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(+/-)-methyl 5-[3-(6-amino-5-cyano-4-isopropyl-3-methyl-1,4-dihydropyrano[2,3-c]pyrazol-4-yl)-5-cyanophenyl]thiophene-2-carboxylate
-
-
(4R)-6-amino-4-(5-cyano-3'-fluoro[1,1'-biphenyl]-3-yl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
(4R,4S)-5-cyano-4-(3-cyano-5-[5-[((S)-1,3-dicarboxypropyl)-carbamoyl]thiophen-2-yl]phenyl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-6-aminium trifluoroacetate
(4S)-6-amino-4-(5-cyano-3'-fluoro[1,1'-biphenyl]-3-yl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
2-mercaptopropionic acid
-
-
3'-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5'-cyano[1,1'-biphenyl]-3-carboxylic acid
3-Bromopyruvate
isoform SHMT1 is completely inhibited by 3-bromopyruvate; isoform SHMT2 retains a significant fraction of activity with 3-bromopyruvate
5,10-methenyltetrahydrofolate
-
-
5,10-methylene-5,6,7,8-tetrahydrofolic acid
-
-
5,5-dithiobis(2-nitrobenzoic acid)
5-formyltetrahydrofolate
-
can inhibit SHMT in vivo and thereby influence glycine pool size, can accumulate glycine in both wild-type and 5-CHO-THF cycloligase mutant
5-formyltetrahydrofolate monoglutamate
5-methyl-5,6,7,8-tetrahydrofolate
-
-
5-methyltetrahydrofolate monoglutamate
5-Methyltetrahydrofolate triglutamate
5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]-N,N-dimethylthiophene-2-carboxamide
5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]-N-[3-(diethylamino)propyl]thiophene-2-carboxamide
5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylic acid
6-amino-3-methyl-4-[3-(morpholin-4-yl)-5-(trifluoromethyl)phenyl]-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
6-amino-4-(3,5-dichlorophenyl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
6-amino-4-(5-cyano-3'-fluoro[1,1'-biphenyl]-3-yl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
6-amino-4-[3-cyano-5-(piperazin-1-yl)phenyl]-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitril
-
-
6-amino-4-[3-cyano-5-(piperazin-1-yl)phenyl]-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
6-amino-5-cyano-4-[3-cyano-5-(5-[[3-(morpholin-4-ium-4-yl)propyl]carbamoyl]thiophen-2-yl)phenyl]-3-methyl-4-isopropyl-2,4-dihydropyrano[2,3-c]pyrazol-1-ium bis-(trifluoroacetate)
Antibodies to cytosolic enzyme
-
-
-
Antibodies to mitochondrial enzyme
-
no inhibition of cytosolic enzyme
-
benzyl 4-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]piperazine-1-carboxylate
benzyl 5-[3-[(4R)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
benzyl 5-[3-[(4S)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
benzyl 5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
beta-chloroalanine
-
suicide substrate
beta-trifluoroallothreonine
carboxymethoxylamine
-
strong
CO(NH2)2
60.59% residual activity at 1 mM
dithiothreitol
59.29% residual activity at 1 mM
ethyl 4-[[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl](methyl)amino]butanoate
guanidine hydrochloride
86% loss of activity at 0.25 M
L-alpha,beta-diaminopropionic acid
-
-
L-mimosine
-
inhibits SHMT1 transcription by chelating zinc, eliminates the metal regulatory element- and Sp1-binding activity in nuclear extracts from MCF-7 cells, but not in nuclear extracts from the mimosine-resistant cell line, MCF-7/2a
leucovorin
leucovorin (N5-CHO-THF) exhibits a differential inhibition pattern: it significantly inhibits the aldol cleavage of serine catalyzed by zebrafish cytosolic SHMT but it inhibits to a lesser extent the reaction catalyzed by the mitochondrial isozyme. Approximately 70% and 30% inhibition are observed for zebrafish cytosolic- and zebrafish mitochondrial SHMT activities, respectively, in the presence of 70 mM leucovorin. An even larger difference between both isoenzymes is observed when the inhibition is assayed in the presence of 50 mM serine; leucovorin (N5-CHO-THF) exhibits a differential inhibition pattern: it significantly inhibits the aldol cleavage of serine catalyzed by zebrafish cytosolic SHMT but it inhibits to a lesser extent the reaction catalyzed by the mitochondrial isozyme. Approximately 70% and 30% inhibition are observed for zebrafish cytosolic- and zebrafish mitochondrial SHMT activities, respectively, in the presence of 70 mM leucovorin. An even larger difference between both isoenzymes is observed when the inhibition is assayed in the presence of 50 mM serine
methyl 3'-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5'-chloro[1,1'-biphenyl]-4-carboxylate
methyl 5-[3-[(4R)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
methyl 5-[3-[(4S)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
methyl 5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
-
methyl methanethiosulfonate
nolatrexed
-
poor inhibition
phenylhydrazine
-
partially reversible by pyridoxal 5'-phosphate
S-adenosyl-L-methionine
-
-
substituted hydroxylamine derivates
-
sulfonyl fluoride triazine derivates
tetrahydrofolate derivatives
-
tetrahydropteroylglutamate
-
(4R)-6-amino-4-(5-cyano-3'-fluoro[1,1'-biphenyl]-3-yl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
-
(4R)-6-amino-4-(5-cyano-3'-fluoro[1,1'-biphenyl]-3-yl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
(4R,4S)-5-cyano-4-(3-cyano-5-[5-[((S)-1,3-dicarboxypropyl)-carbamoyl]thiophen-2-yl]phenyl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-6-aminium trifluoroacetate
-
-
(4R,4S)-5-cyano-4-(3-cyano-5-[5-[((S)-1,3-dicarboxypropyl)-carbamoyl]thiophen-2-yl]phenyl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-6-aminium trifluoroacetate
-
(4S)-6-amino-4-(5-cyano-3'-fluoro[1,1'-biphenyl]-3-yl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
-
(4S)-6-amino-4-(5-cyano-3'-fluoro[1,1'-biphenyl]-3-yl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
1,10-phenanthroline
-
-
3'-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5'-cyano[1,1'-biphenyl]-3-carboxylic acid
-
-
3'-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5'-cyano[1,1'-biphenyl]-3-carboxylic acid
-
4-chloro-L-threonine
-
-
5,5-dithiobis(2-nitrobenzoic acid)
-
-
5,5-dithiobis(2-nitrobenzoic acid)
-
-
5-formyltetrahydrofolate monoglutamate
-
-
5-formyltetrahydrofolate monoglutamate
-
-
5-methyltetrahydrofolate monoglutamate
-
-
5-methyltetrahydrofolate monoglutamate
-
-
5-Methyltetrahydrofolate triglutamate
-
-
5-Methyltetrahydrofolate triglutamate
-
-
5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]-N,N-dimethylthiophene-2-carboxamide
-
-
5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]-N,N-dimethylthiophene-2-carboxamide
-
5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]-N-[3-(diethylamino)propyl]thiophene-2-carboxamide
-
-
5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]-N-[3-(diethylamino)propyl]thiophene-2-carboxamide
-
5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylic acid
-
-
5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylic acid
-
6-amino-3-methyl-4-[3-(morpholin-4-yl)-5-(trifluoromethyl)phenyl]-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
-
6-amino-3-methyl-4-[3-(morpholin-4-yl)-5-(trifluoromethyl)phenyl]-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
6-amino-4-(3,5-dichlorophenyl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
-
6-amino-4-(3,5-dichlorophenyl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
6-amino-4-(5-cyano-3'-fluoro[1,1'-biphenyl]-3-yl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
-
6-amino-4-(5-cyano-3'-fluoro[1,1'-biphenyl]-3-yl)-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazole-5-carbonitrile
-
6-amino-5-cyano-4-[3-cyano-5-(5-[[3-(morpholin-4-ium-4-yl)propyl]carbamoyl]thiophen-2-yl)phenyl]-3-methyl-4-isopropyl-2,4-dihydropyrano[2,3-c]pyrazol-1-ium bis-(trifluoroacetate)
-
-
6-amino-5-cyano-4-[3-cyano-5-(5-[[3-(morpholin-4-ium-4-yl)propyl]carbamoyl]thiophen-2-yl)phenyl]-3-methyl-4-isopropyl-2,4-dihydropyrano[2,3-c]pyrazol-1-ium bis-(trifluoroacetate)
-
aminopterin
-
-
benzyl 4-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]piperazine-1-carboxylate
-
-
benzyl 4-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]piperazine-1-carboxylate
-
benzyl 5-[3-[(4R)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
-
benzyl 5-[3-[(4R)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
benzyl 5-[3-[(4S)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
-
benzyl 5-[3-[(4S)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
benzyl 5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
-
benzyl 5-[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
beta-Alanine
-
-
beta-trifluoroallothreonine
-
-
beta-trifluoroallothreonine
-
-
beta-trifluoroallothreonine
-
-
beta-trifluoroallothreonine
-
-
beta-trifluoroallothreonine
-
-
beta-trifluorothreonine
-
-
beta-trifluorothreonine
-
-
beta-trifluorothreonine
-
-
beta-trifluorothreonine
-
-
beta-trifluorothreonine
-
-
beta-trifluorothreonine
-
-
Bromopyruvate
-
irreversible inactivation, substrates partially protect
Bromopyruvate
-
only cytoplasmac not mitochondrial enzyme
Chloroacetaldehyde
-
irreversible inactivation, substrates partially protect
Chloroacetaldehyde
-
only cytoplasmic not mitochondrial enzyme
Cibacron blue F3GA
-
reversible by dialysis
Cibacron blue F3GA
-
complete inhibition, NAD(H) protects, reversible by tetrahydrofolate
Co2+
-
strong inhibition at 1 mM
Co2+
60.03% residual activity at 1 mM
Co2+
strong inhibition at 1 mM
Co2+
slight inhibition; strong inhibition
CTAB
-
-
Cu2+
-
strong inhibition
Cu2+
-
strong inhibition at 1 mM
Cu2+
8.95% residual activity at 1 mM
Cu2+
strong inhibition at 1 mM
D-alanine
-
-
D-alanine
-
inactivates enzyme by converting the enzyme bound pyridoxal 5'-phosphate to pyridoxamine phosphate in a transamination reaction
D-alanine
inactivates enzyme by converting the enzyme bound pyridoxal 5'-phosphate to pyridoxamine phosphate in a transamination reaction
D-alanine
-
inactivates enzyme by converting the enzyme bound pyridoxal 5'-phosphate to pyridoxamine phosphate in a transamination reaction
D-beta-fluoroalanine
-
-
D-cycloserine
-
-
D-cycloserine
-
overexpression of SHMT-S increases resistance in a rich folate containing medium
D-cycloserine
-
interaction extreme rapidly and irreversible
Dichloromethotrexate
-
-
DL-2-methylserine
-
-
ethyl 4-[[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl](methyl)amino]butanoate
-
-
ethyl 4-[[3-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl](methyl)amino]butanoate
-
Fe2+
-
strong inhibition at 1 mM
Fe2+
complete inhibition at 1 mM
Fe2+
strong inhibition at 1 mM
formaldehyde
inactivation
formaldehyde
inactivation
Glycidaldehyde
-
directed to C1-binding-site
Glycidaldehyde
-
only cytoplasmic enzyme
glycine
-
-
glycine
-
glycine inhibits His6-tagged SHMT competitively with respect to serine and non-competitively with respect to tetrahydrofolate
Hg2+
-
strong inhibition at 1 mM
Hg2+
complete inhibition at 1 mM
Hg2+
strong inhibition at 1 mM
iodoacetamide
-
irreversible inactivation, substrates partially protect
iodoacetamide
-
only cytoplasmic not mitochondrial enzyme
KCl
-
-
L-alanine
-
-
L-amino acids
-
-
L-amino acids
-
weak, e.g. L-aspartic acid, ornithine, lysine, methionine, phenylalanine, homoserine, threonine, 4-aminobutyric acid
L-cysteine
-
-
L-cysteine
-
mitochondrial enzyme
L-methionine
-
not
L-serine
-
-
L-serine
-
competitive to glycine
lometrexol
-
competitive inhibition
lometrexol
49.7% residual activity at 0.1 mM
methotrexate
-
-
methotrexate
87.4% residual activity at 0.1 mM
methyl 3'-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5'-chloro[1,1'-biphenyl]-4-carboxylate
-
-
methyl 3'-[6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5'-chloro[1,1'-biphenyl]-4-carboxylate
-
methyl 5-[3-[(4R)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
-
methyl 5-[3-[(4R)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
methyl 5-[3-[(4S)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
-
methyl 5-[3-[(4S)-6-amino-5-cyano-3-methyl-4-(propan-2-yl)-2,4-dihydropyrano[2,3-c]pyrazol-4-yl]-5-cyanophenyl]thiophene-2-carboxylate
-
methyl methanethiosulfonate
-
-
methyl methanethiosulfonate
-
-
methyl methanethiosulfonate
-
-
methyl methanethiosulfonate
-
-
methyl methanethiosulfonate
-
-
Mn2+
-
strong inhibition at 1 mM
Mn2+
60.81% residual activity at 1 mM
Mn2+
strong inhibition at 1 mM
NaCl
60% inhibition at 100 mM, restored to 66-71% activity in presence of 50 mM glycine betaine
NH2OH
-
-
PCMB
-
strong
pemetrexed
-
i.e. (S)-2-[4-[2-(4-amino-2-oxo-3,5,7-triazabicyclo[4.3.0]nona-3,8,10-trien-9-yl) ethyl] benzoyl]aminopentanedioic acid, brand name Alimta, low micromolar inhibitor
pemetrexed
79.2% residual activity at 0.1 mM
raltitrexed
-
-
raltitrexed
94% residual activity at 0.1 mM
SDS
-
strong inhibition
substituted hydroxylamine derivates
-
-
-
substituted hydroxylamine derivates
-
-
-
substituted hydroxylamine derivates
-
-
-
substituted hydroxylamine derivates
-
-
-
substituted hydroxylamine derivates
-
-
-
substituted hydroxylamine derivates
-
-
-
sulfonyl fluoride triazine derivates
-
-
sulfonyl fluoride triazine derivates
-
-
sulfonyl fluoride triazine derivates
-
-
sulfonyl fluoride triazine derivates
-
-
sulfonyl fluoride triazine derivates
-
-
sulfonyl fluoride triazine derivates
-
-
tetrahydrofolate
strong substrate inhibition
tetrahydrofolate
-
strong and pH-dependent substrate inhibition due to the formation of the enzyme-glycine:tetrahydrofolate dead-end complex (at low pH values)
tetrahydrofolate
isoform SHMT2 maintains a pronounced tetrahydrofolate substrate inhibition even at the alkaline pH characteristic of the mitochondrial matrix
tetrahydrofolate
inhibitory at non-saturating concentration of serine, at concentrations above 1.5 mM
tetrahydrofolate
at concentrations above 0.015 mM, substrate inhibition is observed
tetrahydrofolate derivatives
-
-
-
tetrahydrofolate derivatives
-
-
-
tetrahydrofolate derivatives
-
-
-
tetrahydrofolate derivatives
-
-
-
tetrahydrofolate derivatives
-
-
-
tetrahydrofolate derivatives
-
-
-
tetrahydrofolate derivatives
-
-
-
Thiosemicarbazide
-
-
Thiosemicarbazide
-
poorly active against promastigotes, but SHMT-S transfectants can provide a small but significant resistance
Urea
in 1 M urea, almost all the cofactor is bound to the enzyme as internal aldimine, indicating that the loss of activity does not result from the denaturation of the active site, these observations suggest that urea might act as an enzyme inhibitor
Urea
81% loss of activity at 1M
Zn2+
2.91% residual activity at 1 mM
additional information
model of uncompetitive substrate inhibition using tetrahydropteroylglutamates with different numbers of glutamate residues, overview
-
additional information
-
model of uncompetitive substrate inhibition using tetrahydropteroylglutamates with different numbers of glutamate residues, overview
-
additional information
-
not: iodoacetate
-
additional information
-
-
-
additional information
-
not: ethanolamine, ethylenediamine; not: valine, leucine, glutamic acid, 3-hydroxybutyric acid
-
additional information
-
not: valine, leucine, glutamic acid, 3-hydroxybutyric acid
-
additional information
the enzyme is not significantly influenced in activity by NH4+, Sl2+, Ca2+, Pb2+, SDS and CTAB
-
additional information
-
the enzyme is not significantly influenced in activity by NH4+, Sl2+, Ca2+, Pb2+, SDS and CTAB
-
additional information
-
not: methionine, S-adenosyl-L-methionine, XMP, IMP, phosphoglycerate
-
additional information
prototypes with negative total charge have greater affinity for Plasmodium falciparum SHMT than for human SHMT
-
additional information
-
not: EDTA
-
additional information
-
inhibition kinetics
-
additional information
-
not: iodoacetate; not: NaN3, mono- or divalent cations, 2-mercaptoethanol, DTT; not: purine nucleoside mono-, di- and triphosphates
-
additional information
-
not: chloroacetamide; not: iodoacetate
-
additional information
-
inhibition kinetics
-
additional information
-
inhibition kinetics
-
additional information
-
not: N-/O-chloroacetyl and N-/O-bromoacetyl derivatives of glycine and L-serine
-
additional information
-
inhibition kinetics
-
additional information
-
in order to act as selective ligands for the active site, the tails of the 5-formyl-6-hydrofolic acid analogues as potential selective inhibitors should be short to avoid the repulsive interactions with residues Lys138, Lys139 and Lys140 of the active site of SHMT, the tails may be longer, but in that case they must possess both negative and positive charges at the right positions, in order to explore their interactions with Lys138, Lys139, Lys140 and Glu137, prototypes with negative total charge have greater affinity for Plasmodium falciparum SHMT than for human SHMT
-
additional information
-
not: mercaptopropionic acid, mercaptoethanolamine; not: valine, leucine, glutamic acid, 3-hydroxybutyric acid
-
additional information
-
not: EDTA; not: purine nucleoside mono-, di- and triphosphates
-