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Literature summary for 2.1.1.5 extracted from

  • Vanek, V.; Budesinsky, M.; Kabeleova, P.; Sanda, M.; Kozisek, M.; Hanclova, I.; Mladkova, J.; Brynda, J.; Rosenberg, I.; Koutmos, M.; Garrow, T.A.; Jiracek, J.
    Structure-activity study of new inhibitors of human betaine-homocysteine S-methyltransferase (2009), J. Med. Chem., 52, 3652-3665.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(RS)-2-amino-4-[(2-carboxyethylthio)methylthio]butanoic acid 97.6% inhibition at 0.02 mM Homo sapiens
(RS)-2-amino-4-[(3-carboxypropyl)disulfanyl]butanoic acid 19.1% inhibition at 0.02 mM Homo sapiens
(RS)-2-amino-4-[2-(carboxymethylamino)ethylthio]butanoic acid 37.1% inhibition at 0.02 mM Homo sapiens
(RS)-2-amino-4-[2-(R)-(1-carboxyethylamino)ethylthio]butanoic acid 15.5% inhibition at 0.02 mM Homo sapiens
(RS)-2-amino-4-[2-(S)-(1-carboxyethylamino)ethylthio]butanoic acid 19.8% inhibition at 0.02 mM Homo sapiens
(RS)-2-amino-4-[2-[(carboxymethyl)(methyl)amino]ethylthio]-butanoic acid 98.5% inhibition at 0.02 mM Homo sapiens
(RS)-2-amino-4-[3-[(carboxymethyl)(methyl)amino]propylthio]butanoic acid 79.01% inhibition at 0.02 mM Homo sapiens
(RS)-2-amino-5-(3-carboxypropylthio)pentanoic acid 5.4% inhibition at 0.02 mM Homo sapiens
(RS)-2-aminodecanedioic acid 2.11% inhibition at 0.02 mM Homo sapiens
(RS)-2-[[2-(3-amino-3-carboxypropylthio)ethyl]dimethylammonium]acetate 23.8% inhibition at 0.02 mM Homo sapiens
(RS)-2-[[3-(3-amino-3-carboxypropylthio)propyl]dimethylammonio]acetate 3.3% inhibition at 0.02 mM Homo sapiens
(RS)-5-(3-amino-3-carboxypropoxy)pentanoic acid 9.8% inhibition at 0.02 mM Homo sapiens
(RS)-5-(3-amino-3-carboxypropylselanyl)pentanoic acid complete inhibition at 0.02 mM Homo sapiens
(RS)-5-(3-amino-3-carboxypropylthio)-3,3-dimethylpentanoic acid highly potent inhibitor of BHMT, complete inhibition at 0.02 mM Homo sapiens
(RS)-5-(3-amino-3-carboxypropylthio)-3-methylpentanoic acid highly potent inhibitor of BHMT, complete inhibition at 0.02 mM Homo sapiens
5-[(3-amino-3-carboxypropyl)sulfanyl]pentanoic acid complete inhibition at 0.02 mM Homo sapiens
additional information not inhibited by (RS)-2-[[(3-amino-3-carboxypropylthio)methyl]dimethylammonium] acetate and (RS)-2-amino-4-[2-(2-carboxyethylamino)ethylthio]butanoic acid Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-homocysteine + betaine
-
Homo sapiens L-methionine + dimethylglycine
-
?

Synonyms

Synonyms Comment Organism
BHMT
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000084
-
in 50 mM potassium phosphate buffer, at pH 7.5, at 37°C Homo sapiens (RS)-5-(3-amino-3-carboxypropylthio)-3,3-dimethylpentanoic acid
0.000139
-
in 50 mM potassium phosphate buffer, at pH 7.5, at 37°C Homo sapiens (RS)-5-(3-amino-3-carboxypropylthio)-3-methylpentanoic acid
0.000649
-
in 50 mM potassium phosphate buffer, at pH 7.5, at 37°C Homo sapiens (RS)-5-(3-amino-3-carboxypropylselanyl)pentanoic acid
0.0025
-
in 50 mM potassium phosphate buffer, at pH 7.5, at 37°C Homo sapiens (RS)-2-amino-4-[2-[(carboxymethyl)(methyl)amino]ethylthio]-butanoic acid
0.00326
-
in 50 mM potassium phosphate buffer, at pH 7.5, at 37°C Homo sapiens (RS)-2-amino-4-[(2-carboxyethylthio)methylthio]butanoic acid