Target Information
Target General Information | Top | |||||
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Target ID |
T72042
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Target Name |
GAR transformylase (GART)
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Synonyms |
Phosphoribosylglycinamide formyltransferase; 5'-phosphoribosylglycinamide transformylase; GART
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Gene Name |
GART
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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 |
A folate-dependent enzyme, essential for the de novo purine synthesis pathway.
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UniProt ID | ||||||
EC Number |
EC 2.1.2.2
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Sequence |
VAVLISGTGSNLQALIDSTREPNSSAQIDIVISNKAAVAGLDKAERAGIPTRVINHKLYK
NRVEFDSAIDLVLEEFSIDIVCLAGFMRILSGPFVQKWNGKMLNIHPSLLPSFKGSNAHE QALETGVTVTGCTVHFVAEDVDAGQIILQEAVPVKRGDTVATLSERVKLAEHKIFPAALQ LVASGTVQLGENGKICWVKEE Click to Show/Hide
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3D Structure | Click to Show 3D Structure of This Target | PDB |
Drugs and Modes of Action | Top | |||||
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Clinical Trial Drug(s) | [+] 1 Clinical Trial Drugs | + | ||||
1 | AG2034 | Drug Info | Phase 1 | Solid tumour/cancer | [1] | |
Mode of Action | [+] 1 Modes of Action | + | ||||
Modulator | [+] 2 Modulator drugs | + | ||||
1 | AG2034 | Drug Info | [1] | |||
2 | DDATHF | Drug Info | [2] |
References | Top | |||||
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REF 1 | Phase I study of AG2034, a targeted GARFT inhibitor, administered once every 3 weeks. Cancer Chemother Pharmacol. 2000;45(5):423-7. | |||||
REF 2 | Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,... Biochemistry. 2003 May 27;42(20):6043-56. |
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