Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.11.30 extracted from

  • Long, L.; Crosby, A.; Yang, X.; Southwood, M.; Upton, P.D.; Kim, D.K.; Morrell, N.W.
    Altered bone morphogenetic protein and transforming growth factor-beta signaling in rat models of pulmonary hypertension: potential for activin receptor-like kinase-5 inhibition in prevention and progression of disease (2009), Circulation, 119, 566-576.
    View publication on PubMed
Search for more literature for 2.7.11.30

Application

Application Comment Organism
medicine potential for activin receptor-like kinase-5 inhibition in prevention and progression of disease, inhibition of activin receptor-like kinase-5 signaling in vivo with the selective small-molecule inhibitor IN-1233 prevented pulmonary arterial hypertension, right ventricular hypertrophy, and vascular remodeling after monocrotaline injection and inhibited the progression of established pulmonary arterial hypertension in this model Rattus norvegicus

Inhibitors

Inhibitors Comment Organism Structure
3-((4-(6-methylpyridin-2-yl)-5-(quinolin-6-yl)-1H-imidazol-2-yl)methyl)benzamide IN-1233, inhibitor specifically inhibits TGF-beta signaling via ALK-5 by acting as a competitive inhibitor of the ATP-binding site, inhibition of activin receptor-like kinase-5 signaling in vivo with the selective small-molecule inhibitor prevents pulmonary arterial hypertension, right ventricular hypertrophy, and vascular remodeling after monocrotaline injection and inhibits the progression of established pulmonary arterial hypertension in this model Rattus norvegicus
SD-208 inhibitor reduces the monocrotaline-induced increase in RV systolic pressure, but the effects on established pulmonary arterial hypertension are modest, and no convincing evidence for in vivo inhibition of TGF-beta-driven target genes is presented Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
 male sprague-dawley rats
-

Source Tissue

Source Tissue Comment Organism Textmining

Synonyms

Synonyms Comment Organism
activin receptor-like kinase-5
-
 Rattus norvegicus
ALK-1
-
 Rattus norvegicus
BMPR-II
-
 Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000034
-
-
 Rattus norvegicus 3-((4-(6-methylpyridin-2-yl)-5-(quinolin-6-yl)-1H-imidazol-2-yl)methyl)benzamide

Expression

Organism Comment Expression
Rattus norvegicus exposure to monocrotaline and chronic hypoxia leads to a reduction in the expression of BMPR-II mRNA in rat lungs by day 21 down

General Information

General Information Comment Organism
malfunction mutations in the TGF-type I receptor, activin receptor-like kinase (ALK)-1, cause hereditary hemorrhagic telangiectasia but have also been found in some cases of severe pulmonary arterial hypertension Rattus norvegicus