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Literature summary for 2.7.1.1 extracted from

  • Coghlan, M.; Leighton, B.
    Glucokinase activators in diabetes management (2008), Expert Opin. Investig. Drugs, 17, 145-167.
    View publication on PubMed

Activating Compound

Activating Compound Comment Organism Structure
(2E)-3-cyclopentyl-2-[4-(cyclopropylsulfonyl)phenyl]-N-[4-(1,2-dihydroxyethyl)-1,3-thiazol-2-yl]prop-2-enamide
-
Homo sapiens
2-amino-N-(4-methyl-1,3-thiazol-2-yl)-5-[(4-methyl-4H-1,2,4-triazol-3-yl)sulfanyl]benzamide
-
Homo sapiens
2-[(3-cyclopentyl-2-[4-[(4-methylpiperazin-1-yl)sulfonyl]phenyl]propanoyl)amino]-5-methoxy-1H-[1,3]thiazolo[5,4-b]pyridin-3-ium
-
Homo sapiens
3-(5-chloro-1,3-thiazol-2-yl)-1-[4-(methylsulfonyl)phenyl]-1-(thiophen-2-ylmethyl)urea
-
Homo sapiens
4-[4-(dimethylcarbamoyl)-3-fluorophenoxy]-2-ethyl-2-methyl-N-(5-methylpyridin-2-yl)-2,3-dihydro-1-benzofuran-6-carboxamide
-
Homo sapiens
5-(2-methylpropyl)-N-(1,3-thiazol-2-yl)-1H-indazol-3-amine
-
Homo sapiens
fructose
-
Homo sapiens
GKA50
-
Homo sapiens
N,N-dicyclohexyl-N'-methyldicarbonimidic diamide
-
Homo sapiens
N-(4-methyl-1,3-thiazol-2-yl)-3-(pyridin-3-ylmethoxy)pyridin-2-amine
-
Homo sapiens
RO-281675
-
Homo sapiens
RO-4389620 also known as R1440, GK2, or piragliatin Homo sapiens

Application

Application Comment Organism
medicine activation of glucokinase as glucose lowering therapy for type 2 diabetes Homo sapiens

Protein Variants

Protein Variants Comment Organism
T65I mutant shows reduced activity (41%) compared to the wild type enzyme Homo sapiens
V455M mutant shows increased activity (108%) compared to the wild type enzyme Homo sapiens
W99R mutant shows slightly increased activity (219%) compared to the wild type enzyme Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Homo sapiens
-
pancreatic beta cell
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
glucokinase
-
Homo sapiens

General Information

General Information Comment Organism
malfunction heterozygous or homozygous loss of function in the glucokinase gene causes either mild diabetes (maturity onset diabetes of the young type 2 [MODY2]) or severe neo-natal onset diabetes, respectively Homo sapiens