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Literature summary for 1.1.1.146 extracted from

  • Cabrera Perez, L.C.; Padilla-Martinez, I.I.; Cruz, A.; Correa Basurto, J.; Miliar Garcia, A.; Hernandez Zavala, A.A.; Gomez Lopez, M.; Rosales Hernandez, M.C.
    Design, synthesis, molecular docking and in vitro evaluation of benzothiazole derivatives as 11beta-hydroxysteroid dehydrogenase type 1 inhibitors (2020), Mol. Divers., 24, 971-984 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2S)-2-[[(E)-[(1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-3-(4-hydroxyphenyl)propanoic acid
-
Rattus norvegicus
(E)-5-((benzo[d]thiazol-2-ylimino)(methylthio)methylamino)-2-hydroxybenzoic acid
-
Rattus norvegicus
2-hydroxy-5-[[(E)-[(5-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
Rattus norvegicus
2-hydroxy-5-[[(E)-[(5-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
Rattus norvegicus
2-hydroxy-5-[[(E)-[(6-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
Rattus norvegicus
2-hydroxy-5-[[(E)-[(6-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
Rattus norvegicus
2-hydroxy-5-[[(E)-[(7-methoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
Rattus norvegicus
2-hydroxy-5-[[(E)-[(7-methyl-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]benzoic acid
-
Rattus norvegicus
5-[[(E)-[(5-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
Rattus norvegicus
5-[[(E)-[(5-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
Rattus norvegicus
5-[[(E)-[(5-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
Rattus norvegicus
5-[[(E)-[(6-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
Rattus norvegicus
5-[[(E)-[(6-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
Rattus norvegicus
5-[[(E)-[(6-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
Rattus norvegicus
5-[[(E)-[(7-chloro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
Rattus norvegicus
5-[[(E)-[(7-ethoxy-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
Rattus norvegicus
5-[[(E)-[(7-fluoro-1,3-benzothiazol-2-yl)imino](methylsulfanyl)methyl]amino]-2-hydroxybenzoic acid
-
Rattus norvegicus
carbenoxolone
-
Rattus norvegicus
clobenzorex
-
Rattus norvegicus
PF-877423
-
Rattus norvegicus
resveratrol
-
Rattus norvegicus
SAR184841
-
Rattus norvegicus

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.193
-
cortisone at pH 7.5 and 37°C Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
corticosterone + NADPH + H+ Rattus norvegicus
-
corticosterol + NADP+
-
?
cortisone + NADPH + H+ Rattus norvegicus
-
cortisol + NADP+
-
?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus P16232
-
-

Source Tissue

Source Tissue Comment Organism Textmining
white adipose tissue
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
corticosterone + NADPH + H+
-
Rattus norvegicus corticosterol + NADP+
-
?
cortisone + NADPH + H+
-
Rattus norvegicus cortisol + NADP+
-
?

Synonyms

Synonyms Comment Organism
11-beta hydroxysteroid dehydrogenase type 1
-
Rattus norvegicus
11beta-HSD1
-
Rattus norvegicus
11beta-hydroxysteroid dehydrogenase type 1
-
Rattus norvegicus

General Information

General Information Comment Organism
malfunction the inhibition of isoform 11beta-HSD1 attenuates the development of type 2 diabetes mellitus, insulin resistance, metabolic syndrome and other diseases mediated by excessive cortisol production Rattus norvegicus