Information on EC 2.7.11.30 - receptor protein serine/threonine kinase and Organism(s) Mus musculus

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The taxonomic range for the selected organisms is: Mus musculus

The enzyme appears in selected viruses and cellular organisms

EC NUMBER
COMMENTARY hide
2.7.11.30
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RECOMMENDED NAME
GeneOntology No.
receptor protein serine/threonine kinase
SYSTEMATIC NAME
IUBMB Comments
ATP:[receptor-protein] phosphotransferase
The transforming growth factor beta (TGF-beta) family of cytokines regulates cell proliferation, differentiation, recognition and death. Signalling occurs by the binding of ligand to the type II receptor, which is the constitutively active kinase. Bound TGF-beta is then recognized by receptor I, which is phosphorylated and can propagate the signal to downstream substrates [1,3].
CAS REGISTRY NUMBER
COMMENTARY hide
146702-86-5
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152060-53-2
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154907-75-2
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ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
-
association of ACVRL1 mutations with a vascular disease, familial pulmonary artery hypertension
physiological function
-
activin receptor-like-kinase 1 is a receptor for ligands of the transforming growth factor-beta family
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + Smad1
ADP + phosphorylated Smad1
show the reaction diagram
-
phosphorylation by ALK1
-
-
?
ATP + Smad2
ADP + phosphorylated Smad2
show the reaction diagram
ATP + Smad3
ADP + phosphorylated Smad3
show the reaction diagram
ATP + Smad5
ADP + phosphorylated Smad5
show the reaction diagram
-
phosphorylation by ALK1
-
-
?
additional information
?
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + Smad1
ADP + phosphorylated Smad1
show the reaction diagram
-
phosphorylation by ALK1
-
-
?
ATP + Smad2
ADP + phosphorylated Smad2
show the reaction diagram
ATP + Smad3
ADP + phosphorylated Smad3
show the reaction diagram
ATP + Smad5
ADP + phosphorylated Smad5
show the reaction diagram
-
phosphorylation by ALK1
-
-
?
additional information
?
-
COFACTOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Mg2+
-
-
Mn2+
-
-
INHIBITORS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
4(quinolin-4-yl)-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives
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IC50 of 0.00015-0.0051 mM, overview
4-phenyl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives
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IC50 of 0.00011-0.020 mM, overview
LY364947
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IC50 is 31 nM
additional information
-
ALK1 mediates inhibition of the ALK5/Smad2/3 pathway
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ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
ALK5
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is important for ALK1/TGF-beta signaling
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TGF-beta
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IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.00015 - 0.0051
4(quinolin-4-yl)-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives
Mus musculus;
-
IC50 of 0.00015-0.0051 mM, overview
0.00011 - 0.02
4-phenyl-substituted 5,6-dihydro-4H-pyrrolo[1,2-b]pyrazole derivatives
Mus musculus;
-
IC50 of 0.00011-0.020 mM, overview
0.000031
LY364947
Mus musculus;
-
IC50 is 31 nM
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
-
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
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assay at
7.5
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assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
22
-
assay at
30
-
assay at
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
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embryonic cells
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
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enbryonic fibroblast cell line
Manually annotated by BRENDA team
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fibroblast cell line
Manually annotated by BRENDA team
-
-
Manually annotated by BRENDA team
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
PDB
SCOP
CATH
UNIPROT
ORGANISM
Mus musculus;
Cloned/COMMENTARY
ORGANISM
UNIPROT
LITERATURE
expression of ALK1 and ALK5 in 293T cells, Hep-G2 cells, and in COS-7 cells using the adenovirus transfection system
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EXPRESSION
ORGANISM
UNIPROT
LITERATURE
in endoglin +/- mice, ACVRL1 is expressed in small regions of the distal arteries where endoglin is below detectable limits, co-expression of ACVRL1 and endoglin and associated pSmad1/5/8 signalling in the endothelial cells of distal arterioles
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ENGINEERING
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
-
knockdown of ALK5 expression in embryonic endothelial cells by antisense oligonucleotides results in inhibition of both TGF-beta-induced Smad 2 and Smad1/5 phosphorylation, an ALk5mutant defective in Smad activation rescues TGF-beta/ALK1-induced signaling in ALK5 null mutant endothelial cells