | - |
Homo sapiens | - |
Mv1Lu cell | - |
Homo sapiens | - |
Substrates | Comment Substrates | Organism | Products | Comment (Products) | Rev. | Reac. |
---|---|---|---|---|---|---|
ATP + Smad2 | - |
Homo sapiens | ADP + phosphorylated Smad2 | - |
? | |
ATP + Smad3 | - |
Homo sapiens | ADP + phosphorylated Smad3 | - |
? |
Synonyms | Comment | Organism |
---|---|---|
activin receptor-like kinase 5 | - |
Homo sapiens |
ALK5 | - |
Homo sapiens |
ALK5 | gene and protein name | Homo sapiens |
TGF-beta type I receptor serine/threonine kinase | - |
Homo sapiens |
TGFBR1 | - |
Homo sapiens |
Cofactor | Comment | Organism | Structure |
---|---|---|---|
ATP | - |
Homo sapiens |
Organism | Comment | Expression |
---|---|---|
Homo sapiens | (1'R,5'S,6'S)-2-(3',5'-dibromo-1',6'-dihydroxy-4'-oxocyclohex-2'-enyl) acetonitrile has no effects on TGF-beta receptor synthesis | additional information |