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Literature summary for 1.1.1.146 extracted from

  • Anderson, S.; Carreiro, S.; Quenzer, T.; Gale, D.; Xiang, C.; Gukasyan, H.; Lafontaine, J.; Cheng, H.; Krauss, A.; Prasanna, G.
    In vivo evaluation of 11beta-hydroxysteroid dehydrogenase activity in the rabbit eye (2009), J. Ocul. Pharmacol. Ther., 25, 215-222.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
carbenoxolone potent and selective 11beta-HSD1 inhibitor Oryctolagus cuniculus
PF-3319913 potent and selective 11beta-HSD1 inhibitor, a 1% dose of PF-3319913 inhibits in vivo 11beta-HSD1 enzyme activity in the rabbit eye by 100% at 2 h Oryctolagus cuniculus
PF-3859622 potent and selective 11beta-HSD1 inhibitor, a 2% dose of PF-3859622 consistently inhibits in vivo 11beta-HSD1 enzyme activity in the rabbit eye by 100% at 6 and 12 h, a 0.2% dose of PF-3859622 causes 81% inhibition of cortisone conversion at 6 h Oryctolagus cuniculus
PF-904955 potent and selective 11beta-HSD1 inhibitor, a 1% dose of PF-904955 inhibits in vivo 11beta-HSD1 enzyme activity in the rabbit eye by 88% at 2 h Oryctolagus cuniculus

Organism

Organism UniProt Comment Textmining
Oryctolagus cuniculus
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
eye 11beta-HSD1 is widely expressed in the eye, particularly ciliary epithelium Oryctolagus cuniculus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
cortisol + NADP+
-
Oryctolagus cuniculus cortisone + NADPH
-
r

Synonyms

Synonyms Comment Organism
11beta-HSD1
-
Oryctolagus cuniculus
11beta-hydroxysteroid dehydrogenase-1
-
Oryctolagus cuniculus

Cofactor

Cofactor Comment Organism Structure
NADP+
-
Oryctolagus cuniculus