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Literature summary for 2.7.11.30 extracted from

  • Chen, C.L.; Kao, Y.C.; Yang, P.H.; Sung, P.J.; Wen, Z.H.; Chen, J.J.; Huang, Y.B.; Chen, P.Y.
    A small dibromotyrosine derivative purified from Pseudoceratina sp. suppresses TGF-beta responsiveness by inhibiting TGF-beta type I receptor serine/threonine kinase activity (2016), J. Cell. Biochem., 117, 2800-2814.
    View publication on PubMed

Application

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(Commentary)

Cloned (Comment) Organism
gene ALK5, transient recombinant expression of FLAG-tagged enzyme mutant T202D in HEKT293 cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
T202D site-directed mutagenesis Homo sapiens

Inhibitors

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

Metals/Ions Comment Organism Structure
Mg2+ required Homo sapiens

Natural Substrates/ Products (Substrates)

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

Organism UniProt Comment Textmining
Homo sapiens P36897
-
-

Source Tissue

Source Tissue Comment Organism Textmining
A-549 cell
-
Homo sapiens
-
epithelial cell
-
Homo sapiens
-
Mv1Lu cell
-
Homo sapiens
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + Smad2
-
Homo sapiens ADP + phosphorylated Smad2
-
?
ATP + Smad3
-
Homo sapiens ADP + phosphorylated Smad3
-
?

Synonyms

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

Cofactor Comment Organism Structure
ATP
-
Homo sapiens

Expression

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