Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T19433
|
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| Former ID |
TTDS00192
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| Target Name |
Glutathione S-transferase
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| Gene Name |
HPGDS
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| Synonyms |
GST class-alpha; Glutathione-S-transferase; HPGDS
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| Target Type |
Successful
|
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| 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.
|
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| BioChemical Class |
Intramolecular oxidoreductases
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| Target Validation |
T19433
|
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| UniProt ID | |||||
| EC Number |
EC 2.5.1.18
|
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| Sequence |
MPNYKLTYFNMRGRAEIIRYIFAYLDIQYEDHRIEQADWPEIKSTLPFGKIPILEVDGLT
LHQSLAIARYLTKNTDLAGNTEMEQCHVDAIVDTLDDFMSCFPWAEKKQDVKEQMFNELL TYNAPHLMQDLDTYLGGREWLIGNSVTWADFYWEICSTTLLVFKPDLLDNHPRLVTLRKK VQAIPAVANWIKRRPQTKL |
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| Drugs and Mode of Action | |||||
| Drug(s) | Praziquantel | Drug Info | Approved | Flatworms infection | [1] |
| HF-0220 | Drug Info | Phase 2 | Alzheimer disease | [2] | |
| Inhibitor | Cibacron blue | Drug Info | [3] | ||
| Formic Acid | Drug Info | [4] | |||
| HQL-79 | Drug Info | [5] | |||
| Praziquantel | Drug Info | [6] | |||
| Protoporphyrin IX | Drug Info | [7] | |||
| S-hexylglutathione | Drug Info | [8] | |||
| Antagonist | H-PGDS inhibitors | Drug Info | [9] | ||
| Stimulator | HF-0220 | Drug Info | [10] | ||
| 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 1 | Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. | ||||
| REF 2 | ClinicalTrials.gov (NCT00357357) European Study of HF0220 in Mild to Moderate Alzheimer's Disease Patients. U.S. National Institutes of Health. | ||||
| REF 3 | A novel method for screening the glutathione transferase inhibitors. BMC Biochem. 2009 Mar 16;10:6. | ||||
| REF 4 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
| REF 5 | Structural 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 6 | X-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 7 | Inhibition 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 8 | Purification and catalytic properties of glutathione transferase from the hepatopancreas of crayfish macrobrachium vollenhovenii (herklots). J Biochem Mol Toxicol. 2004;18(6):332-44. | ||||
| REF 9 | (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 10 | US patent application no. 2009,0062,529, Multi-cyclic compounds. | ||||
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