Reference on EC 2.1.1.45 - thymidylate synthase
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REF. 
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Bachmann, B.; Follmann, H.
Deoxyribonucleotide biosynthesis in green algae: characterization of thymidylate synthase-dihydrofolate reductase in Scenedesmus obliquus
Arch. Biochem. Biophys.
256
244-252
1987
Abies sp., Bos taurus, Saccharomyces cerevisiae, Chlamydomonas reinhardtii, Daucus carota, Leishmania major, Mus musculus, Nicotiana tabacum, Tetradesmus obliquus
Wahba, A.J.; Friedkin, M.
The enzymatic synthesis of thymidylate. I. Early steps in the purification of thymidylate synthetase of Escherichia coli
J. Biol. Chem.
237
3794-3801
1962
Escherichia coli, Enterococcus faecalis, Escherichia coli B / ATCC 11303
Blakeley, R.L.
The biosythesis of thymidylic acid. IV. Further studies on thymidylate synthetase
J. Biol. Chem.
238
2113-2118
1963
Escherichia coli, Enterococcus faecalis, Homo sapiens
-
Fridland, A.; Langenbach, R.J.; Heidelberger, C.
Purification of thymidylate synthetase from Ehrlich ascites carcinoma cells
J. Biol. Chem.
246
7110-7114
1971
Bos taurus, Gallus gallus, Escherichia coli, Enterococcus faecalis, Homo sapiens, Lacticaseibacillus casei, Mus musculus
Kalman, T.I.
On the mechanism of the reaction catalyzed by thymidylate synthetase
Ann. N. Y. Acad. Sci.
186
166-167
1971
Lacticaseibacillus casei, Mus musculus
Danenberg, P.V.; Langenbach, R.J.; Heidelberger, C.
Purification of thymidylate synthetase from L. casei by affinity chromatography
Biochem. Biophys. Res. Commun.
49
1029-1033
1972
Lacticaseibacillus casei, Mus musculus
Gupta, V.S.; Meldrum, J.B.
Purification and properties of thymidylate synthetase from pig thymus
Can. J. Biochem.
50
353-362
1972
Sus scrofa
-
Horinishi, H.; Greenberg, D.M.
Purification and properties of thymidylate synthase from calf thymus
Biochim. Biophys. Acta
258
741-752
1972
Escherichia phage T2, Enterobacteria phage T6, Bos taurus, Gallus gallus, Escherichia coli, Enterococcus faecalis, Lacticaseibacillus casei, Mus musculus
Loeble, R.B.; Dunlap, R.B.
Characterization of the subunits of thymidylate synthetase
Biochem. Biophys. Res. Commun.
49
1671-1677
1972
Homo sapiens, Lacticaseibacillus casei
Santi, D.V.; Sakai, T.T.
Irreversible inhibition of thymidylate synthetase by 5-formyl-2-deoxyuridylic acid
Biochem. Biophys. Res. Commun.
46
1320-1325
1972
Escherichia coli, Lacticaseibacillus casei, Mus musculus, Escherichia coli B / ATCC 11303
Capco, G.R.; Krupp, J.R.; Mathews, C.K.
Bacteriophage-coded thymidylate synthetase: characteristics of the T4 and T5 enzymes
Arch. Biochem. Biophys.
158
726-735
1973
Tequatrovirus T4, Tequintavirus T5, Lacticaseibacillus casei
Carpenter, N.J.
Properties and inhibition of thymidylate synthetase in Drosophila melanogaster
J. Insect Physiol.
20
1389-1401
1974
Drosophila melanogaster
Danenberg, P.V.; Heidelberger, C.
Purification of thymidylate synthetase with 2'-deoxyuridylate-agarose
Methods Enzymol.
34 B
520-523
1974
Lacticaseibacillus casei, Mus musculus
-
Galivan, J.; Maley, G.F.; Maley, F.
Purification and properties of T2 bacteriophage-induced thymidylate synthetase
Biochemistry
13
2282-2289
1974
Escherichia phage T2, Tequatrovirus T4, Enterobacteria phage T6, Bos taurus, Escherichia coli, Lacticaseibacillus casei, Mus musculus, Rattus norvegicus
Kisliuk, R.L.; Gaumont, Y.
Polyglutamyl derivatives of folate as substrates and inhibitors of thymidylate synthetase
J. Biol. Chem.
249
4100-4103
1974
Lacticaseibacillus casei
Friedkin, M.; Plante, L.T.; Crawford, E.J.; Crumm, M.
Inhibition of thymidylate synthetase and dihydrofolate reductase by naturally occurring oligoglutamate derivatives of folic acid
J. Biol. Chem.
250
5614-5621
1975
Escherichia coli, Escherichia coli B / ATCC 11303
McCuen, R.W.; Sirotnak, F.M.
Thymidylate synthetase from Diplococcus pneumoniae, properties and inhibition by folate analogs
Biochim. Biophys. Acta
384
369-380
1975
Gallus gallus, Streptococcus pneumoniae, Escherichia coli, Enterococcus faecium, Lacticaseibacillus casei, Escherichia coli B / ATCC 11303
Slavik, K.; Rode, W.; Slavikova, V.
Purification of thymidylate synthetase from enzyme-poor sources by affinity chromatography
Biochemistry
15
4222-4227
1976
Bos taurus, Escherichia coli, Mus musculus, Escherichia coli B / ATCC 11303
Al Chalabi, K.; Gutteridge, W.E.
Presence and properties of thymidylate synthase in trypanosomatids
Biochim. Biophys. Acta
481
71-79
1977
Crithidia fasciculata, Strigomonas oncopelti, Escherichia coli, Rattus norvegicus, Trypanosoma brucei, Trypanosoma brucei gambiense, Trypanosoma congolense, Trypanosoma cruzi, Trypanosoma lewisi, Trypanosoma rhodesiense
Danenberg, P.V.
Thymidylate synthetase - a target enzyme in cancer chemotherapy
Biochim. Biophys. Acta
473
73-92
1977
Streptococcus pneumoniae, Escherichia coli, Enterococcus faecalis, Homo sapiens, Lacticaseibacillus casei, Mus musculus, Escherichia coli B / ATCC 11303
Dolnick, B.J.; Cheng, Y.C.
Human thymidylate synthetase. II. Derivatives of pteroylmono- and -polyglutamates as substrates and inhibitors
J. Biol. Chem.
253
3563-3567
1978
Escherichia coli, Homo sapiens, Lacticaseibacillus casei, Escherichia coli B / ATCC 11303, Escherichia coli R2
Dunlap, R.B.
TMP synthetase from Lactobacillus casei
Methods Enzymol.
51
90-97
1978
Lacticaseibacillus casei
Mertes, M.P.; Chang, C.T.C.; de Clercq, E.; Huang, G.F.; Torrence, P.F.
5-Nitro-2-deoxyuridine 5-monophosphate is a potent irreversible inhibitor of Lactobacillus caesi thymidylate synthetase
Biochem. Biophys. Res. Commun.
84
1054-1059
1978
Lacticaseibacillus casei
Whiteley, J.M.
5-Fluoro-2-deoxyuridylate-agarose in the affinity-chromatographic purification of thymidylate synthetase
Methods Enzymol.
51
98-104
1978
Lacticaseibacillus casei
Haertle, T.; Wohlrab, F.; Guschlbauer, W.
Thymidylate synthetase from Escherichia coli K12. Purification, and dependence of kinetic properties on sugar conformation and size of the 2 substituent
Eur. J. Biochem.
102
223-230
1979
Escherichia phage T2, Streptococcus pneumoniae, Escherichia coli, Lacticaseibacillus casei, Escherichia coli B / ATCC 11303, Escherichia coli EM 20031 K12
Lockshin, A.; Moran, R.G.; Danenberg, P.V.
Thymidylate synthetase purified to homogeneity from human leukemic cells
Proc. Natl. Acad. Sci. USA
76
750-754
1979
Escherichia phage T2, Bos taurus, Escherichia coli, Homo sapiens, Lacticaseibacillus casei
Rode, W.; Scanlon, K.J.; Hynes, J.; Bertino, J.R.
Purification of mammalian tumor (L1210) thymidylate synthetase by affinity chromatography on stable biospecific adsorbent. Stabilization of the enzyme with neutral detergents
J. Biol. Chem.
254
11538-11543
1979
Escherichia coli, Homo sapiens, Lacticaseibacillus casei, Mus musculus
Slavik, K.; Slavikova, V.
Purification of thymidylate synthetase from enzyme-poor sources by affinity chromatography
Methods Enzymol.
66
709-723
1980
Bos taurus, Escherichia coli, Lacticaseibacillus casei, Mus musculus, Escherichia coli B / ATCC 11303
Bisson, L.F.; Thorner, J.
Thymidylate synthetase from Saccharomyces cerevisiae. Purification and enzymic properties
J. Biol. Chem.
256
12456-12462
1981
Saccharomyces cerevisiae, Gallus gallus, Enterococcus faecalis, Homo sapiens, Lacticaseibacillus casei, Mus musculus
Kalman, T.I.; Goldman, D.
Inactivation of thymidylate synthetase by a novel mechanism-based enzyme inhibitor: 1-(beta-D-2-deoxyribofuranosyl) 8-azapurin-2-one 5-monophosphate
Biochem. Biophys. Res. Commun.
102
682-689
1981
Lacticaseibacillus casei
Priest, D.G.; Doig, M.T.; Hynes, J.B.
Purification of mouse liver thymidylate synthetase by affinity chromatography using 10-methyl-5,8-dideazafolate as the affinant
Experientia
37
119-120
1981
Mus musculus
Banerjee, C.K.; Bennett, L.L.; Brockman, R.W.; Sani, B.P.; Temple, C.
A convenient procedure for purification of thymidylate synthase from L1210 cells
Anal. Biochem.
121
275-280
1982
Gallus gallus, Homo sapiens, Lacticaseibacillus casei, Mus musculus
Belfort, M.; Moelleken, A.; Maley, G.F.; Maley, F.
Purification and properties of T4 phage thymidylate synthetase produced by the cloned gene in an amplification vector
J. Biol. Chem.
258
2045-2051
1983
Bacillus subtilis, Escherichia phage T2, Tequatrovirus T4, Escherichia coli, Lacticaseibacillus casei, Rattus norvegicus, Escherichia coli B / ATCC 11303
Pattanakitsakul, S.N.; Ruenwongsa, P.
Characterization of thymidylate synthetase and dihydrofolate reductase from Plasmodium berghei
Int. J. Parasitol.
14
513-520
1984
Crithidia fasciculata, Streptococcus pneumoniae, Escherichia coli, Homo sapiens, Lacticaseibacillus casei, Leishmania major, Plasmodium berghei
Kanai, F.; Kaneko, T.; Morishima, H.; Isshiki, K.; Takita, T.; Takeuchi, T.; Umezawa, H.
Vanoxonin, a new inhibitor of thymidylate synthetase. III. Inhibition of thymidylate synthetase by vanoxonin-vanadium complex
J. Antibiot.
38
39-50
1985
Mus musculus
Sani, B.P.; Vaid, A.; Cory, J.G.; Brockman, R.W.; Elliott, R.D.; Montgomery, J.A.
5-Haloacetamido-5-deoxythymidines: novel inhibitors of thymidylate synthase
Biochim. Biophys. Acta
881
175-184
1986
Mus musculus
Nakata, R.; Tsukamoto, I.; Miyoshi, M.; Kojo, S.
Purification and characterization of thymidylate synthetase from rat regenerating liver
Biochim. Biophys. Acta
924
297-302
1987
Saccharomyces cerevisiae, Homo sapiens, Lacticaseibacillus casei, Mus musculus, Rattus norvegicus, Rattus norvegicus Wistar
Nielsen, E.; Cella, R.
Thymidylate synthase in plant cells: Kinetic and molecular properties of the enzyme from Daucus carota L. cell cultures
Plant Cell Physiol.
29
503-508
1988
Daucus carota
-
Radparvar, S.; Houghton, P.J.; Houghton, J.A.
Characteristics of thymidylate synthase purified from a human colon adenocarcinoma
Arch. Biochem. Biophys.
260
342-350
1988
Homo sapiens, Sus scrofa
Chen, S.C.; Daron, H.H.; Aull, J.L.
Inhibition of thymidylate synthase by pyridoxal phosphate
Int. J. Biochem.
21
1217-1221
1989
Lacticaseibacillus casei
Matthews, D.A.; Villafranca, J.E.; Janson, C.A.; Smith, W.W.; Welsh, K.; Freer, S.
Stereochemical mechanism of action for thymidylate synthase based on the X-ray structure of the covalent inhibitory ternary complex with 5-fluoro-2-deoxyuridylate and 5,10-methylenetetrahydrofolate
J. Mol. Biol.
214
937-948
1990
Escherichia coli, Lacticaseibacillus casei
Balinska, M.; Rhee, M.; Whiteley, J.M.; Priest, D.G.; Galivan, J.
Inhibition of mammalian thymidylate synthase by 10-formyltetrahydropteroylpolyglutamate
Arch. Biochem. Biophys.
284
219-222
1991
Homo sapiens, Mus musculus, Rattus norvegicus
Bures, A.K.; Daron, H.H.; Aull, J.L.
Inhibition of thymidylate synthase by glyceraldehyde 3-phosphate
Int. J. Biochem.
23
733-736
1991
Lacticaseibacillus casei
Zhang, H.; Cisneros, R.J.; Deng, W.; Zapf, J.W.; Johnson, L.F.; Dunlap, R.B.
Purification and characterization of recombinant mouse thymidylate synthase
Biochim. Biophys. Acta
1077
35-46
1991
Homo sapiens, Lacticaseibacillus casei, Mus musculus
Chen, D.H.; Daron, H.H.; Aull, J.L.
1-Phenyl-3-trimethylaminopropyl carbodiimide: a new inhibitor of thymidylate synthase
J. Enzyme Inhib.
5
259-268
1992
Lacticaseibacillus casei
Galova, M.; Koptidesova, D.; Rusznakova, D.; Racay, P.; Kollarova, M.
Characteristics of NADPH-dependent thymidylate synthetase purified from Streptomyces aureofaciens
Arch. Biochem. Biophys.
296
81-87
1992
Bos taurus, Crithidia fasciculata, Escherichia coli, Kitasatospora aureofaciens, Mus musculus, Saccharomyces cerevisiae
Livi, L.L.; Edman, U.; Schneider, G.P.; Greene, P.J.; Santi, D.V.
Cloning, expression and characterization of thymidylate synthase from Cryptococcus neoformans
Gene
150
221-226
1994
Tequatrovirus T4, Candida albicans, Homo sapiens, Lacticaseibacillus casei, Mus musculus, Pneumocystis carinii, Cryptococcus neoformans (P0CS13), Cryptococcus neoformans, Cryptococcus neoformans B-3501A (P0CS13)
So, N.N.C.; Wong, P.C.L.; Ko, R.C.
Angiostrongylus cantonensis: Characterization of thymidylate synthetase
Exp. Parasitol.
79
526-535
1994
Aedes aegypti, Angiostrongylus cantonensis, Bos taurus, Saccharomyces cerevisiae, Brugia pahangi, Candida albicans, Gallus gallus, Crithidia fasciculata, Homo sapiens, Leishmania major, Mus musculus, Plasmodium falciparum, Rattus norvegicus, Sus scrofa, Toxoplasma gondii
Garcia-Fuentes, L.; Reche, P.; Lopez-Mayorga, O.; Santi, D.V.; Gonzalez-Pacanowska, D.; Baron, C.
Thermodynamic analysis of the binding of 5-fluoro-2'-deoxyuridine 5'-monophosphate to thymidylate synthase over a range of temperatures
Eur. J. Biochem.
232
641-645
1995
Escherichia coli, Lacticaseibacillus casei
Maley, F.; Pedersen-Lane, J.; Changchien, L.
Complete restoration of activity to inactive mutants of Escherichia coli thymidylate synthase: Evidence that E. coli thymidylate synthase is a half-the-sites activity enzyme
Biochemistry
34
1469-1474
1995
Escherichia coli, Lacticaseibacillus casei
Schiffer, C.A.; Clifton, I.J.; Davisson, V.J.; Santi, D.V.; Stroud, R.M.
Crystal structure of human thymidylate synthase: a structural mechanism for guiding substrates into the active site
Biochemistry
34
16279-16287
1995
Homo sapiens
Voeller, D.M.; Changchien, L.M.; Maley, G.F.; Maley, F.; Takechi, T.; Turner, R.E.; Montfort, W.R.; Allegra, C.J.; Chu, E.
Characterization of a specific interaction between Escherichia coli thymidylate synthase and Escherichia coli thymidylate synthase mRNA
Nucleic Acids Res.
23
869-875
1995
Tequatrovirus T4, Escherichia coli, Enterococcus faecium, Homo sapiens
Cho, S.W.; Lee, J.; Cho, E.H.
Effects of mutation at arginine-218 residue on the reaction of synthetic thymidylate synthase and 5-fluorouracil
Exp. Mol. Med.
28
77-83
1996
Tequatrovirus T4, Escherichia coli, Lacticaseibacillus casei, Plasmodium falciparum
-
Finer-Moore, J.S.; Liu, L.; Schafmeister, C.E.; Birdsall, D.L.; Mau, T.; Santi, D.V.; Stroud, R.M.
Partitioning roles of side chains in affinity, orientation, and catalysis with structures for mutant complexes: Asparagine-229 in thymidylate synthase
Biochemistry
35
5125-5136
1996
Lacticaseibacillus casei, Lacticaseibacillus casei TS N229D
Gokhale, R.S.; Agarwalla, S.; Santi, D.V.; Balaram, P.
Covalent reinforcement of a fragile region in the dimeric enzyme thymidylate synthase stabilizes the protein against chaotrope-induced unfolding
Biochemistry
35
7150-7158
1996
Tequatrovirus T4, Lacticaseibacillus casei
Hekmat-Nejad, M.; Rathod, P.K.
Kinetics of Plasmodium flaciparum thymidylate synthase: interactions with high-affinity metabolites of 5-fluoroorotate and D1694
Antimicrob. Agents Chemother.
40
1628-1632
1996
Crithidia fasciculata, Escherichia coli, Homo sapiens, Leishmania major, Mus musculus, Plasmodium berghei, Plasmodium falciparum, Plasmodium yoelii
Carlson, J.H.; Hill, S.A.
Identification and characterization of thymidylate synthase from Neisseria gonorrhoeae
FEMS Microbiol. Lett.
151
225-230
1997
Bacillus subtilis, Haemophilus influenzae, Neisseria gonorrhoeae, Neisseria gonorrhoeae MS11
Spencer, H.T.; Villafranca, J.E.; Appleman, J.R.
Kinetic scheme for thymidylate synthase from Escherichia coli: determination from measurements of ligand binding, primary and secondary isotope effects, and pre-steady-state catalysis
Biochemistry
36
4212-4222
1997
Tequatrovirus T4, Candida albicans, Escherichia coli, Homo sapiens, Lacticaseibacillus casei, Mus musculus
Chiericatti, G.; Santi, D.V.
Aspartate 221 of thymidylate synthase is involved in folate cofactor binding and in catalysis
Biochemistry
37
9038-9042
1998
Escherichia coli, Lacticaseibacillus casei
Liang, P.H.; Anderson, K.S.
Substrate channeling and domain-domain interactions in bifunctional thymidylate synthase-dihydrofolate reductase
Biochemistry
37
12195-12205
1998
Escherichia coli, Leishmania major, Toxoplasma gondii
Stout, T.J.; Schellenberger, U.; Santi, D.V.; Stroud, R.M.
Crystal structures of a unique thermal-stable thymidylate synthase from Bacillus subtilis
Biochemistry
37
14736-14747
1998
Bacillus phage phi3T, Bacillus subtilis (P0CI79), Bacillus subtilis, Escherichia coli (P0A884), Escherichia coli, Lacticaseibacillus casei, Lactococcus lactis
Tong, Y.; Liu-Chen, X.; Ercikan-Abali, E.A.; Capiaux, G.M.; Zhao, S.C.; Banerjee, D.; Bertino, J.R.
Isolation and characterization of Thymitaq (AG337) and 5-fluoro-2-deoxyuridylate-resistant mutants of human thymidylate synthase from ethyl methanesulfonate-exposed human sarcoma HT1080 cells
J. Biol. Chem.
273
11611-11618
1998
Escherichia coli, Homo sapiens, Lacticaseibacillus casei, Cryptococcus neoformans (P0CS13), Cryptococcus neoformans B-3501A (P0CS13)
Anderson, A.C.; O'Neil, R.H.; DeLano, W.L.; Stroud, R.M.
The structural mechanism for half-the-sites reactivity in an enzyme, thymidylate synthase, involves a relay of changes between subunits
Biochemistry
38
13829-13836
1999
Pneumocystis carinii (P13100), Pneumocystis carinii
Fox, K.M.; Maley, F.; Garibian, A.; Changchien, L.M.; Van Roey, P.
Crystal structure of thymidylate synthase A from Bacillus subtilis
Protein Sci.
8
538-544
1999
Bacillus subtilis, Escherichia coli
Mahdavian, E.; Spencer, H.T.; Dunlap, R.B.
Kinetic studies on drug-resistant variants of Escherichia coli thymidylate sythase: Functional effects of amino acid sunstitutions at residue 4
Arch. Biochem. Biophys.
368
257-264
1999
Escherichia coli, Homo sapiens
Steadman, D.J.; Spencer, H.T.; Dunlap, R.B.; Berger, S.H.
Substitution at residue 214 of human thymidylate synthase alters nucleotide binding and isomerization of ligand-protein complexes
Biochemistry
38
5582-5587
1999
Escherichia coli, Homo sapiens, Lacticaseibacillus casei
Anderson, A.C.; Perry, K.M.; Freymann, D.M.; Stroud, R.M.
The crystal structure of thymidylate synthase from Pneumocystis carinii reveals a fungal insert important for drug design
J. Mol. Biol.
297
645-657
2000
Pneumocystis carinii
Changchien, L.M.; Garibian, A.; Frasca, V.; Lobo, A.; Maley, G.F.; Maley, F.
High-Level expression of Escherichia coli and Bacillus subtilis thymidylate synthases
Protein Expr. Purif.
19
265-270
2000
Bacillus subtilis, Escherichia coli
Fantz, C.; Shaw, D.; Jennings, W.; Forsthoefel, A.; Kitchens, M.; Phan, J.; Minor, W.; Lebioda, L.; Berger, F.G.; Spencer, H.T.
Drug-resistant variants of Escherichia coli thymidylate synthase: effects of substitutions at Pro-254
Mol. Pharmacol.
57
359-366
2000
Homo sapiens, Mus musculus, Escherichia coli (P0A884), Escherichia coli
Felczak, K.; Miazga, A.; Poznanski, J.; Bretner, M.; Kulikowski, T.; Dzik, J.M.; Golos, B.; Zielinski, Z.; Ciesla, J.; Rode, W.
5-Substituted N4-hydroxy-2'-deoxycytidines and their 5'-monophosphates: Synthesis, conformation, interaction with tumor thymidylate synthase, and in vitro antitumor activity
J. Med. Chem.
43
4647-4656
2000
Lacticaseibacillus casei, Mus musculus, Rattus norvegicus, Trichinella spiralis
Jarmula, A.; Les, A.; Rode, W.
Different activities of 5-hydroxy-dUMP and 5-hydroxymethyl-dUMP in thymidylate synthase-catalyzed reaction in view of molecular modeling and structural studies
Bioorg. Chem.
28
156-162
2000
Homo sapiens
Phan, J.; Mahdavian, E.; Nivens, M.C.; Minor, W.; Berger, S.; Spencer, H.T.; Dunlap, R.B.; Lebioda, L.
Catalytic cysteine of thymidylate synthase is activated upon substrate binding
Biochemistry
39
6969-6978
2000
Homo sapiens, Lacticaseibacillus casei, Escherichia coli (P0A884), Escherichia coli
Golos, B.; Dzik, J.M.; Kazimierczuk, Z.; Ciesla, J.; Zielinski, Z.; Jankowska, J.; Kraszewski, A.; Stawinski, J.; Rode, W.; Shugar, D.
Interaction of thymidylate synthase with the 5'-thiophosphates, 5'-dithiophosphates, 5'-H-phosphonates and 5'-S-thiosulfates of 2'-deoxyuridine, thymidine and 5-fluoro-2'-deoxyuridine
Biol. Chem.
382
1439-1445
2001
Escherichia coli, Homo sapiens, Lacticaseibacillus casei, Mus musculus, Pneumocystis carinii, Rattus norvegicus, Trichinella pseudospiralis, Trichinella spiralis
Saxl, R.L.; Changchien, L.M.; Hardy, L.W.; Maley, F.
Parameters affecting the restoration of activity to inactive mutants of thymidylate synthase via subunit exchange: Further evidence that thymidylate synthase Is a half-of-the-sites activity enzyme
Biochemistry
40
5275-5282
2001
Escherichia coli, Lacticaseibacillus casei, Pneumocystis carinii
Fritz, T.A.; Liu, L.; Finer-Moore, J.S.; Stroud, R.M.
Tryptophan 80 and leucine 143 are critical for the hydride transfer step of thymidylate synthase by controlling active site access
Biochemistry
41
7021-7029
2002
Escherichia coli (P0A884), Escherichia coli
Kawate, H.; Landis, D.M.; Loeb, L.A.
Distribution of mutations in human thymidylate synthase yielding resistance to 5-fluorodeoxyuridine
J. Biol. Chem.
277
36304-36311
2002
Homo sapiens (P04818), Homo sapiens
Leduc, D.; Graziani, S.; Meslet-Cladiere, L.; Sodolescu, A.; Liebl, U.; Myllykallio, H.
Two distinct pathways for thymidylate (dTMP) synthesis in (hyper)thermophilic bacteria and archaea
Biochem. Soc. Trans.
32
231-235
2004
Archaeoglobus fulgidus, Methanothermobacter thermautotrophicus, Methanocaldococcus jannaschii, Methanopyrus kandleri, no activity in Aquifex aeolicus, no activity in Thermotoga maritima, no activity in Pyrococcus abyssi, no activity in Pyrobaculum aerophilum, no activity in Aeropyrum pernix, no activity in Sulfolobus solfataricus, no activity in Sulfolobus tokodaii, no activity in Pyrococcus horikoshii, no activity in Pyrococcus furiosus, no activity in Thermoplasma acidophilum, no activity in Thermoplasma volcanium
Dasgupta, T.; Anderson, K.S.
Probing the role of parasite-specific, distant structural regions on communication and catalysis in the bifunctional thymidylate synthase-dihydrofolate reductase from Plasmodium falciparum
Biochemistry
47
1336-1345
2008
Plasmodium falciparum (P13922), Plasmodium falciparum TM4/8.2 (P13922)
Gangjee, A.; Li, W.; Yang, J.; Kisliuk, R.L.
Design, synthesis, and biological evaluation of classical and nonclassical 2-amino-4-oxo-5-substituted-6-methylpyrrolo[3,2-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors
J. Med. Chem.
51
68-76
2008
Escherichia coli, Homo sapiens, Toxoplasma gondii
Kim, S.; Park, D.H.; Shim, J.
Thymidylate synthase and dihydropyrimidine dehydrogenase levels are associated with response to 5-fluorouracil in Caenorhabditis elegans
Mol. Cells
26
344-349
2008
Caenorhabditis elegans, Caenorhabditis elegans Bristol N2
Sienkiewicz, N.; Jaros?awski, S.; Wyllie, S.; Fairlamb, A.H.
Chemical and genetic validation of dihydrofolate reductase-thymidylate synthase as a drug target in African trypanosomes
Mol. Microbiol.
69
520-533
2008
Trypanosoma brucei
Aboge, G.O.; Jia, H.; Terkawi, M.A.; Goo, Y.K.; Nishikawa, Y.; Sunaga, F.; Namikawa, K.; Tsuji, N.; Igarashi, I.; Suzuki, H.; Fujisaki, K.; Xuan, X.
Cloning, expression and characterization of Babesia gibsoni dihydrofolate reductase-thymidylate synthase: inhibitory effect of antifolates on its catalytic activity and the parasite proliferation
Antimicrob. Agents Chemother.
52
4072-4080
2008
Babesia gibsoni, Babesia gibsoni (B5U9U8)
Lovelace, L.L.; Gibson, L.M.; Lebioda, L.
Cooperative inhibition of human thymidylate synthase by mixtures of active site binding and allosteric inhibitors
Biochemistry
46
2823-2830
2007
Homo sapiens, Homo sapiens (P04818)
Gibson, L.M.; Lovelace, L.L.; Lebioda, L.
The R163K mutant of human thymidylate synthase is stabilized in an active conformation: structural asymmetry and reactivity of cysteine 195
Biochemistry
47
4636-4643
2008
Homo sapiens (P04818), Homo sapiens
Giovannetti, E.; Backus, H.H.; Wouters, D.; Ferreira, C.G.; van Houten, V.M.; Brakenhoff, R.H.; Poupon, M.F.; Azzarello, A.; Pinedo, H.M.; Peters, G.J.
Changes in the status of p53 affect drug sensitivity to thymidylate synthase (TS) inhibitors by altering TS levels
Br. J. Cancer
96
769-775
2007
Homo sapiens
Clamp, A.R.; Schoeffski, P.; Valle, J.W.; Wilson, R.H.; Marreaud, S.; Govaerts, A.S.; Debois, M.; Lacombe, D.; Twelves, C.; Chick, J.; Jayson, G.C.; Jayson, G.C.
A phase I and pharmacokinetic study of OSI-7904L, a liposomal thymidylate synthase inhibitor in combination with oxaliplatin in patients with advanced colorectal cancer
Cancer Chemother. Pharmacol.
61
579-585
2008
Homo sapiens
Pillai, R.G.; Forster, M.; Perumal, M.; Mitchell, F.; Leyton, J.; Aibgirhio, F.I.; Golovko, O.; Jackman, A.L.; Aboagye, E.O.
Imaging pharmacodynamics of the alpha-folate receptor-targeted thymidylate synthase inhibitor BGC 945
Cancer Res.
68
3827-3834
2008
Homo sapiens
Chernyshev, A.; Fleischmann, T.; Koehn, E.M.; Lesley, S.A.; Kohen, A.
The relationships between oxidase and synthase activities of flavin dependent thymidylate synthase (FDTS)
Chem. Commun. (Camb. )
19
2861-2863
2007
Thermotoga maritima
Luo, Y.; Walla, M.; Wyatt, M.D.
Uracil incorporation into genomic DNA does not predict toxicity caused by chemotherapeutic inhibition of thymidylate synthase
DNA Repair
7
162-169
2008
Homo sapiens
Waldman, B.C.; Wang, Y.; Kilaru, K.; Yang, Z.; Bhasin, A.; Wyatt, M.D.; Waldman, A.S.
Induction of intrachromosomal homologous recombination in human cells by raltitrexed, an inhibitor of thymidylate synthase
DNA Repair
7
1624-1635
2008
Homo sapiens
Nief, N.; Le Morvan, V.; Robert, J.
Involvement of gene polymorphisms of thymidylate synthase in gene expression, protein activity and anticancer drug cytotoxicity using the NCI-60 panel
Eur. J. Cancer
43
955-962
2007
Homo sapiens
Jason, T.L.; Berg, R.W.; Vincent, M.D.; Koropatnick, J.
Antisense targeting of thymidylate synthase (TS) mRNA increases TS gene transcription and TS protein: effects on human tumor cell sensitivity to TS enzyme-inhibiting drugs
Gene Expr.
13
227-239
2007
Homo sapiens
Arvizu-Flores, A.A.; Sugich-Miranda, R.; Arreola, R.; Garcia-Orozco, K.D.; Velazquez-Contreras, E.F.; Montfort, W.R.; Maley, F.; Sotelo-Mundo, R.R.
Role of an invariant lysine residue in folate binding on Escherichia coli thymidylate synthase: calorimetric and crystallographic analysis of the K48Q mutant
Int. J. Biochem. Cell Biol.
40
2206-2217
2008
Escherichia coli (P0A884), Escherichia coli
Curtin, K.; Ulrich, C.M.; Samowitz, W.S.; Bigler, J.; Caan, B.; Potter, J.D.; Slattery, M.L.
Thymidylate synthase polymorphisms and colon cancer: associations with tumor stage, tumor characteristics and survival
Int. J. Cancer
120
2226-2232
2007
Homo sapiens
Gangjee, A.; Qiu, Y.; Li, W.; Kisliuk, R.L.
Potent dual thymidylate synthase and dihydrofolate reductase inhibitors: classical and nonclassical 2-amino-4-oxo-5-arylthio-substituted-6-methylthieno[2,3-d]pyrimidine antifolates
J. Med. Chem.
51
5789-5797
2008
Escherichia coli, Homo sapiens (P04818), Homo sapiens, Toxoplasma gondii
Okabe, T.; Okamoto, I.; Tsukioka, S.; Uchida, J.; Iwasa, T.; Yoshida, T.; Hatashita, E.; Yamada, Y.; Satoh, T.; Tamura, K.; Fukuoka, M.; Nakagawa, K.
Synergistic antitumor effect of S-1 and the epidermal growth factor receptor inhibitor gefitinib in non-small cell lung cancer cell lines: role of gefitinib-induced down-regulation of thymidylate synthase
Mol. Cancer Ther.
7
599-606
2008
Homo sapiens
Jung, W.S.; Shin, S.; Park, I.K.
Novobiocin inhibits the self-splicing of the primary transcripts of T4 phage thymidylate synthase gene
Mol. Cell. Biochem.
314
143-149
2008
Tequatrovirus T4
Codacci-Pisanelli, G.; Noordhuis, P.; van der Wilt, C.L.; Peters, G.J.
Selective protection by uridine of growth inhibition by 5-fluorouracil (5FU) mediated by 5FU incorporation into RNA, but not the thymidylate synthase mediated growth inhibition by 5FU-leucovorin
Nucleosides Nucleotides Nucleic Acids
27
733-739
2008
Homo sapiens, Mus musculus
Giovannetti, E.; Backus, H.H.; Wouters, D.; Peters, G.J.
Functional inactivity and mutations of p53 differentially affect sensitivity to 5-fluorouracil and antifolate inhibitors of thymidylate synthase (TS) by altering TS levels in colorectal cancer cells
Nucleosides Nucleotides Nucleic Acids
27
740-745
2008
Homo sapiens
Bijnsdorp, I.V.; Comijn, E.M.; Padron, J.M.; Gmeiner, W.H.; Peters, G.J.
Mechanisms of action of FdUMP[10]: metabolite activation and thymidylate synthase inhibition
Oncol. Rep.
18
287-291
2007
Mus musculus
Hunter, J.H.; Gujjar, R.; Pang, C.K.; Rathod, P.K.
Kinetics and ligand-binding preferences of Mycobacterium tuberculosis thymidylate synthases, ThyA and ThyX
PLoS ONE
3
e2237
2008
Mycobacterium tuberculosis, Mycobacterium tuberculosis (P9WFR9), Mycobacterium tuberculosis H37Rv (P9WFR9)
Yan, S.; Niu, R.; Wang, Z.; Lin, X.
In vitro selected peptides bind with thymidylate synthase mRNA and inhibit its translation
Sci. China C Life Sci.
50
630-636
2007
Homo sapiens
Giudice, S.; Benassi, L.; Bertazzoni, G.; Costi, M.P.; Gelain, A.; Venturelli, A.; Bernardi, C.; Gualdi, G.; Coppi, A.; Rossi, T.; Giannetti, A.; Magnoni, C.
New thymidylate synthase inhibitors induce apoptosis in melanoma cell lines
Toxicol. in Vitro
21
240-248
2007
Homo sapiens
Wang, Y.; Zhang, X.
Identification and characterization of a novel thymidylate synthase from deep-sea thermophilic bacteriophage Geobacillus virus E2
Virus Genes
37
218-224
2008
Geobacillus virus E2, Geobacillus virus E2 (A6M9A2)
Senkovich, O.; Schormann, N.; Chattopadhyay, D.
Structures of dihydrofolate reductase-thymidylate synthase of Trypanosoma cruzi in the folate-free state and in complex with two antifolate drugs, trimetrexate and methotrexate
Acta Crystallogr. Sect. D
65
704-716
2009
Trypanosoma cruzi (Q27793)
Chitnumsub, P.; Yuvaniyama, J.; Chahomchuen, T.; Vilaivan, T.; Yuthavong, Y.
Crystallization and preliminary crystallographic studies of dihydrofolate reductase-thymidylate synthase from Trypanosoma cruzi, the Chagas disease pathogen
Acta Crystallogr. Sect. F
65
1175-1178
2009
Trypanosoma cruzi
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
Jarmula, A.; Dowiercial, A.; Rode, W.
A molecular modeling study of the interaction of 2-fluoro-substituted analogues of dUMP/FdUMP with thymidylate synthase
Bioorg. Med. Chem. Lett.
18
2701-2708
2008
Escherichia coli (P0A884)
Showalter, S.L.; Showalter, T.N.; Witkiewicz, A.; Havens, R.; Kennedy, E.P.; Hucl, T.; Kern, S.E.; Yeo, C.J.; Brody, J.R.
Evaluating the drug-target relationship between thymidylate synthase expression and tumor response to 5-fluorouracil. Is it time to move forward?
Cancer Biol. Ther.
7
986-994
2008
Homo sapiens
Ferrari, S.; Losasso, V.; Costi, M.
Sequence-based identification of specific drug target regions in the thymidylate synthase enzyme family
ChemMedChem
3
392-401
2008
Acinetobacter baumannii, Aeromonas hydrophila, Ascaris suum, Aspergillus clavatus, Aspergillus fischeri, Aspergillus fumigatus, Aspergillus nidulans, Bacillus amyloliquefaciens, Bacillus anthracis, Bacillus cereus, Bacillus licheniformis, Bacillus mycoides, Bacteroides fragilis, Bacteroides thetaiotaomicron, Bartonella bacilliformis, Bartonella henselae, Bartonella quintana, Bordetella bronchiseptica, Bordetella parapertussis, Bordetella pertussis, Brucella abortus, Brucella melitensis, Brucella suis, Burkholderia ambifaria, Burkholderia dolosa, Burkholderia mallei, Burkholderia multivorans, Burkholderia pseudomallei, Burkholderia vietnamiensis, Candida albicans, Chaetomium globosum, Chromobacterium violaceum, Clostridioides difficile, Coccidioides immitis, Comamonas testosteroni, Corynebacterium diphtheriae, Corynebacterium jeikeium, Coxiella burnetii, Cryptococcus neoformans, Cryptosporidium hominis, Cryptosporidium parvum, Cutibacterium acnes, Debaryomyces hansenii, Encephalitozoon cuniculi, Enterobacter sp., Enterococcus faecalis, Enterococcus faecium, Francisella tularensis, Fusobacterium nucleatum, Haemophilus influenzae, Human alphaherpesvirus 1, Legionella pneumophila, Leishmania amazonensis, Leishmania braziliensis, Leishmania donovani, Leishmania infantum, Leishmania major, Leishmania tropica, Listeria monocytogenes, Malacoplasma penetrans, Mycobacterium avium, Mycobacterium leprae, Mycobacterium tuberculosis, Mycobacterium tuberculosis variant bovis, Mycobacterium ulcerans, Mycoplasma genitalium, Mycoplasma pneumoniae, Neisseria gonorrhoeae, Neisseria meningitidis, Nocardia farcinica, Novosphingobium aromaticivorans, Pasteurella multocida, Plasmodium falciparum (P13922), Plasmodium malariae, Plasmodium vivax, Pneumocystis carinii, Porphyromonas gingivalis, Pseudomonas aeruginosa, Pseudomonas mendocina, Salmonella enterica, Salmonella enterica subsp. enterica serovar Paratyphi A, Salmonella enterica subsp. enterica serovar Typhi, Salmonella enterica subsp. enterica serovar Typhimurium, Schistosoma japonicum, Serratia proteamaculans, Shewanella putrefaciens, Shigella boydii, Shigella dysenteriae, Shigella flexneri, Shigella sonnei, Staphylococcus aureus, Staphylococcus epidermidis, Staphylococcus haemolyticus, Staphylococcus saprophyticus, Stenotrophomonas maltophilia, Streptococcus agalactiae, Streptococcus mutans, Streptococcus pneumoniae, Streptococcus pyogenes, Streptococcus sanguinis, Toxoplasma gondii, Trichinella spiralis, Trypanosoma brucei, Trypanosoma cruzi, Vibrio alginolyticus, Vibrio cholerae serotype O1, Vibrio parahaemolyticus, Vibrio vulnificus, Yersinia bercovieri, Yersinia enterocolitica, Yersinia frederiksenii, Yersinia intermedia, Yersinia mollaretii, Yersinia pestis, Yersinia pseudotuberculosis, [Candida] glabrata, [Haemophilus] ducreyi
Monica, V.; Scagliotti, G.V.; Ceppi, P.; Righi, L.; Cambieri, A.; Lo Iacono, M.; Saviozzi, S.; Volante, M.; Novello, S.; Papotti, M.
Differential thymidylate synthase expression in different variants of large-cell carcinoma of the lung
Clin. Cancer Res.
15
7547-7552
2009
Homo sapiens
Arvizu-Flores, A.A.; Aispuro-Hernandez, E.; Garcia-Orozco, K.D.; Varela-Romero, A.; Valenzuela-Soto, E.; Velazquez-Contreras, E.F.; Rojo-Dominguez, A.; Yepiz-Plascencia, G.; Maley, F.; Sotelo-Mundo, R.R.
Functional identity of the active sites of crustacean and viral thymidylate synthases
Comp. Biochem. Physiol. C
150
406-413
2009
Penaeus vannamei (C6GJB8), Penaeus vannamei, Shrimp white spot syndrome virus (Q8QTF3)
Jason, T.L.; Figueredo, R.; Ferguson, P.J.; Vincent, M.D.; Berg, R.W.; Koropatnick, J.
ODN 491, a novel antisense oligodeoxynucleotide that targets thymidylate synthase, exerts cell-specific effects in human tumor cell lines
DNA Cell Biol.
27
229-240
2008
Homo sapiens
Bielas, J.H.; Schmitt, M.W.; Icreverzi, A.; Ericson, N.G.; Loeb, L.A.
Molecularly evolved thymidylate synthase inhibits 5-fluorodeoxyuridine toxicity in human hematopoietic cells
Hum. Gene Ther.
20
1703-1707
2009
Homo sapiens
Chatterjee, I.; Kriegeskorte, A.; Fischer, A.; Deiwick, S.; Theimann, N.; Proctor, R.; Peters, G.; Herrmann, M.; Kahl, B.
In vivo mutations of thymidylate synthase (encoded by thyA) are responsible for thymidine dependency in clinical small-colony variants of Staphylococcus aureus
J. Bacteriol.
190
834-842
2008
Staphylococcus aureus
Pena, M.M.; Melo, S.P.; Xing, Y.Y.; White, K.; Barbour, K.W.; Berger, F.G.
The intrinsically disordered N-terminal domain of thymidylate synthase targets the enzyme to the ubiquitin-independent proteasomal degradation pathway
J. Biol. Chem.
284
31597-31607
2009
Mus musculus
Gangjee, A.; Li, W.; Kisliuk, R.L.; Cody, V.; Pace, J.; Piraino, J.; Makin, J.
Design, synthesis, and X-ray crystal structure of classical and nonclassical 2-amino-4-oxo-5-substituted-6-ethylthieno[2,3-d]pyrimidines as dual thymidylate synthase and dihydrofolate reductase inhibitors and as potential antitumor agents
J. Med. Chem.
52
4892-4902
2009
Escherichia coli, Homo sapiens, Toxoplasma gondii
Kanaan, N.; Marti, S.; Moliner, V.; Kohen, A.
QM/MM study of thymidylate synthase: Enzymatic motions and the temperature dependence of the rate limiting step (dagger)
J. Phys. Chem. A
113
2176-2182
2009
Escherichia coli
Leclerc, G.J.; Mou, C.; Leclerc, G.M.; Mian, A.M.; Barredo, J.C.
Histone deacetylase inhibitors induce FPGS mRNA expression and intracellular accumulation of long-chain methotrexate polyglutamates in childhood acute lymphoblastic leukemia: implications for combination therapy
Leukemia
24
552-562
2010
Homo sapiens
Lovelace, L.L.; Johnson, S.R.; Gibson, L.M.; Bell, B.J.; Berger, S.H.; Lebioda, L.
Variants of human thymidylate synthase with loop 181-197 stabilized in the inactive conformation
Protein Sci.
18
1628-1636
2009
Homo sapiens (P04818), Homo sapiens
Arvizu-Flores, A.; Velazquez-Contreras, E.; Machi, L.; Arreola, R.; Maley, F.; Sotelo-Mundo, R.
Spectroscopic analysis of folate binding to thymidylate synthase active site
Spectrosc. Lett.
42
142-146
2009
Escherichia coli
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Gangjee, A.; Jain, H.D.; Phan, J.; Guo, X.; Queener, S.F.; Kisliuk, R.L.
2,4-Diamino-5-methyl-6-substituted arylthio-furo[2,3-d]pyrimidines as novel classical and nonclassical antifolates as potential dual thymidylate synthase and dihydrofolate reductase inhibitors
Bioorg. Med. Chem.
18
953-961
2010
Escherichia coli, Homo sapiens, Toxoplasma gondii
Huang, X.; Gibson, L.M.; Bell, B.J.; Lovelace, L.L.; Pena, M.M.; Berger, F.G.; Berger, S.H.; Lebioda, L.
Replacement of Val3 in human thymidylate synthase affects its kinetic properties and intracellular stability
Biochemistry
49
2475-2482
2010
Homo sapiens
Kan, S.C.; Liu, J.S.; Hu, H.Y.; Chang, C.M.; Lin, W.D.; Wang, W.C.; Hsu, W.H.
Biochemical characterization of two thymidylate synthases in Corynebacterium glutamicum NCHU 87078
Biochim. Biophys. Acta
1804
1751-1759
2010
Corynebacterium glutamicum, Corynebacterium glutamicum NCHU 87078
Jarmula, A.; Fraczyk, T.; Cieplak, P.; Rode, W.
Mechanism of influence of phosphorylation on serine 124 on a decrease of catalytic activity of human thymidylate synthase
Bioorg. Med. Chem.
18
3361-3370
2010
Homo sapiens
Park, M.; Cho, S.; Lee, H.; Sibley, C.H.; Rhie, H.
Alternative thymidylate synthase, ThyX, involved in Corynebacterium glutamicum ATCC 13032 survival during stationary growth phase
FEMS Microbiol. Lett.
307
128-134
2010
Corynebacterium glutamicum, Corynebacterium glutamicum ATCC 13032
Wang, Z.; Kohen, A.
Thymidylate synthase catalyzed H-transfers: two chapters in one tale
J. Am. Chem. Soc.
132
9820-9825
2010
Homo sapiens
Chanama, M.; Chanama, S.; Shaw, P.J.; Chitnumsub, P.; Leartsakulpanich, U.; Yuthavong, Y.
Formation of catalytically active cross-species heterodimers of thymidylate synthase from Plasmodium falciparum and Plasmodium vivax
Mol. Biol. Rep.
38
1029-1037
2011
Plasmodium falciparum, Plasmodium vivax
Zhang, Y.; Yang, S.; Liu, M.; Song, C.; Wu, N.; Ling, P.; Chu, E.; Lin, X.
Interaction between thymidylate synthase and its cognate mRNA in zebrafish embryos
PLoS ONE
5
e10618
2010
Danio rerio
Cardinale, D.; Salo-Ahen, O.; Guaitoli, G.; Ferrari, S.; Venturelli, A.; Franchini, S.; Battini, R.; Ponterini, G.; Wade, R.; Costi, M.
Design and characterization of a mutation outside the active site of human thymidylate synthase that affects ligand binding
Protein Eng.
23
81-89
2010
Homo sapiens
Zhang, X.; Zhang, J.; Guo, G.; Mao, X.; Hu, Y.; Zou, Q.
Crystal structure of a flavin-dependent thymidylate synthase from Helicobacter pylori strain 26695
Protein Pept. Lett.
19
1225-1230
2012
Helicobacter pylori (O26061)
Wang, K.; Wang, Q.; Chen, J.; Chen, L.; Jiang, H.; Shen, X.
Crystal structure and enzymatic characterization of thymidylate synthase X from Helicobacter pylori strain SS1
Protein Sci.
20
1398-1410
2011
Helicobacter pylori, Helicobacter pylori SS1
Luo, B.; Repalli, J.; Yousef, A.M.; Johnson, S.R.; Lebioda, L.; Berger, S.H.
Human thymidylate synthase with loop 181-197 stabilized in an inactive conformation: ligand interactions, phosphorylation, and inhibition profiles
Protein Sci.
20
87-94
2011
Homo sapiens
Islam, Z.; Strutzenberg, T.S.; Ghosh, A.K.; Kohen, A.
Activation of two sequential H-transfers in the thymidylate synthase catalyzed reaction
ACS Catal.
5
6061-6068
2015
Escherichia coli (P0A884), Escherichia coli
Dowiercial, A.; Wilk, P.; Rypniewski, W.; Rode, W.; Jarmula, A.
Crystal structure of mouse thymidylate synthase in tertiary complex with dUMP and raltitrexed reveals N-terminus architecture and two different active site conformations
BioMed Res. Int.
2014
945803
2014
Mus musculus (P07607), Mus musculus
Osorio, E.; Aguilera, C.; Naranjo, N.; Marin, M.; Muskus, C.
Biochemical characterization of the bifunctional enzyme dihydrofolate reductase-thymidylate synthase from Leishmania (Viannia) and its evaluation as a drug target
Biomedica
33
393-401
2014
Leishmania braziliensis (A4H4P8), Leishmania braziliensis
Kumar, V.P.; Cisneros, J.A.; Frey, K.M.; Castellanos-Gonzalez, A.; Wang, Y.; Gangjee, A.; White, A.C.; Jorgensen, W.L.; Anderson, K.S.
Structural studies provide clues for analog design of specific inhibitors of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase
Bioorg. Med. Chem. Lett.
24
4158-4161
2014
Cryptosporidium hominis
Cannazza, G.; Cazzato, A.S.; Marraccini, C.; Pavesi, G.; Pirondi, S.; Guerrini, R.; Pela, M.; Frassineti, C.; Ferrari, S.; Marverti, G.; Ponterini, G.; Costi, M.P.
Internalization and stability of a thymidylate synthase peptide inhibitor in ovarian cancer cells
J. Med. Chem.
57
10551-10556
2014
Homo sapiens
Swiderek, K.; Kohen, A.; Moliner, V.
The influence of active site conformations on the hydride transfer step of the thymidylate synthase reaction mechanism
Phys. Chem. Chem. Phys.
17
30793-30804
2015
Escherichia coli (P0A884)
Sharma, H.; Landau, M.; Vargo, M.; Spasov, K.; Anderson, K.
First three-dimensional structure of Toxoplasma gondii thymidylate synthase-dihydrofolate reductase Insights for catalysis, interdomain interactions, and substrate channeling
Biochemistry
52
7305-7317
2013
Toxoplasma gondii (Q07422), Toxoplasma gondii
Osorio, E.; Aguilera, C.; Naranjo, N.; Marin, M.; Muskus, C.
Biochemical characterization of the bifunctional enzyme dihydrofolate reductase-thymidylate synthase from Leishmania (Viannia) and its evaluation as a drug target
Biomedica
33
393-401
2013
Leishmania braziliensis (A4H4P8), Leishmania braziliensis, Trypanosoma cruzi (Q27793), Leishmania panamensis (S5M3K7)
Kumar, V.P.; Cisneros, J.A.; Frey, K.M.; Castellanos-Gonzalez, A.; Wang, Y.; Gangjee, A.; White, A.C.; Jorgensen, W.L.; Anderson, K.S.
Structural studies provide clues for analog design of specific inhibitors of Cryptosporidium hominis thymidylate synthase-dihydrofolate reductase
Bioorg. Med. Chem. Lett.
24
4158-4161
2014
Cryptosporidium hominis (A0A0S4TER9), Cryptosporidium hominis
Gibson, M.W.; Dewar, S.; Ong, H.B.; Sienkiewicz, N.; Fairlamb, A.H.
Trypanosoma brucei DHFR-TS revisited characterisation of a bifunctional and highly unstable recombinant dihydrofolate reductase-thymidylate synthase
PLoS Negl. Trop. Dis.
10
e0004714
2016
Trypanosoma brucei (Q27783), Trypanosoma brucei 427 (Q27783)
Wang, N.; McCammon, J.A.
Substrate channeling between the human dihydrofolate reductase and thymidylate synthase
Protein Sci.
25
79-86
2016
Homo sapiens (P04818), Homo sapiens
Deschamps, P.; Rety, S.; Bareille, J.; Leulliot, N.
Crystal structure of the active form of native human thymidylate synthase in the absence of bound substrates
Acta Crystallogr. Sect. F
73
336-341
2017
Homo sapiens (P04818), Homo sapiens
Sobich, J.; Prokopowicz, M.; Maj, P.; Wilk, P.; Zielinski, Z.; Fraczyk, T.; Rode, W.
Thymidylate synthase-catalyzed, tetrahydrofolate-dependent self-inactivation by 5-FdUMP
Arch. Biochem. Biophys.
674
108106
2019
Mus musculus (P07607), Mus musculus
Sapienza, P.J.; Popov, K.I.; Mowrey, D.D.; Falk, B.T.; Dokholyan, N.V.; Lee, A.L.
Inter-active site communication mediated by the dimer interface beta-sheet in the half-the-sites enzyme, thymidylate synthase
Biochemistry
58
3302-3313
2019
Escherichia coli (P0A884)
Amin, L.H.T.; Shawer, T.Z.; El-Naggar, A.M.; El-Sehrawi, H.M.A.
Design, synthesis, anticancer evaluation and docking studies of new pyrimidine derivatives as potent thymidylate synthase inhibitors
Bioorg. Chem.
91
103159
2019
Homo sapiens (P04818)
Catalano, A.; Luciani, R.; Carocci, A.; Cortesi, D.; Pozzi, C.; Borsari, C.; Ferrari, S.; Mangani, S.
X-ray crystal structures of Enterococcus faecalis thymidylate synthase with folate binding site inhibitors
Eur. J. Med. Chem.
123
649-664
2016
Enterococcus faecalis (Q834R3), Enterococcus faecalis, Enterococcus faecalis ATCC 700802 (Q834R3)
Li, X.Y.; Liang, J.W.; Mohamed O, K.; Zhang, T.J.; Lu, G.Q.; Meng, F.H.
Design, synthesis and biological evaluation of N-phenyl-(2,4-dihydroxypyrimidine-5-sulfonamido)benzoyl hydrazide derivatives as thymidylate synthase (TS) inhibitors and as potential antitumor drugs
Eur. J. Med. Chem.
154
267-279
2018
Homo sapiens (P04818)
Lu, G.Q.; Li, X.Y.; Mohamed O, K.; Wang, D.; Meng, F.H.
Design, synthesis and biological evaluation of novel uracil derivatives bearing 1, 2, 3-triazole moiety as thymidylate synthase (TS) inhibitors and as potential antitumor drugs
Eur. J. Med. Chem.
171
282-296
2019
Homo sapiens (P04818)
Czyzyk, D.J.; Valhondo, M.; Deiana, L.; Tirado-Rives, J.; Jorgensen, W.L.; Anderson, K.S.
Structure activity relationship towards design of Cryptosporidium specific thymidylate synthase inhibitors
Eur. J. Med. Chem.
183
111673
2019
Cryptosporidium hominis (A0A2Z1FET6), Cryptosporidium hominis
Sapienza, P.J.; Falk, B.T.; Lee, A.L.
Bacterial thymidylate synthase binds two molecules of substrate and cofactor without cooperativity
J. Am. Chem. Soc.
137
14260-14263
2015
Escherichia coli
Heble, N.; Mavillapalli, R.; Selvaraj, R.; Jeyabalan, S.
Molecular docking studies of phytoconstituents identified in Crocus sativus, Curcuma longa, Cassia occidentalis and Moringa oleifera on thymidylate synthase - An enzyme target for anti-cancer activity
J. Appl. Pharm. Sci.
6
131-135
2016
Homo sapiens (P04818)
-
Chen, D.; Jansson, A.; Sim, D.; Larsson, A.; Nordlund, P.
Structural analyses of human thymidylate synthase reveal a site that may control conformational switching between active and inactive states
J. Biol. Chem.
292
13449-13458
2017
Homo sapiens (P04818), Homo sapiens
Antosiewicz, A.; Jarmula, A.; Przybylska, D.; Mosieniak, G.; Szczepanowska, J.; Kowalkowska, A.; Rode, W.; Ciesla, J.
Human dihydrofolate reductase and thymidylate synthase form a complex in vitro and co-localize in normal and cancer cells
J. Biomol. Struct. Dyn.
35
1474-1490
2017
Homo sapiens (P04818), Homo sapiens
Tochowicz, A.; Santucci, M.; Saxena, P.; Guaitoli, G.; Trande, M.; Finer-Moore, J.; Stroud, R.; Costi, M.
Alanine mutants of the interface residues of human thymidylate synthase decode key features of the binding mode of allosteric anticancer peptides
J. Med. Chem.
58
1012-1018
2015
Homo sapiens (P04818), Homo sapiens
Islam, Z.; Gurevic, I.; Strutzenberg, T.S.; Ghosh, A.K.; Iqbal, T.; Kohen, A.
Bacterial versus human thymidylate synthase Kinetics and functionality
PLoS ONE
13
e0196506
2018
Homo sapiens (P04818), Homo sapiens
Dowiercial, A.; Jarmula, A.; Wilk, P.; Rypniewski, W.; Kowalska, M.; Fraczyk, T.; Ciesla, J.; Rode, W.
Mouse thymidylate synthase does not show the inactive conformation, observed for the human enzyme
Struct. Chem.
28
667-674
2017
Mus musculus (P07607)
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