Therapeutic Targets Database
BIDD Pharmainformatics Databases
 
   
   

 

TTD Target ID: TTDR01240

Target Information
NameGlycinamide ribonucleotide formyltransferase    
Type of targetResearch target    
Synonyms5'-phosphoribosylglycinamide transformylase    
GAR transformylase    
GARFT    
GART    
Glycinamide ribonucleotide transformylase    
Phosphoribosylglycinamide formyltransferase    
DiseaseSolid tumor
[ICD9: 140-199, 210-229   ICD10: C00-C75, C7A, C7B, D10-D36, D3A]
[1][2][3]
EC NumberEC 2.1.2.2
PathwayMetabolic pathways
One carbon pool by folate
Purine metabolism
UniProt IDP22102
PDB Structure1MEJ; 1MEN; 1MEO; 1NJS; 1RBM; 1RBQ; 1RBY; 1RBZ; 1RC0; 1RC1; 1ZLX; 1ZLY; 2QK4; 2V9Y.    
SequenceMAARVLIIGSGGREHTLAWKLAQSHHVKQVLVAPGNAGTACSEKISNTAISISDHTALAQ FCKEKKIEFVVVGPEAPLAAGIVGNLRSAGVQCFGPTAEAAQLESSKRFAKEFMDRHGIP TAQWKAFTKPEEACSFILSADFPALVVKASGLAAGKGVIVAKSKEEACKAVQEIMQEKAF GAAGETIVIEELLDGEEVSCLCFTDGKTVAPMPPAQDHKRLLEGDGGPNTGGMGAYCPAP QVSNDLLLKIKDTVLQRTVDGMQQEGTPYTGILYAGIMLTKNGPKVLEFNCRFGDPECQV ILPLLKSDLYEVIQSTLDGLLCTSLPVWLENHTALTVVMASKGYPGDYTKGVEITGFPEA QALGLEVFHAGTALKNGKVVTHGGRVLAVTAIRENLISALEEAKKGLAAIKFEGAIYRKD VGFRAIAFLQQPRSLTYKESGVDIAAGNMLVKKIQPLAKATSRSGCKVDLGGFAGLFDLK AAGFKDPLLASGTDGVGTKLKIAQLCNKHDTIGQDLVAMCVNDILAQGAEPLFFLDYFSC GKLDLSVTEAVVAGIAKACGKAGCALLGGETAEMPDMYPPGEYDLAGFAVGAMERDQKLP HLERITEGDVVVGIASSGLHSNGFSLVRKIVAKSSLQYSSPAPDGCGDQTLGDLLLTPTR IYSHSLLPVLRSGHVKAFAHITGGGLLENIPRVLPEKLGVDLDAQTWRIPRVFSWLQQEG HLSEEEMARTFNCGVGAVLVVSKEQTEQILRDIQQHKEEAWVIGSVVARAEGSPRVKVKN LIESMQINGSVLKNGSLTNHFSFEKKKARVAVLISGTGSNLQALIDSTREPNSSAQIDIV ISNKAAVAGLDKAERAGIPTRVINHKLYKNRVEFDSAIDLVLEEFSIDIVCLAGFMRILS GPFVQKWNGKMLNIHPSLLPSFKGSNAHEQALETGVTVTGCTVHFVAEDVDAGQIILQEA VPVKRGDTVATLSERVKLAEHKIFPAALQLVASGTVQLGENGKICWVKEE
Target ValidationClick to Find Target Validation Information.    
Inhibitor (10r)-10-Formyl-5,8,10-Trideazafolic Acid[4]
10-CF3C (OH)2-DDACTHF[4]
10-Formyl-5,8,10-Trideazafolic Acid[4]
10-trifluoroacetyl-DDACTHF[5]
AG2034[1]
DDATHF[6]
DIDEAZAFOLATE[7]
Glycinamide Ribonucleotide[4]
LOMETREXOL[8]
LY309887[1][9]
dideazaacyclotetrahydrofolic acid[10]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1New antimetabolites in cancer chemotherapy and their clinical impact. Br J Cancer. 1998;78 Suppl 3:1-7. To Reference
Ref 2New Antifolates: Pharmacology and Clinical Applications. Oncologist. 1996;1(1 & 2):68-81. To Reference
Ref 3Cobalamin-dependent methionine synthase and serine hydroxymethyltransferase: targets for chemotherapeutic intervention? Adv Enzyme Regul. 1998;38:377-92. To Reference
Ref 4Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. To Reference
Ref 5J Med Chem. 2006 May 18;49(10):2998-3002.Discovery of a potent, nonpolyglutamatable inhibitor of glycinamide ribonucleotide transformylase. To Reference
Ref 6Loss of folylpoly-gamma-glutamate synthetase activity is a dominant mechanism of resistance to polyglutamylation-dependent novel antifolates in multiple human leukemia sublines. Int J Cancer. 2003 Feb 20;103(5):587-99. To Reference
Ref 7J Med Chem. 1987 Jul;30(7):1254-6.N10-substituted 5,8-dideazafolate inhibitors of glycinamide ribonucleotide transformylase. To Reference
Ref 8J Med Chem. 2010 Feb 11;53(3):1306-18.Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidine thienoyl antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors and the proton-coupled folate transporter over the reduced folate carrier for cellular entry. To Reference
Ref 9Cellular pharmacology of MTA: a correlation of MTA-induced cellular toxicity and in vitro enzyme inhibition with its effect on intracellular folate and nucleoside triphosphate pools in CCRF-CEM cells. Semin Oncol. 1999 Apr;26(2 Suppl 6):48-54. To Reference
Ref 10J Med Chem. 2008 Sep 11;51(17):5441-8. Epub 2008 Aug 8.Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase. To Reference



 

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