Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDC00099

Target Information
NameGlycogen phosphorylase, muscle form    
Type of targetDiscontinued target    
SynonymsGlycogen phosphorylase b    
Muscle glycogen phosphorylase    
DiseaseDiabetes Mellitus Type 2
[ICD9: 250   ICD10: E11]
[1]
Noninsulin-dependent diabetes mellitus
[ICD9: 250   ICD10: E08-E13]
[2][1]
Drug(s)PSN357Discontinued in Phase IIDiabetes Mellitus Type 2[3]
BioChemical ClassGlycosyltransferases    
EC NumberEC 2.4.1.1
PathwayInsulin signaling pathway
Starch and sucrose metabolism
UniProt IDP11217
PDB Structure1Z8D.    
FunctionPhosphorylase is an important allosteric enzyme in carbohydrate metabolism. Enzymes from different sources differ in their regulatory mechanisms and in their natural substrates. However, all known phosphorylases share catalytic and structural properties.    
SequenceMAKPLTDQEKRRQISIRGIVGVENVAELKKSFNRHLHFTLVKDRNVATTRDYYFALAHTV RDHLVGRWIRTQQHYYDKCPKRVYYLSLEFYMGRTLQNTMINLGLQNACDEAIYQLGLDI EELEEIEEDAGLGNGGLGRLAACFLDSMATLGLAAYGYGIRYEYGIFNQKIRDGWQVEEA DDWLRYGNPWEKSRPEFMLPVHFYGKVEHTNTGTKWIDTQVVLALPYDTPVPGYMNNTVN TMRLWSARAPNDFNLRDFNVGDYIQAVLDRNLAENISRVLYPNDNFFEGKELRLKQEYFV VAATLQDIIRRFKASKFGSTRGAGTVFDAFPDQVAIQLNDTHPALAIPELMRIFVDIEKL PWSKAWELTQKTFAYTNHTVLPEALERWPVDLVEKLLPRHLEIIYEINQKHLDRIVALFP KDVDRLRRMSLIEEEGSKRINMAHLCIVGSHAVNGVAKIHSDIVKTKVFKDFSELEPDKF QNKTNGITPRRWLLLCNPGLAELIAEKIGEDYVKDLSQLTKLHSFLGDDVFLRELAKVKQ ENKLKFSQFLETEYKVKINPSSMFDVQVKRIHEYKRQLLNCLHVITMYNRIKKDPKKLFV PRTVIIGGKAAPGYHMAKMIIKLITSVADVVNNDPMVGSKLKVIFLENYRVSLAEKVIPA TDLSEQISTAGTEASGTGNMKFMLNGALTIGTMDGANVEMAEEAGEENLFIFGMRIDDVA ALDKKGYEAKEYYEALPELKLVIDQIDNGFFSPKQPDLFKDIINMLFYHDRFKVFADYEA YVKCQDKVSQLYMNPKAWNTMVLKNIAASGKFSSDRTIKEYAQNIWNVEPSDLKISLSNE SNKVNGN
Related US Patent6,277,877
6,399,601
6,576,653
6,649,634
6,696,574
Target ValidationClick to Find Target Validation Information.    
Inhibitor1-D-glucopyranosyl cytosine[4]
1-D-glucopyranosyl uracil[4]
1-Deoxy-1-Methoxycarbamido-Beta-D-Glucopyranose[5]
1-N-Acetyl-Beta-D-Glucosamine[5]
2-Deoxy-Glucose-6-Phosphate[5]
2-Hydroxyiminoolean-12-en-28-oic acid[6]
2-Hydroxyiminours-12-en-28-oic acid[6]
2-Oxoolean-12-en-28-oic acid[6]
2-isooleanolic acid[6]
2-isoursolic acid[6]
23-hydroxybetulinic acid[7]
2alpha-Hydroxyolean-12-en-28-oic acid[6]
2alpha-Hydroxyurs-12-en-28-oic acid[6]
2beta,3alpha-dihydroxyolean-12-en-28-oic acid[8]
2beta,3alpha-dihydroxyurs-12-en-28-oic acid[8]
3-Oxoolean-12-en-28-oic Acid[7]
3alpha-Hydroxyurs-12-en-28-oic Acid[7]
4-{2-[ (3-Nitrobenzoyl)Amino]Phenoxy}Phthalic Acid[9]
ASIATIC ACID[7]
Acurea[1]
Alpha-D-Glucopyranosyl-2-Carboxylic Acid Amide[5]
Alpha-D-Glucose-1-Phosphate[5]
Alpha-D-Glucose-6-Phosphate[5]
BETULIN[7]
Benzyl 2-hydroxyiminoolean-12-en-28-oate[6]
Beta-D-Glucopyranose Spirohydantoin[5]
Beta-D-Glucose[5]
Bzurea[1]
C- (1-Azido-Alpha-D-Glucopyranosyl) Formamide[10]
C- (1-Hydrogyl-Beta-D-Glucopyranosyl) Formamide[5]
Ethyl 2beta-hydroxyolean-12-en-28-oate[6]
Flavopiridol[11]
Fluoro-Phosphite Ion[5]
Heptulose-2-Phosphate[5]
ISOFAGOMINE[12]
Indirubin-5-Sulphonate[5]
Inosinic Acid[5]
N'-Pyridoxyl-Lysine-5'-Monophosphate[5]
N-Acetyl-N'-Beta-D-Glucopyranosyl Urea[10]
N-Benzoyl-N'-Beta-D-Glucopyranosyl Urea[5]
Nojirimycine Tetrazole[9]
OLEANOLIC_ACID[7]
PSN357[3]
Phosphonoserine[5]
URSOLIC ACID[6]
n-Butyl 2beta-hydroxyolean-12-en-28-oate[6]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Binding of N-acetyl-N '-beta-D-glucopyranosyl urea and N-benzoyl-N '-beta-D-glucopyranosyl urea to glycogen phosphorylase b: kinetic and crystallographic studies. Eur J Biochem. 2002 Mar;269(6):1684-96. To Reference
Ref 2Glycogen phosphorylase as a molecular target for type 2 diabetes therapy. Curr Protein Pept Sci. 2002 Dec;3(6):561-86. To Reference
Ref 3CenterWatch. Drugs in Clinical Trials Database. CenterWatch. 2008. To Reference
Ref 4Bioorg 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. To Reference
Ref 5Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 6J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase. To Reference
Ref 7J 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. To Reference
Ref 8J Nat Prod. 2008 Nov;71(11):1877-80. Epub 2008 Oct 11.Practical synthesis of bredemolic Acid, a natural inhibitor of glycogen phosphorylase. To Reference
Ref 9Berman HM, Westbrook J, Feng Z, Gilliland G, Bhat TN, Weissig H, Shindyalov IN, Bourne PE: The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. To Reference
Ref 10Nucleic Acids Res. 2011 January; 39(Database issue): D1035¨CD1041. DrugBank 3.0: a comprehensive resource for ¡®Omics¡¯ research on drugs To Reference
Ref 11Zvelebil MJ: Flavopiridol (Hoechst AG). IDrugs. 1998 Jun;1(2):241-6. To Reference
Ref 12J Med Chem. 2006 Sep 21;49(19):5687-701.Iminosugars as potential inhibitors of glycogenolysis: structural insights into the molecular basis of glycogen phosphorylase inhibition. To Reference



 

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