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Literature summary for 3.1.3.11 extracted from

  • Dang, Q.; Kasibhatla, S.R.; Reddy, K.R.; Jiang, T.; Reddy, M.R.; Potter, S.C.; Fujitaki, J.M.; van Poelje, P.D.; Huang, J.; Lipscomb, W.N.; Erion, M.D.
    Discovery of potent and specific fructose-1,6-bisphosphatase inhibitors and a series of orally-bioavailable phosphoramidase-sensitive prodrugs for the treatment of type 2 diabetes (2007), J. Am. Chem. Soc., 129, 15491-15502.
    View publication on PubMed
Search for more literature for 3.1.3.11

Application

Application Comment Organism
medicine oral administration of the prodrug, MB06322, to Zucker Diabetic Fatty rats leads to dose-dependent inhibition of gluconeogenesis and endogenous glucose production and consequently to significant blood glucose reduction Rattus norvegicus

Crystallization (Commentary)

Crystallization (Comment) Organism
three-dimensional structure of the human FBPase-2-amino-5-isobutyl-4-[2-(5-phosphono)furanyl]thiazole inhibitor complex is solved at 2.0 A resolution, hanging drop method Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
2-amino-5-isobutyl-4-[2-(5-phosphono)furanyl]thiazole poor oral bioavailability Homo sapiens
2-amino-5-isobutyl-4-[2-(5-phosphono)furanyl]thiazole poor oral bioavailability Rattus norvegicus
AMP
-
 Homo sapiens
AMP
-
 Rattus norvegicus
MB06322 oral administration of the prodrug, MB06322, to Zucker Diabetic Fatty rats leads to dose-dependent inhibition of gluconeogenesis and endogenous glucose production and consequently to significant blood glucose reduction Rattus norvegicus
[5-(1,3-thiazol-4-yl)-2-furyl]phosphonic acid
-
 Homo sapiens
[5-(2-amino-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
-
 Homo sapiens
[5-(2-amino-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
-
 Rattus norvegicus
[5-(2-amino-5-isobutyl-1,3-oxazol-4-yl)-2-furyl]phosphonic acid
-
 Homo sapiens
[5-(2-amino-5-isobutyl-1,3-oxazol-4-yl)-2-furyl]phosphonic acid
-
 Rattus norvegicus
[5-(2-amino-5-isobutyl-1H-imidazol-4-yl)-2-furyl]phosphonic acid
-
 Homo sapiens
[5-(2-amino-5-phenyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
-
 Homo sapiens
[5-(2-amino-5-phenyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
-
 Rattus norvegicus
[5-(2-amino-5-propyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
-
 Homo sapiens
[5-(5-isobutyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
-
 Homo sapiens
[5-(5-isobutyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
-
 Rattus norvegicus
[5-(6-amino-3-phenylpyridin-2-yl)-2-furyl]phosphonic acid
-
 Homo sapiens
[5-(6-amino-3-phenylpyridin-2-yl)-2-furyl]phosphonic acid
-
 Rattus norvegicus
[5-[2-amino-5-(2-methylpropyl)-1,3-selenazol-4-yl]furan-2-yl]phosphonic acid
-
 Homo sapiens
[5-[2-amino-5-(2-methylpropyl)-1,3-selenazol-4-yl]furan-2-yl]phosphonic acid
-
 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-
Rattus norvegicus
-
-
-

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000014
-
-
 Homo sapiens [5-(2-amino-5-phenyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
0.00003
-
-
 Homo sapiens [5-(2-amino-5-propyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
0.000039
-
-
 Homo sapiens [5-[2-amino-5-(2-methylpropyl)-1,3-selenazol-4-yl]furan-2-yl]phosphonic acid
0.000042
-
-
 Homo sapiens [5-(6-amino-3-phenylpyridin-2-yl)-2-furyl]phosphonic acid
0.00012
-
-
 Homo sapiens [5-(2-amino-5-isobutyl-1,3-oxazol-4-yl)-2-furyl]phosphonic acid
0.00015
-
-
 Rattus norvegicus [5-[2-amino-5-(2-methylpropyl)-1,3-selenazol-4-yl]furan-2-yl]phosphonic acid
0.00045
-
-
 Homo sapiens [5-(2-amino-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
0.0005
-
-
 Homo sapiens [5-(5-isobutyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
0.0005
-
-
 Rattus norvegicus [5-(2-amino-5-phenyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
0.001
-
-
 Homo sapiens AMP
0.0016
-
-
 Rattus norvegicus [5-(6-amino-3-phenylpyridin-2-yl)-2-furyl]phosphonic acid
0.002
-
-
 Rattus norvegicus [5-(2-amino-5-isobutyl-1,3-oxazol-4-yl)-2-furyl]phosphonic acid
0.0035
-
-
 Rattus norvegicus [5-(5-isobutyl-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
0.005
-
-
 Homo sapiens [5-(2-amino-5-isobutyl-1H-imidazol-4-yl)-2-furyl]phosphonic acid
0.005
-
-
 Homo sapiens [5-(1,3-thiazol-4-yl)-2-furyl]phosphonic acid
0.013
-
-
 Rattus norvegicus [5-(2-amino-1,3-thiazol-4-yl)-2-furyl]phosphonic acid
0.016
-
-
 Homo sapiens 2-amino-5-isobutyl-4-[2-(5-phosphono)furanyl]thiazole
0.02
-
-
 Rattus norvegicus AMP
0.061
-
-
 Rattus norvegicus 2-amino-5-isobutyl-4-[2-(5-phosphono)furanyl]thiazole