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Literature summary for 5.1.1.18 extracted from

  • Takahara, S.; Nakagawa, K.; Uchiyama, T.; Yoshida, T.; Matsumoto, K.; Kawasumi, Y.; Mizuguchi, M.; Obita, T.; Watanabe, Y.; Hayakawa, D.; Gouda, H.; Mori, H.; Toyooka, N.
    Design, synthesis, and evaluation of novel inhibitors for wild-type human serine racemase (2017), Bioorg. Med. Chem. Lett., 28, 441-445 .
    View publication on PubMed

Application

Application Comment Organism
drug development serine racemase inhibitors are therapeutic candidates for the treatment of neurodegenerative disorders and epileptic states Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
1-(4-acetamidoanilino)-1-oxopropan-2-yl 3-[(2-chlorophenyl)sulfanyl]propanoate
-
Homo sapiens
1-(4-ethoxyanilino)-1-oxopropan-2-yl 3-[(2-chlorophenyl)sulfanyl]propanoate
-
Homo sapiens
1-anilino-1-oxopropan-2-yl 3-[(2-chlorophenyl)sulfanyl]propanoate
-
Homo sapiens
2-(4-acetamidoanilino)-2-oxoethyl 3-(2-fluorophenoxy)propanoate
-
Homo sapiens
2-(4-acetamidoanilino)-2-oxoethyl 3-(phenylsulfanyl)propanoate
-
Homo sapiens
2-(4-acetamidoanilino)-2-oxoethyl 3-[(2-chlorophenyl)sulfanyl]propanoate
-
Homo sapiens
2-(4-acetamidoanilino)-2-oxoethyl 3-[(2-fluorophenyl)sulfanyl]propanoate
-
Homo sapiens
2-(4-acetamidoanilino)-2-oxoethyl 3-[(2-methoxyphenyl)sulfanyl]propanoate
-
Homo sapiens
2-(4-acetamidoanilino)-2-oxoethyl 3-[(3-methoxyphenyl)sulfanyl]propanoate
-
Homo sapiens
2-(4-acetamidoanilino)-2-oxoethyl 3-[(4-methoxyphenyl)sulfanyl]propanoate
-
Homo sapiens
2-(4-acetamidoanilino)-2-oxoethyl 4-(2-methoxyphenyl)butanoate
-
Homo sapiens
additional information design, synthesis, and evaluation of inhibitors for wild-type human serine racemase. Serine racemase inhibitors are therapeutic candidates for the treatment of neurodegenerative disorders and epileptic states. No inhibition by 2-(4-acetamidoanilino)-2-oxoethyl 3-[(3-chlorophenyl)sulfanyl]propanoate, N-[2-(4-acetamidoanilino)-2-oxoethyl]-3-[(2-chlorophenyl)sulfanyl]propanamide, N-[2-(4-acetamidoanilino)-2-oxoethyl]-3-[(2-methoxyphenyl)sulfanyl]propanamide, and N-(4-acetamidophenyl)-7-(2-methoxyphenyl)-4-oxoheptanamide Homo sapiens
N-(4-acetamidophenyl)-N2-[3-[(2-chlorophenyl)sulfanyl]propanoyl]alaninamide
-
Homo sapiens
N-(4-acetamidophenyl)-N2-[3-[(2-methoxyphenyl)sulfanyl]propanoyl]alaninamide
-
Homo sapiens
N-(4-acetylphenyl)-2-[(3,4-dichlorophenyl)acetyl]hydrazine-1-carboxamide
-
Homo sapiens
N2-[(4-chlorophenoxy)acetyl]-N-(2,3,4-trifluorophenyl)glycinamide
-
Homo sapiens

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-serine Homo sapiens
-
D-serine
-
r

Organism

Organism UniProt Comment Textmining
Homo sapiens Q9GZT4
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-serine
-
Homo sapiens D-serine
-
r

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
8
-
assay at Homo sapiens

General Information

General Information Comment Organism
physiological function most of the endogenous free D-serine (about 90%) in the brain is produced by serine racemase. D-Serine in the brain is involved in neurodegenerative disorders and epileptic states as an endogenous co-agonist of the NMDA-type glutamate receptor Homo sapiens