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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