Target Information
| Target General Infomation | |||||
|---|---|---|---|---|---|
| Target ID |
T99616
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| Former ID |
TTDR00585
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| Target Name |
Trypanothione reductase
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| Gene Name |
TPR
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| Synonyms |
N(1),N(8)-bis(glutathionyl)spermidine reductase; Parasite-specific trypanothione reductase; TR; TRYR; TPR
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| Target Type |
Research
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| Disease | Kinetoplastids [ICD9: 085, 086; ICD10: B55, B56, B57] | ||||
| Function |
Trypanothione is the parasite analog of glutathione; this enzyme is the equivalent of glutathione reductase.
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| BioChemical Class |
Oxidoreductases acting on a sulfur group of donors
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| Target Validation |
T99616
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| UniProt ID | |||||
| EC Number |
EC 1.8.1.12
|
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| Sequence |
MSKIFDLVVIGAGSGGLEAGWNAATLYKKRVAVIDVQTHHGPPHYAALGGTCVNVGCVPK
KLMVTGAQYMDHLRESAGFGWEFDGSSVKANWKKLIAAKNEAVLDINKSYEGMFNDTEGL DFFLGWGSLESKNVVVVRETADPKSAVKERLQADHILLATGSWPQMPAIPGVEHCISSNE AFYLPEPPRRVLTVGGGFISVEFAGIFNAYKPPGGKVTLCYRNNLILRGFDETIREEVTK QLTANGIEIMTNENPAKVSLNTDGSKHVTFESGKTLDVDVVMMAIGRIPRTNDLQLGNVG VKLTPKGGVQVDEFSRTNVPNIYAIGDITDRLMLTPVAINEGAALVDTVFGNKPRKTDHT RVASAVFSIPPIGTCGLIEEVAAKEFEKVAVYMSSFTPLMHNISGSKYKKFVAKIVTNHS DGTVLGVHLLGDGAPEIIQAVGVCLRLNAKISDFYNTIGVHPTSAEELCSMRTPSYYYLK GEKMETLPESSL |
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| Inhibitor | 1-(2'-chlorophenyl)penta-1,4-dien-3-one | Drug Info | [1] | ||
| 8-Methoxy-naphtho[2,3-b]thiophen-4,9-quinone | Drug Info | [2] | |||
| CEPHARANTINE | Drug Info | [3] | |||
| CONESSINE | Drug Info | [3] | |||
| Flavin-Adenine Dinucleotide | Drug Info | [4] | |||
| Maleic Acid | Drug Info | [5] | |||
| N-(5-chloro-2-(phenylthio)phenyl)butyramide | Drug Info | [6] | |||
| N1,N2-bis(dihydrocaffeoyl)spermine | Drug Info | [3] | |||
| Trypanothione | Drug Info | [4] | |||
| Binder | Tricyclics | Drug Info | [7] | ||
| References | |||||
| REF 1 | J Med Chem. 2005 Nov 17;48(23):7400-10.Irreversible inactivation of trypanothione reductase by unsaturated Mannich bases: a divinyl ketone as key intermediate. | ||||
| REF 2 | 8-Methoxy-naphtho[2,3-b]thiophen-4,9-quinone, a non-competitive inhibitor of trypanothione reductase. Mem Inst Oswaldo Cruz. 2003 Jun;98(4):565-8. Epub 2003 Aug 18. | ||||
| REF 3 | Bioorg Med Chem. 2008 Jul 15;16(14):6689-95. Epub 2008 Jun 2.The use of natural product scaffolds as leads in the search for trypanothione reductase inhibitors. | ||||
| REF 4 | How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. | ||||
| REF 5 | The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42. | ||||
| REF 6 | J Med Chem. 2005 Dec 15;48(25):8087-97.Antitrypanosomal, antileishmanial, and antimalarial activities of quaternary arylalkylammonium 2-amino-4-chlorophenyl phenyl sulfides, a new class of trypanothione reductase inhibitor, and of N-acyl derivatives of 2-amino-4-chlorophenyl phenyl sulfide. | ||||
| REF 7 | Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40. | ||||
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