Reference on EC 2.1.2.2 - phosphoribosylglycinamide formyltransferase 1
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Daubner, S.C.; Schrimsher, J.L.; Schendel, F.J.; Young, M.; Henikoff, S.; Patterson, D.; Stubbe, J.; Benkovic, S.J.
A multifunctional protein possessing glycinamide ribonucleotide synthetase, glycinamide ribonucleotide transformylase, and aminoimidazole ribonucleotide synthetase activities in de novo purine biosynthesis
Biochemistry
24
7059-7062
1985
Saccharomyces cerevisiae, Gallus gallus, Drosophila melanogaster, Schizosaccharomyces pombe
Caperelli, C.A.; Liu, D.
Carbocyclic substrates for de novo purine biosynthesis. Enantiospecific synthesis and enantiospecificity of enzymatic utilization
J. Biol. Chem.
267
9783-9787
1992
Homo sapiens, Mus musculus
Caperelli, C.A.; Benkovic, P.A.; Chettur, G.; Benkovic, S.J
Purification of a complex catalizing folate cofactor synthesis and transformylation in de novo purine biosynthesis
J. Biol. Chem.
255
1885-1890
1980
Saccharomyces cerevisiae, Gallus gallus, Columba sp., Oryctolagus cuniculus, Ovis aries, Sus scrofa
Hards, R.G.; Graw, S.L.; Patterson, D.
Purification of mammalian glycinamide ribonucleotide (GAR) synthetase
Adv. Exp. Med. Biol.
195
315-319
1986
Rattus norvegicus
-
Caperelli, C.A.; Chettur, G.; Lin-Kosley, L.
Purification of glycineamide ribonucleotide transformylase
Dev. Biochem.
4
371-376
1979
Gallus gallus
-
Warren, L.; Buchanan, J.M.
Biosynthesis of the purines. XIX. 2-Amino-N-ribosylacetamide 5'-phosphate(glycinamide ribotide) transformylase
J. Biol. Chem.
229
613-626
1957
Gallus gallus, Clostridium cylindrosporum, Columba sp.
Smith, G.K.; Benkovic, P.A.; Benkovic, S.J.
L(-)-10-formyltetrahydrofolate is the cofactor for glycinamide ribonucleotide transformylase from chicken liver
Biochemistry
20
4034-4036
1981
Gallus gallus, Escherichia coli
Chen, P.; Schulze-Gahmen, U.; Stura, E.A.; Inglese, J.; Johnson, D.L.; Marolewski, A.; Benkovic, S.J.; Wilson, I.A.
Crystal structure of glycinamide ribonucleotide transformylase from Escherichia coli at 3.0 A resolution
J. Mol. Biol.
227
283-292
1992
Bacillus subtilis, Saccharomyces cerevisiae, Drosophila melanogaster, Escherichia coli, Homo sapiens, Mus musculus
Caperelli, C.A.; Chettur, G.; Lin, L.Y.; Benkovic, S.J.
Purification of glycineamide ribonucleotide transformylase
Biochem. Biophys. Res. Commun.
82
403-410
1978
Saccharomyces cerevisiae, Gallus gallus, Ovis aries, Sus scrofa
Caperelli, C.A.; Price, M.F.
Carbocyclic glycinamide ribonucleotide is a substrate for glycinamide ribonucleotide transformylase
Arch. Biochem. Biophys.
264
340-342
1988
Mus musculus
Inglese, J.; Johnson, D.L.; Shiau, A.; Smith, J.M.; Benkovic, S.J.
Subcloning, characterization, and affinity labeling of Escherichia coli glycinamide ribonucleotide transformylase
Biochemistry
29
1436-1443
1990
Bacillus subtilis, Cricetulus griseus, Drosophila melanogaster, Escherichia coli, Gallus gallus, Homo sapiens, Mus musculus, Saccharomyces cerevisiae
Almassy, R.J.; Janson, C.A.; Kann, C.C.; Hostomska, Z.
Structures of apo and complexed Escherichia coli glycinamide ribonucleotide transformylase
Proc. Natl. Acad. Sci. USA
89
6114-6118
1992
Escherichia coli, Mus musculus
Stura, E.A.; Johnson, D.L; Inglese, J.; Smith, J.M.; Benkovic, S.J.; Wilson, I.A.
Preliminary crystallographic investigations of glycinamide ribonucleotide transformylase
J. Biol. Chem.
264
9703-9706
1989
Escherichia coli
Young, M.; Sammons, R.D.; Mueller, W.T.; Benkovic, S.J.
An antibody probe to determine the native species of glycinamide ribonucleotide transformylase in chicken liver
Biochemistry
23
3979-3986
1984
Gallus gallus, Mus musculus
Caperelli, C.A.
Mammalian glycinamide ribonucleotide transformylase: Purification and some properties
Biochemistry
24
1316-1320
1985
Gallus gallus, Mus musculus
Caperelli, C.A.
Mammalian glycinamide ribonucleotide transformylase. Kinetic mechanism and associated de novo purine biosynthesis activities
J. Biol. Chem.
264
5053-5057
1989
Gallus gallus, Drosophila melanogaster, Homo sapiens, Mus musculus
Dev, I.K.; Harvey, R.J.
N10-Formyltetrahydrofolate is the formyl donor for glycinamide ribonucleotide transformylase in Escherichia coli
J. Biol. Chem.
253
4242-4244
1978
Escherichia coli, Escherichia coli B / ATCC 11303, Gallus gallus, Salmonella enterica subsp. enterica serovar Typhimurium
Smith, G.K.; Mueller, W.T.; Wasserman, G.F.; Taylor, W.D.; Benkovic, S.J.
Characterization of the enzyme complex involving the folate-requiring enzymes of de novo purine biosynthesis
Biochemistry
19
4313-4321
1980
Gallus gallus, Escherichia coli
Warren, M.S.; Marolewski, A.E.; Benkovic, S.J.
A rapid screen of active site mutants in glycinamide ribonucleotide transformylase
Biochemistry
35
8855-8862
1996
Bacillus subtilis, Saccharomyces cerevisiae, Gallus gallus, Drosophila melanogaster, Escherichia coli, Homo sapiens
Liu, C.; Shim, J.H.; Benkovic, S.J.
The unexpected catalytic properties of a heterodimer of GAR transformylase
Bioorg. Chem.
28
316-323
2000
Escherichia coli
Sanghani, S.P.; Moran, R.G.
Tight binding of folate substrates and inhibitors to recombinant mouse glycinamide ribonucleotide formyltransferase
Biochemistry
36
10506-10516
1997
Gallus gallus, Escherichia coli, Homo sapiens, Mus musculus
Marolewski, A.; Smith, J.M.; Benkovic, S.J.
Cloning and characterization of a new purine biosynthetic enzyme: a non-folate glycinamide ribonucleotide transformylase from E. coli
Biochemistry
33
2531-2537
1994
Escherichia coli, Escherichia coli TX635
Nixon, A.E.; Benkovic, S.J.
Improvement in the efficiency of formyl transfer of a GAR transformylase hybrid enzyme
Protein Eng.
13
323-327
2000
Escherichia coli
Caperelli, C.A.; Giroux, E.L.
The human glycinamide ribonucleotide transformylase domain: purification, characterization, and kinetic mechanism
Arch. Biochem. Biophys.
341
98-103
1997
Bacillus subtilis, Saccharomyces cerevisiae, Gallus gallus, Escherichia coli, Homo sapiens
Antle, V.D.; Donat, N.; Hua, M.; Liao, P.L.; Vince, R.; Caperelli, C.A.
Substrate specificity of human glycinamide ribonucleotide transformylase
Arch. Biochem. Biophys.
370
231-235
1999
Gallus gallus, Escherichia coli, Homo sapiens
McMorran, B.J.; Kumara, H.M.C.S.; Sullivan, K.; Lamont, I.L.
Involvement of a transformylase enzyme in siderophore synthesis in Pseudomonas aeruginosa
Microbiology
147
1517-1524
2001
Arabidopsis thaliana, Bacillus subtilis, Saccharomyces cerevisiae, Drosophila melanogaster, Escherichia coli, Pseudomonas aeruginosa
Habeck, L.L.; Leitner, T.A.; Shackelford, K.A.; Gossett, L.S.; Schultz, R.M.; Andis, S.L.; Shih, C.; Grindey, G.B.; Mendelsohn, L.G.
A novel class of monoglutamated antifolates exhibits tight-binding inhibition of human glycinamide ribonucleotide formyltransferase and potent activity against solid tumors
Cancer Res.
54
1021-1026
1994
Homo sapiens, Mus musculus
Antle, V.D.; Liu, D.; McKellar, B.R.; Caperelli, C.A.; Hua, M.; Vince, R.
Substrate specificity of glycinamide ribonucleotide transformylase from chicken liver
J. Biol. Chem.
271
6045-6049
1996
Gallus gallus, Escherichia coli
Shim, J.H.; Benkovic, S.J.
Evaluation of the kinetic mechanism of Escherichia coli glycinamide ribonucleotide transformylase
Biochemistry
37
8776-8782
1998
Escherichia coli, Homo sapiens, Mus musculus
Gooljarsingh, L.T.; Ramcharan, J.; Gilroy, S.; Benkovic, S.J.
Localization of GAR transformylase in Escherichia coli and mammalian cells
Proc. Natl. Acad. Sci. USA
98
6565-6570
2001
Escherichia coli, Homo sapiens
Shim, J.H.; Benkovic, S.J.
Evaluation of the kinetic mechanism of Escherichia coli glycinamide ribonucleotide transformylase probed by site-directed mutagenesis and pH-dependent studies
Biochemistry
38
10024-10031
1999
Escherichia coli
Hartman, S.C.; Buchanan, J.M.
Biosynthesis of the purines. XXVI. The Identification of the formyl donors of the transformylation reactions
J. Biol. Chem.
234
1812-1816
1959
Gallus gallus
Zhang, Y.; Desharnais, J.; Marsilje, T.H.; Li, C.; Hedrick, M.P.; Gooljarsingh, L.T.; Tavassoli, A.; Benkovic, S.J.; Olson, A.J.; Boger, D.L.; Wilson, I.A.
Rational design, synthesis, evaluation, and crystal structure of a potent inhibitor of human GAR Tfase: 10-(trifluoroacetyl)-5,10-dideazaacyclic-5,6,7,8-tetrahydrofolic acid
Biochemistry
42
6043-6056
2003
Homo sapiens (P22102), Homo sapiens
Shi, C.; Chen, V.J.; et.al.
LY231514, a pyrrolo[2,3-d]pyrimidine-based antifolate that inhibits multiple folate-requiring enzymes
Cancer Res.
57
1116-1123
1997
Homo sapiens
Lee, S.G.; Lutz, S.; Benkovic, S.J.
On the structural and functional modularity of glycinamide ribonucleotide formyltransferases
Protein Sci.
12
2206-2214
2003
Homo sapiens
Cheng, H.; Chong, Y.; Hwang, I.; Tavassoli, A.; Zhang, Y.; Wilson, I.A.; Benkovic, S.J.; Boger, D.L.
Design, synthesis, and biological evaluation of 10-methanesulfonyl-DDACTHF, 10-methanesulfonyl-5-DACTHF, and 10-methylthio-DDACTHF as potent inhibitors of GAR Tfase and the de novo purine biosynthetic pathway
Bioorg. Med. Chem.
13
3577-3585
2005
Escherichia coli, Homo sapiens
Chong, Y.; Hwang, I.; Tavassoli, A.; Zhang, Y.; Wilson, I.A.; Benkovic, S.J.; Boger, D.L.
Synthesis and biological evaluation of alpha- and gamma-carboxamide derivatives of 10-CF3CO-DDACTHF
Bioorg. Med. Chem.
13
3587-3592
2005
Escherichia coli, Homo sapiens
Cheng, H.; Hwang, I.; Chong, Y.; Tavassoli, A.; Webb, M.E.; Zhang, Y.; Wilson, I.A.; Benkovic, S.J.; Boger, D.L.
Synthesis and biological evaluation of N-[4-[5-(2,4-diamino-6-oxo-1,6-dihydropyrimidin-5-yl)-2-(2,2,2-trifluoroacetyl)pentyl]benzoyl]-L-glutamic acid as a potential inhibitor of GAR Tfase and the de novo purine biosynthetic pathway
Bioorg. Med. Chem.
13
3593-3599
2005
Escherichia coli, Homo sapiens
Woehlke, A.; Droegemueller, C.; Kuiper, H.; Leeb, T.; Distl, O.
Molecular characterization and chromosomal assignment of the bovine glycinamide ribonucleotide formyltransferase (GART) gene on cattle chromosome 1q12.1-q12.2
Gene
348
73-81
2005
Bos taurus (Q599X3), Bos taurus (Q599X4), Bos taurus (Q599X5), Bos taurus
Manieri, W.; Moore, M.E.; Soellner, M.B.; Tsang, P.; Caperelli, C.A.
Human glycinamide ribonucleotide transformylase: active site mutants as mechanistic probes
Biochemistry
46
156-163
2007
Homo sapiens
Deng, Y.; Wang, Y.; Cherian, C.; Hou, Z.; Buck, S.A.; Matherly, L.H.; Gangjee, A.
Synthesis and discovery of high affinity folate receptor-specific glycinamide ribonucleotide formyltransferase inhibitors with antitumor activity
J. Med. Chem.
51
5052-5063
2008
Homo sapiens, Mus musculus
DeMartino, J.K.; Hwang, I.; Connelly, S.; Wilson, I.A.; Boger, D.L.
Asymmetric synthesis of inhibitors of glycinamide ribonucleotide transformylase
J. Med. Chem.
51
5441-5448
2008
Homo sapiens
Liang, Y.H.; Liu, X.Y.; Wang, J.; Li, L.F.
Protein preparation, crystallization and preliminary crystallographic studies of Bacillus subtilis glycinamide ribonucleotide transformylase
Acta Crystallogr. Sect. F
65
709-711
2009
Bacillus subtilis (P12040), Bacillus subtilis
McGuire, J.J.; Haile, W.H.
Metabolism-blocked antifolates as potential anti-rheumatoid arthritis agents: 4-amino-4-deoxy-5,8,10-trideazapteroyl-D,L-4-methyleneglutamic acid (CH-1504) and its analogs
Biochem. Pharmacol.
77
1161-1172
2009
Homo sapiens
Deng, Y.; Zhou, X.; Kugel Desmoulin, S.; Wu, J.; Cherian, C.; Hou, Z.; Matherly, L.H.; Gangjee, A.
Synthesis and biological activity of a novel series of 6-substituted thieno[2,3-d]pyrimidine antifolate inhibitors of purine biosynthesis with selectivity for high affinity folate receptors over the reduced folate carrier and proton-coupled folate transpo
J. Med. Chem.
52
2940-2951
2009
Homo sapiens, Mus musculus
Zhang, Z.; Caradoc-Davies, T.T.; Dickson, J.M.; Baker, E.N.; Squire, C.J.
Structures of glycinamide ribonucleotide transformylase (PurN) from Mycobacterium tuberculosis reveal a novel dimer with relevance to drug discovery
J. Mol. Biol.
389
722-733
2009
Mycobacterium tuberculosis (P9WHM5), Mycobacterium tuberculosis, Mycobacterium tuberculosis H37Rv (P9WHM5)
Zhai, F.; Liu, X.; Ruan, J.; Li, J.; Liu, Z.; Hu, Y.; Li, S.
Expression, crystallization and preliminary X-ray analysis of the phosphoribosylglycinamide formyltransferase from Streptococcus mutans
Acta Crystallogr. Sect. F
67
287-290
2011
Streptococcus mutans
Connelly, S.; DeMartino, J.K.; Boger, D.L.; Wilson, I.A.
Biological and structural evaluation of 10R- and 10S-methylthio-DDACTHF reveals a new role for sulfur in inhibition of glycinamide ribonucleotide transformylase
Biochemistry
52
5133-5144
2013
Homo sapiens (P22102), Homo sapiens
Liu, Y.; Zhang, C.; Zhang, H.; Li, M.; Yuan, J.; Zhang, Y.; Zhou, J.; Guo, H.; Zhao, L.; Du, Y.; Wang, L.; Ren, L.
Synthesis and antitumor activity of a novel series of 6-substituted pyrrolo[2,3-d]pyrimidines as potential nonclassical antifolates targeting both thymidylate and purine nucleotide biosynthesis
Eur. J. Med. Chem.
93
142-155
2015
Homo sapiens (P22102)
Cong, X.; Lu, C.; Huang, X.; Yang, D.; Cui, X.; Cai, J.; Lv, L.; He, S.; Zhang, Y.; Ni, R.
Increased expression of glycinamide ribonucleotide transformylase is associated with a poor prognosis in hepatocellular carcinoma, and it promotes liver cancer cell proliferation
Hum. Pathol.
45
1370-1378
2014
Homo sapiens (P22102), Homo sapiens
Mitchell-Ryan, S.; Wang, Y.; Raghavan, S.; Ravindra, M.P.; Hales, E.; Orr, S.; Cherian, C.; Hou, Z.; Matherly, L.H.; Gangjee, A.
Discovery of 5-substituted pyrrolo[2,3-d]pyrimidine antifolates as dual-acting inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase in de novo purine nucleotide biosynthesis: Implications of inhibiting 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase to AMPK activation and anti-tumor activity
J. Med. Chem.
56
10016-10032
2013
Homo sapiens (P22102), Homo sapiens
Wang, Y.; Cherian, C.; Orr, S.; Mitchell-Ryan, S.; Hou, Z.; Raghavan, S.; Matherly, L.H.; Gangjee, A.
Tumor-targeting with novel non-benzoyl 6-substituted straight chain pyrrolo[2,3-d]pyrimidine antifolates via cellular uptake by folate receptor alpha and inhibition of de novo purine nucleotide biosynthesis
J. Med. Chem.
56
8684-8695
2013
Homo sapiens (P22102), Homo sapiens
Wang, Y.; Mitchell-Ryan, S.; Raghavan, S.; George, C.; Orr, S.; Hou, Z.; Matherly, L.H.; Gangjee, A.
Novel 5-substituted pyrrolo[2,3-d]pyrimidines as dual inhibitors of glycinamide ribonucleotide formyltransferase and 5-aminoimidazole-4-carboxamide ribonucleotide formyltransferase and as potential antitumor agents
J. Med. Chem.
58
1479-1493
2015
Homo sapiens (P22102), Homo sapiens
Liu, X.; Ding, Z.; Liu, Y.; Zhang, J.; Liu, F.; Wang, X.; He, X.; Cui, G.; Wang, D.
Glycinamide ribonucleotide formyl transferase is frequently overexpressed in glioma and critically regulates the proliferation of glioma cells
Pathol. Res. Pract.
210
256-263
2014
Homo sapiens (P22102)
Liu, X.; Ding, Z.; Liu, Y.; Zhang, J.; Liu, F.; Wang, X.; He, X.; Cui, G.; Wang, D.
Glycinamide ribonucleotide formyl transferase is frequently overexpressed in glioma and critically regulates the proliferation of glioma cells
Pathol. Res. Pract.
210
256-263
2014
Homo sapiens (P22102)
Deis, S.M.; Doshi, A.; Hou, Z.; Matherly, L.H.; Gangjee, A.; Dann, C.E.
Structural and enzymatic analysis of tumor-targeted antifolates that inhibit glycinamide ribonucleotide formyltransferase
Biochemistry
55
4574-4582
2016
Homo sapiens
Xing, R.; Zhang, H.; Yuan, J.; Zhang, K.; Li, L.; Guo, H.; Zhao, L.; Zhang, C.; Li, S.; Gao, T.; Liu, Y.; Wang, L.
Novel 6-substituted benzoyl and non-benzoyl straight chain pyrrolo[2,3-d]pyrimidines as potential antitumor agents with multitargeted inhibition of TS, GARFTase and AICARFTase
Eur. J. Med. Chem.
139
531-541
2017
Homo sapiens
Xu, L.; Wang, L.; Wang, J.; Zhu, Z.; Chang, G.; Guo, Y.; Tian, X.; Niu, B.
The effect of inhibiting glycinamide ribonucleotide formyl transferase on the development of neural tube in mice
Nutr. Metab.
13
56
2016
Mus musculus
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