Target Information

Target General Infomation
Target ID
T19433
Former ID
TTDS00192
Target Name
Glutathione S-transferase
Gene Name
HPGDS
Synonyms
GST class-alpha; Glutathione-S-transferase; HPGDS
Target Type
Successful
Disease Allergy [ICD9: 995.3; ICD10: T78.4]
Alzheimer disease [ICD9: 331; ICD10: G30]
Flatworms infection [ICD9: 120-129; ICD10: B65-B83]
Function
Bifunctional enzyme which catalyzes both the conversion of PGH2 to PGD2, a prostaglandin involved in smooth muscle contraction/relaxation and a potent inhibitor of platelet aggregation, and the conjugation of glutathione with a widerange of aryl halides and organic isothiocyanates. Also exhibits low glutathione-peroxidase activity towards cumene hydroperoxide.
BioChemical Class
Intramolecular oxidoreductases
Target Validation
T19433
UniProt ID
O60760
EC Number
EC 2.5.1.18
Sequence
MPNYKLTYFNMRGRAEIIRYIFAYLDIQYEDHRIEQADWPEIKSTLPFGKIPILEVDGLT
LHQSLAIARYLTKNTDLAGNTEMEQCHVDAIVDTLDDFMSCFPWAEKKQDVKEQMFNELL
TYNAPHLMQDLDTYLGGREWLIGNSVTWADFYWEICSTTLLVFKPDLLDNHPRLVTLRKK
VQAIPAVANWIKRRPQTKL
Drugs and Mode of Action
Drug(s) Praziquantel Drug Info Approved Flatworms infection [536135]
HF-0220 Drug Info Phase 2 Alzheimer disease [521861]
Inhibitor Cibacron blue Drug Info [537154]
Formic Acid Drug Info [551393]
HQL-79 Drug Info [528089]
Praziquantel Drug Info [536194]
Protoporphyrin IX Drug Info [536585]
S-hexylglutathione Drug Info [536040]
Antagonist H-PGDS inhibitors Drug Info [543414]
Stimulator HF-0220 Drug Info [550953]
Target Expression Profile (TEP) and Drug Resistance Mutation (DRM)
TEP EXP Info
Pathways
BioCyc Pathway C20 prostanoid biosynthesis
KEGG Pathway Arachidonic acid metabolism
Metabolic pathways
WikiPathways Arachidonic acid metabolism
Aryl Hydrocarbon Receptor
Integrated Pancreatic Cancer Pathway
References
Ref 521861ClinicalTrials.gov (NCT00357357) European Study of HF0220 in Mild to Moderate Alzheimer's Disease Patients. U.S. National Institutes of Health.
Ref 536135Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40.
Ref 528089Structural and functional characterization of HQL-79, an orally selective inhibitor of human hematopoietic prostaglandin D synthase. J Biol Chem. 2006 Jun 2;281(22):15277-86. Epub 2006 Mar 17.
Ref 536040Purification and catalytic properties of glutathione transferase from the hepatopancreas of crayfish macrobrachium vollenhovenii (herklots). J Biochem Mol Toxicol. 2004;18(6):332-44.
Ref 536194X-ray structure of glutathione S-transferase from Schistosoma japonicum in a new crystal form reveals flexibility of the substrate-binding site. Acta Crystallogr Sect F Struct Biol Cryst Commun. 2005Mar 1;61(Pt 3):263-5. Epub 2005 Feb 24.
Ref 536585Inhibition of glutathione-S-transferase from Plasmodium yoelii by protoporphyrin IX, cibacron blue and menadione: implications and therapeutic benefits. Parasitol Res. 2008 Mar;102(4):805-7. Epub 2008 Jan 5.
Ref 537154A novel method for screening the glutathione transferase inhibitors. BMC Biochem. 2009 Mar 16;10:6.
Ref 543414(http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 1381).
Ref 550953US patent application no. 2009,0062,529, Multi-cyclic compounds.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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