Target Information

Target General Infomation
Target ID
T98062
Former ID
TTDC00099
Target Name
Glycogen phosphorylase, muscle form
Gene Name
PYGM
Synonyms
Glycogen phosphorylase b; Muscle glycogen phosphorylase; PYGM
Target Type
Discontinued
Disease Type 2 diabetes [ICD9: 250; ICD10: E11]
Function
Phosphorylase 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.
BioChemical Class
Hexosyltransferase
Target Validation
T98062
UniProt ID
P11217
EC Number
EC 2.4.1.1
Sequence
MSRPLSDQEKRKQISVRGLAGVENVTELKKNFNRHLHFTLVKDRNVATPRDYYFALAHTV
RDHLVGRWIRTQQHYYEKDPKRIYYLSLEFYMGRTLQNTMVNLALENACDEATYQLGLDM
EELEEIEEDAGLGNGGLGRLAACFLDSMATLGLAAYGYGIRYEFGIFNQKISGGWQMEEA
DDWLRYGNPWEKARPEFTLPVHFYGHVEHTSQGAKWVDTQVVLAMPYDTPVPGYRNNVVN
TMRLWSAKAPNDFNLKDFNVGGYIQAVLDRNLAENISRVLYPNDNFFEGKELRLKQEYFV
VAATLQDIIRRFKSSKFGCRDPVRTNFDAFPDKVAIQLNDTHPSLAIPELMRILVDLERM
DWDKAWDVTVRTCAYTNHTVLPEALERWPVHLLETLLPRHLQIIYEINQRFLNRVAAAFP
GDVDRLRRMSLVEEGAVKRINMAHLCIAGSHAVNGVARIHSEILKKTIFKDFYELEPHKF
QNKTNGITPRRWLVLCNPGLAEVIAERIGEDFISDLDQLRKLLSFVDDEAFIRDVAKVKQ
ENKLKFAAYLEREYKVHINPNSLFDIQVKRIHEYKRQLLNCLHVITLYNRIKREPNKFFV
PRTVMIGGKAAPGYHMAKMIIRLVTAIGDVVNHDPAVGDRLRVIFLENYRVSLAEKVIPA
ADLSEQISTAGTEASGTGNMKFMLNGALTIGTMDGANVEMAEEAGEENFFIFGMRVEDVD
KLDQRGYNAQEYYDRIPELRQVIEQLSSGFFSPKQPDLFKDIVNMLMHHDRFKVFADYED
YIKCQEKVSALYKNPREWTRMVIRNIATSGKFSSDRTIAQYAREIWGVEPSRQRLPAPDE
AI
Drugs and Mode of Action
Drug(s) JTT-651 Drug Info Discontinued in Phase 1 Type 2 diabetes [548600]
Inhibitor 1-D-glucopyranosyl cytosine Drug Info [530881]
1-D-glucopyranosyl uracil Drug Info [530881]
1-Deoxy-1-Methoxycarbamido-Beta-D-Glucopyranose Drug Info [551393]
1-N-Acetyl-Beta-D-Glucosamine Drug Info [551393]
2-Deoxy-Glucose-6-Phosphate Drug Info [551393]
2-Hydroxyiminoolean-12-en-28-oic acid Drug Info [530285]
2-Hydroxyiminours-12-en-28-oic acid Drug Info [530285]
2-isooleanolic acid Drug Info [530285]
2-isoursolic acid Drug Info [530285]
2-Oxoolean-12-en-28-oic acid Drug Info [530285]
23-hydroxybetulinic acid Drug Info [529507]
2alpha-Hydroxyolean-12-en-28-oic acid Drug Info [530285]
2alpha-Hydroxyurs-12-en-28-oic acid Drug Info [530285]
2beta,3alpha-dihydroxyolean-12-en-28-oic acid Drug Info [529742]
2beta,3alpha-dihydroxyurs-12-en-28-oic acid Drug Info [529742]
3alpha-Hydroxyurs-12-en-28-oic Acid Drug Info [529507]
4-{2-[(3-Nitrobenzoyl)Amino]Phenoxy}Phthalic Acid Drug Info [551374]
Acurea Drug Info [535400]
Alpha-D-Glucopyranosyl-2-Carboxylic Acid Amide Drug Info [551393]
Alpha-D-Glucose-1-Phosphate Drug Info [551393]
Alpha-D-Glucose-6-Phosphate Drug Info [551393]
ASIATIC ACID Drug Info [529507]
Benzyl 2-hydroxyiminoolean-12-en-28-oate Drug Info [530285]
Beta-D-Glucopyranose Spirohydantoin Drug Info [551393]
Beta-D-Glucose Drug Info [551393]
BETULIN Drug Info [529507]
Bzurea Drug Info [535400]
C-(1-Azido-Alpha-D-Glucopyranosyl) Formamide Drug Info [551391]
C-(1-Hydrogyl-Beta-D-Glucopyranosyl) Formamide Drug Info [551393]
Ethyl 2beta-hydroxyolean-12-en-28-oate Drug Info [530285]
Fluoro-Phosphite Ion Drug Info [551393]
Heptulose-2-Phosphate Drug Info [551393]
Indirubin-5-Sulphonate Drug Info [551393]
Inosinic Acid Drug Info [551393]
JTT-651 Drug Info [548601]
N'-Pyridoxyl-Lysine-5'-Monophosphate Drug Info [551393]
N-Acetyl-N'-Beta-D-Glucopyranosyl Urea Drug Info [551391]
N-Benzoyl-N'-Beta-D-Glucopyranosyl Urea Drug Info [551393]
N-Butyl 2beta-hydroxyolean-12-en-28-oate Drug Info [530285]
Nojirimycine Tetrazole Drug Info [551374]
OLEANOLIC_ACID Drug Info [529507]
Oleanonic acid Drug Info [529507]
Phosphonoserine Drug Info [551393]
URSOLIC ACID Drug Info [530285]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway Glycogenolysis
KEGG Pathway Starch and sucrose metabolism
Metabolic pathways
Insulin signaling pathway
Glucagon signaling pathway
PANTHER Pathway Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway
WikiPathways Glycogen Metabolism
Metabolism of carbohydrates
References
Ref 548600Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026877)
Ref 529507J 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 529742J Nat Prod. 2008 Nov;71(11):1877-80. Epub 2008 Oct 11.Practical synthesis of bredemolic Acid, a natural inhibitor of glycogen phosphorylase.
Ref 530285J Nat Prod. 2009 Aug;72(8):1414-8.Synthesis of 3-deoxypentacyclic triterpene derivatives as inhibitors of glycogen phosphorylase.
Ref 530881Bioorg 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 535400Binding 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.
Ref 548601Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800026877)
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551391DrugBank 3.0: a comprehensive resource for 'omics' research on drugs. Nucleic Acids Res. 2011 Jan;39(Database issue):D1035-4. Nucleic Acids Res. 2011 January
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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