Target Information
| Target General Information | Top | |||||
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| Target ID |
T19433
(Former ID: TTDS00192)
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| Target Name |
Glutathione-dependent PGD synthase (HPGDS)
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| Synonyms |
HPGDS; Glutathione-S-transferase; GST class-alpha
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| Gene Name |
HPGDS
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| Target Type |
Successful target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Flatworm infection [ICD-11: 1F70-1F86] | |||||
| 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.
Click to Show/Hide
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| BioChemical Class |
Intramolecular oxidoreductases
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| UniProt ID | ||||||
| EC Number |
EC 5.3.99.2
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| Sequence |
MPNYKLTYFNMRGRAEIIRYIFAYLDIQYEDHRIEQADWPEIKSTLPFGKIPILEVDGLT
LHQSLAIARYLTKNTDLAGNTEMEQCHVDAIVDTLDDFMSCFPWAEKKQDVKEQMFNELL TYNAPHLMQDLDTYLGGREWLIGNSVTWADFYWEICSTTLLVFKPDLLDNHPRLVTLRKK VQAIPAVANWIKRRPQTKL Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T78T4E | |||||
| Drugs and Modes of Action | Top | |||||
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| Approved Drug(s) | [+] 1 Approved Drugs | + | ||||
| 1 | Praziquantel | Drug Info | Approved | Flatworm infection | [2] | |
| Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
| 1 | HF-0220 | Drug Info | Phase 2 | Alzheimer disease | [3] | |
| Mode of Action | [+] 2 Modes of Action | + | ||||
| Inhibitor | [+] 6 Inhibitor drugs | + | ||||
| 1 | Praziquantel | Drug Info | [1] | |||
| 2 | Cibacron blue | Drug Info | [5] | |||
| 3 | Formic Acid | Drug Info | [6] | |||
| 4 | HQL-79 | Drug Info | [7] | |||
| 5 | Protoporphyrin IX | Drug Info | [8] | |||
| 6 | S-hexylglutathione | Drug Info | [9] | |||
| Stimulator | [+] 1 Stimulator drugs | + | ||||
| 1 | HF-0220 | Drug Info | [4] | |||
| Chemical Structure based Activity Landscape of Target | Top |
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| Drug Property Profile of Target | Top | |
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| (1) Molecular Weight (mw) based Drug Clustering | (2) Octanol/Water Partition Coefficient (xlogp) based Drug Clustering | |
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| (3) Hydrogen Bond Donor Count (hbonddonor) based Drug Clustering | (4) Hydrogen Bond Acceptor Count (hbondacc) based Drug Clustering | |
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| (5) Rotatable Bond Count (rotbonds) based Drug Clustering | (6) Topological Polar Surface Area (polararea) based Drug Clustering | |
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| "RO5" indicates the cutoff set by lipinski's rule of five; "D123AB" colored in GREEN denotes the no violation of any cutoff in lipinski's rule of five; "D123AB" colored in PURPLE refers to the violation of only one cutoff in lipinski's rule of five; "D123AB" colored in BLACK represents the violation of more than one cutoffs in lipinski's rule of five | ||
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Profiles in Patients | Top | |||||
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| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| BioCyc | [+] 1 BioCyc Pathways | + | ||||
| 1 | C20 prostanoid biosynthesis | |||||
| KEGG Pathway | [+] 2 KEGG Pathways | + | ||||
| 1 | Arachidonic acid metabolism | |||||
| 2 | Metabolic pathways | |||||
| WikiPathways | [+] 3 WikiPathways | + | ||||
| 1 | Arachidonic acid metabolism | |||||
| 2 | Aryl Hydrocarbon Receptor | |||||
| 3 | Integrated Pancreatic Cancer Pathway | |||||
| Target-Related Models and Studies | Top | |||||
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| Target Validation | ||||||
| References | Top | |||||
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| REF 1 | 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. 2005 Mar 1;61(Pt 3):263-5. | |||||
| REF 2 | Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. | |||||
| REF 3 | ClinicalTrials.gov (NCT00357357) European Study of HF0220 in Mild to Moderate Alzheimer's Disease Patients. U.S. National Institutes of Health. | |||||
| REF 4 | US patent application no. 2009,0062,529, Multi-cyclic compounds. | |||||
| REF 5 | A novel method for screening the glutathione transferase inhibitors. BMC Biochem. 2009 Mar 16;10:6. | |||||
| REF 6 | How many drug targets are there Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | |||||
| REF 7 | 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. | |||||
| REF 8 | Inhibition of glutathione-S-transferase from Plasmodium yoelii by protoporphyrin IX, cibacron blue and menadione: implications and therapeutic bene... Parasitol Res. 2008 Mar;102(4):805-7. | |||||
| REF 9 | Purification and catalytic properties of glutathione transferase from the hepatopancreas of crayfish macrobrachium vollenhovenii (herklots). J Biochem Mol Toxicol. 2004;18(6):332-44. | |||||
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