Target General Infomation
Target ID
T99616
Former ID
TTDR00585
Target Name
Trypanothione reductase
Gene Name
TPR
Synonyms
N(1),N(8)-bis(glutathionyl)spermidine reductase; Parasite-specific trypanothione reductase; TR; TRYR; TPR
Target Type
Research
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.
BioChemical Class
Oxidoreductases acting on a sulfur group of donors
Target Validation
T99616
UniProt ID
EC Number
EC 1.8.1.12
Sequence
MSKIFDLVVIGAGSGGLEAGWNAATLYKKRVAVIDVQTHHGPPHYAALGGTCVNVGCVPK
KLMVTGAQYMDHLRESAGFGWEFDGSSVKANWKKLIAAKNEAVLDINKSYEGMFNDTEGL
DFFLGWGSLESKNVVVVRETADPKSAVKERLQADHILLATGSWPQMPAIPGVEHCISSNE
AFYLPEPPRRVLTVGGGFISVEFAGIFNAYKPPGGKVTLCYRNNLILRGFDETIREEVTK
QLTANGIEIMTNENPAKVSLNTDGSKHVTFESGKTLDVDVVMMAIGRIPRTNDLQLGNVG
VKLTPKGGVQVDEFSRTNVPNIYAIGDITDRLMLTPVAINEGAALVDTVFGNKPRKTDHT
RVASAVFSIPPIGTCGLIEEVAAKEFEKVAVYMSSFTPLMHNISGSKYKKFVAKIVTNHS
DGTVLGVHLLGDGAPEIIQAVGVCLRLNAKISDFYNTIGVHPTSAEELCSMRTPSYYYLK
GEKMETLPESSL
Inhibitor 1-(2'-chlorophenyl)penta-1,4-dien-3-one Drug Info [527860]
8-Methoxy-naphtho[2,3-b]thiophen-4,9-quinone Drug Info [535783]
CEPHARANTINE Drug Info [529537]
CONESSINE Drug Info [529537]
Flavin-Adenine Dinucleotide Drug Info [551393]
Maleic Acid Drug Info [551374]
N-(5-chloro-2-(phenylthio)phenyl)butyramide Drug Info [527919]
N1,N2-bis(dihydrocaffeoyl)spermine Drug Info [529537]
Trypanothione Drug Info [551393]
Binder Tricyclics Drug Info [536135]
References
Ref 527860J 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 527919J 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 529537Bioorg 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 5357838-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 536135Opportunities and challenges in antiparasitic drug discovery. Nat Rev Drug Discov. 2005 Sep;4(9):727-40.
Ref 551374The Protein Data Bank. Nucleic Acids Res. 2000 Jan 1;28(1):235-42.
Ref 551393How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6.

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