Target Validation Information | |||||
---|---|---|---|---|---|
Target ID | T98062 | ||||
Target Name | Glycogen phosphorylase, muscle form | ||||
Target Type | Discontinued |
||||
Drug Potency against Target | 1-D-glucopyranosyl uracil | Drug Info | Ki = 6100 nM | [530881] | |
2alpha-Hydroxyolean-12-en-28-oic acid | Drug Info | IC50 = 8500 nM | [530285] | ||
2-Hydroxyiminoolean-12-en-28-oic acid | Drug Info | IC50 = 13100 nM | [530285] | ||
2beta,3alpha-dihydroxyolean-12-en-28-oic acid | Drug Info | IC50 = 6250 nM | [529742] | ||
OLEANOLIC_ACID | Drug Info | IC50 = 14000 nM | [529507] | ||
BETULIN | Drug Info | IC50 = 17000 nM | [529507] | ||
3alpha-Hydroxyurs-12-en-28-oic Acid | Drug Info | IC50 = 19000 nM | [529507] | ||
PSN357 | Drug Info | IC50 = 0.14 nM | |||
URSOLIC ACID | Drug Info | IC50 = 15300 nM | [530285] | ||
2beta,3alpha-dihydroxyurs-12-en-28-oic acid | Drug Info | IC50 = 1100 nM | [529742] | ||
1-D-glucopyranosyl cytosine | Drug Info | Ki = 7700 nM | [530881] | ||
Oleanonic acid | Drug Info | IC50 = 18000 nM | [529507] | ||
2-isoursolic acid | Drug Info | IC50 = 5500 nM | [530285] | ||
ASIATIC ACID | Drug Info | IC50 = 17000 nM | [529507] | ||
Ethyl 2beta-hydroxyolean-12-en-28-oate | Drug Info | IC50 = 15300 nM | [530285] | ||
2alpha-Hydroxyurs-12-en-28-oic acid | Drug Info | IC50 = 1200 nM | [530285] | ||
2-Oxoolean-12-en-28-oic acid | Drug Info | IC50 = 14900 nM | [530285] | ||
Benzyl 2-hydroxyiminoolean-12-en-28-oate | Drug Info | IC50 = 16300 nM | [530285] | ||
23-hydroxybetulinic acid | Drug Info | IC50 = 16000 nM | [529507] | ||
2-isooleanolic acid | Drug Info | IC50 = 3500 nM | [530285] | ||
2-Hydroxyiminours-12-en-28-oic acid | Drug Info | IC50 = 14700 nM | [530285] | ||
N-Butyl 2beta-hydroxyolean-12-en-28-oate | Drug Info | IC50 = 13800 nM | [530285] | ||
Action against Disease Model | PSN357 | Preclinical data also suggest a role for glycogen phosphorylase, as exemplified by the results obtained with GPI-688, PSN-357 and CP-368296 in animal models | Drug Info | ||
The Effect of Target Knockout, Knockdown or Genetic Variations | In comparison to the normal course of the encystment process demonstrated in Fig. 3b and Fig. 4a to d, the glycogen phosphorylase knockdown resulted in a dramatic decrease in the n uMber of mature cysts and an increase in the n uMber of immature precysts (Fig. 3a and 4e to h). In both treated and untreated cultures, trophozoites predominated until 12 h poststimulation, whichwas the stage when the cells started to round up (Fig. 4a and e). In the siRNA-treated cultures, approximately 38% of cells (n = 130) detached and became rounded to form the precysts after approximately 24 h of encystment (Fig. 3a). The n uMber of precysts further increased, so that after 72 h, 70% of the cells with the glycogen phosphorylase knockdown presented the precyst phenotype (Fig. 3a and4h). As shown in Fig. 3b and 4d, at the corresponding stage of the normal encystment process, the precysts were absent and the mature cysts constituted 83% of the population. Some mature cysts were detected in siRNA-treated cultures (Fig. 3a and 4h), but their levels did not exceed 4.5%. | [530881] | |||
References | |||||
Ref 530881 | Bioorg Med Chem. 2010 May 15;18(10):3413-25. Epub 2010 Apr 7.1-(3-Deoxy-3-fluoro-beta-d-glucopyranosyl) pyrimidine derivatives as inhibitors of glycogen phosphorylase b: Kinetic, crystallographic and modelling studies. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. | ||||
Ref 529742 | J Nat Prod. 2008 Nov;71(11):1877-80. Epub 2008 Oct 11.Practical synthesis of bredemolic Acid, a natural inhibitor of glycogen phosphorylase. | ||||
Ref 529507 | J Med Chem. 2008 Jun 26;51(12):3540-54. Epub 2008 Jun 3.Naturally occurring pentacyclic triterpenes as inhibitors of glycogen phosphorylase: synthesis, structure-activity relationships, and X-ray crystallographic studies. | ||||
Ref 529507 | J Med Chem. 2008 Jun 26;51(12):3540-54. Epub 2008 Jun 3.Naturally occurring pentacyclic triterpenes as inhibitors of glycogen phosphorylase: synthesis, structure-activity relationships, and X-ray crystallographic studies. | ||||
Ref 529507 | J Med Chem. 2008 Jun 26;51(12):3540-54. Epub 2008 Jun 3.Naturally occurring pentacyclic triterpenes as inhibitors of glycogen phosphorylase: synthesis, structure-activity relationships, and X-ray crystallographic studies. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. | ||||
Ref 529742 | J Nat Prod. 2008 Nov;71(11):1877-80. Epub 2008 Oct 11.Practical synthesis of bredemolic Acid, a natural inhibitor of glycogen phosphorylase. | ||||
Ref 530881 | Bioorg Med Chem. 2010 May 15;18(10):3413-25. Epub 2010 Apr 7.1-(3-Deoxy-3-fluoro-beta-d-glucopyranosyl) pyrimidine derivatives as inhibitors of glycogen phosphorylase b: Kinetic, crystallographic and modelling studies. | ||||
Ref 529507 | J Med Chem. 2008 Jun 26;51(12):3540-54. Epub 2008 Jun 3.Naturally occurring pentacyclic triterpenes as inhibitors of glycogen phosphorylase: synthesis, structure-activity relationships, and X-ray crystallographic studies. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. | ||||
Ref 529507 | J Med Chem. 2008 Jun 26;51(12):3540-54. Epub 2008 Jun 3.Naturally occurring pentacyclic triterpenes as inhibitors of glycogen phosphorylase: synthesis, structure-activity relationships, and X-ray crystallographic studies. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. | ||||
Ref 529507 | J Med Chem. 2008 Jun 26;51(12):3540-54. Epub 2008 Jun 3.Naturally occurring pentacyclic triterpenes as inhibitors of glycogen phosphorylase: synthesis, structure-activity relationships, and X-ray crystallographic studies. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. | ||||
Ref 530285 | J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. |
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