Target Information
| Target General Information | Top | |||||
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| Target ID |
T21669
(Former ID: TTDI02088)
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| Target Name |
Glutathione S-transferase P (GSTP1)
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| Synonyms |
GSTP11; GSTP1-1; GST3; GST classpi; GST class-pi; FAEES3
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| Gene Name |
GSTP1
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| Target Type |
Clinical trial target
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[1] | ||||
| Disease | [+] 1 Target-related Diseases | + | ||||
| 1 | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | |||||
| Function |
Regulates negatively CDK5 activity via p25/p35 translocation to prevent neurodegeneration. Conjugation of reduced glutathione to a wide number of exogenous and endogenous hydrophobic electrophiles.
Click to Show/Hide
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| BioChemical Class |
Alkyl aryl transferase
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| UniProt ID | ||||||
| EC Number |
EC 2.5.1.18
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| Sequence |
MPPYTVVYFPVRGRCAALRMLLADQGQSWKEEVVTVETWQEGSLKASCLYGQLPKFQDGD
LTLYQSNTILRHLGRTLGLYGKDQQEAALVDMVNDGVEDLRCKYISLIYTNYEAGKDDYV KALPGQLKPFETLLSQNQGGKTFIVGDQISFADYNLLDLLLIHEVLAPGCLDAFPLLSAY VGRLSARPKLKAFLASPEYVNLPINGNGKQ Click to Show/Hide
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| 3D Structure | Click to Show 3D Structure of This Target | PDB | ||||
| HIT2.0 ID | T46AQJ | |||||
| Drugs and Modes of Action | Top | |||||
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| Clinical Trial Drug(s) | [+] 2 Clinical Trial Drugs | + | ||||
| 1 | Canfosfamide | Drug Info | Phase 3 | Solid tumour/cancer | [1] | |
| 2 | Ezatiostat | Drug Info | Phase 2 | Myelodysplastic syndrome | [2] | |
| Mode of Action | [+] 1 Modes of Action | + | ||||
| Modulator | [+] 2 Modulator drugs | + | ||||
| 1 | Canfosfamide | Drug Info | [1], [3] | |||
| 2 | Ezatiostat | Drug Info | [4] | |||
| Chemical Structure based Activity Landscape of Target | Top |
|---|---|
| Target Poor or Non Binders | Top | |||||
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| Target Poor or Non Binders | ||||||
| Target Regulators | Top | |||||
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| Target-regulating microRNAs | ||||||
| Target-regulating Transcription Factors | ||||||
| Target-interacting Proteins | ||||||
| Target Profiles in Patients | Top | |||||
|---|---|---|---|---|---|---|
| Target Expression Profile (TEP) | ||||||
| Target Affiliated Biological Pathways | Top | |||||
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| BioCyc | [+] 2 BioCyc Pathways | + | ||||
| 1 | Glutathione-mediated detoxification | |||||
| 2 | 4-hydroxy-2-nonenal detoxification | |||||
| KEGG Pathway | [+] 6 KEGG Pathways | + | ||||
| 1 | Glutathione metabolism | |||||
| 2 | Metabolism of xenobiotics by cytochrome P450 | |||||
| 3 | Drug metabolism - cytochrome P450 | |||||
| 4 | Pathways in cancer | |||||
| 5 | Chemical carcinogenesis | |||||
| 6 | Prostate cancer | |||||
| NetPath Pathway | [+] 1 NetPath Pathways | + | ||||
| 1 | TCR Signaling Pathway | |||||
| References | Top | |||||
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| REF 1 | Mechanism of glutathione transferase P1-1-catalyzed activation of the prodrug canfosfamide (TLK286, TELCYTA). Biochemistry. 2013 Nov 12;52(45):8069-78. | |||||
| REF 2 | ClinicalTrials.gov (NCT01422486) Phase 2 Study of Telintra in Deletion 5q Myelodysplastic Syndrome. U.S. National Institutes of Health. | |||||
| REF 3 | Phase 1 study of TLK286 (Telcyta) administered weekly in advanced malignancies. Clin Cancer Res. 2004 Jun 1;10(11):3689-98. | |||||
| REF 4 | National Cancer Institute Drug Dictionary (drug id 485244). | |||||
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