Target Validation Information
TTD ID T31514
Target Name Lysosomal alpha-glucosidase (GAA)
Type of Target
Successful
Drug Potency against Target Acarbose Drug Info IC50 = 430 nM [8]
(-)-uniflorine A Drug Info IC50 = 12000 nM [4]
(R)-2,6-Bis-hydroxymethyl-piperidine-3,4,5-triol Drug Info IC50 = 2700 nM [7]
2,5-imino-2,5,6-trideoxy-D-manno-heptitol Drug Info IC50 = 7200 nM [6]
7-O-b-D-Glucopyranosyl-a-homonojirimycin Drug Info IC50 = 380 nM [3]
Alpha-7-Deoxyhomonojirimycin Drug Info IC50 = 19000 nM [1]
Alpha-Homonojirimycin Drug Info IC50 = 80 nM [3]
Deoxynojirimycin Drug Info IC50 = 130 nM [3]
N-adamantanemethyloxypentyl-1-deoxynojirimycin Drug Info IC50 = 400 nM [5]
SALACINOL Drug Info Ki = 970 nM [2]
UNIFLORINE B Drug Info IC50 = 4000 nM [4]
VALIOLAMINE Drug Info IC50 = 18000 nM [3]
Action against Disease Model Acarbose Drug Info Acarbose attenuates postprandial hyperlipidemia in an intestinal absorptive cell model, Exposure of Caco-2 cells to acarbose at a concentration of 10 mmol/L reduced oleic acid absorption by 30%, triglyceride-rich lipoprotein secretion by around 10%, and apo B-48 secretion by 50%, whereas apo A-I secretion was not affected [9]
References
REF 1 New polyhydroxylated pyrrolidine, piperidine, and pyrrolizidine alkaloids from Scilla sibirica. J Nat Prod. 2002 Dec;65(12):1875-81.
REF 2 Alpha-glucosidase inhibitor from Kothala-himbutu (Salacia reticulata WIGHT). J Nat Prod. 2008 Jun;71(6):981-4.
REF 3 In vitro inhibition of glycogen-degrading enzymes and glycosidases by six-membered sugar mimics and their evaluation in cell cultures. Bioorg Med Chem. 2008 Aug 1;16(15):7330-6.
REF 4 Total synthesis of (-)-uniflorine A. J Nat Prod. 2009 Nov;72(11):2058-60.
REF 5 Synthesis and evaluation of D-gluco-pyranocyclopropyl amines as potential glucosidase inhibitors. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6600-3.
REF 6 Nitrogen-containing furanose and pyranose analogues from Hyacinthus orientalis. J Nat Prod. 1998 May;61(5):625-8.
REF 7 Homonojirimycin isomers and N-alkylated homonojirimycins: structural and conformational basis of inhibition of glycosidases. J Med Chem. 1998 Jul 2;41(14):2565-71.
REF 8 Luteolin, a flavone, does not suppress postprandial glucose absorption through an inhibition of alpha-glucosidase action. Biosci Biotechnol Biochem. 2002 Mar;66(3):689-92.
REF 9 Acarbose attenuates postprandial hyperlipidemia: investigation in an intestinal absorptive cell model. Metabolism. 2009 May;58(5):583-5.

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