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Literature summary for 2.3.1.15 extracted from

  • Wydysh, E.A.; Vadlamudi, A.; Medghalchi, S.M.; Townsend, C.A.
    Design, synthesis, and biological evaluation of conformationally constrained glycerol 3-phosphate acyltransferase inhibitors (2010), Bioorg. Med. Chem., 18, 6470-6479.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
docking experiments with the soluble squash chloroplast enzyme crystal structure, PDB code 1k30, and inhibitors (1S,2R,3R)-2-hydroxy-3-[(octylsulfonyl)amino]cyclopentanecarboxylic acid, (+-)-2-hydroxy-3-(octylsulfonamido)-cyclohexanecarboxylic acid, (1S,2S,3S)-2-hydroxy-3-[(octylsulfonyl)amino]cyclopentanecarboxylic acid, and (+-)-2-(2-hydroxy-3-(octylsulfonamido)-cyclopentyl)acetic acid. Cyclopentyl and cyclohexyl scaffolds of the inhibitors may be occluded from the enzyme active site by two protein loops that sterically guard the phosphate binding region Cucurbita moschata

Inhibitors

Inhibitors Comment Organism Structure
(+-)-2-(2-hydroxy-3-(octylsulfonamido)-cyclopentyl)acetic acid
-
Cucurbita moschata
(+-)-2-(2-hydroxy-3-(octylsulfonamido)-cyclopentyl)acetic acid 8% inhibition at 40 microg/ml Homo sapiens
(+-)-2-hydroxy-3-(octylsulfonamido)-cyclohexanecarboxylic acid
-
Cucurbita moschata
(+-)-2-hydroxy-3-(octylsulfonamido)-cyclohexanecarboxylic acid 36% inhibition at 40 microg/ml Homo sapiens
(+-)-2-hydroxy-3-(octylsulfonamido)-cyclopentane carboxylic acid 97% inhibition at 40 microg/ml Homo sapiens
(+-)-2-hydroxy-3-(octylsulfonamido)-cyclopentanecarboxylic acid 3% inhibition at 40 microg/ml Homo sapiens
(1S,2R,3R)-2-hydroxy-3-[(octylsulfonyl)amino]cyclopentanecarboxylic acid
-
Cucurbita moschata
(1S,2S,3S)-2-hydroxy-3-[(octylsulfonyl)amino]cyclopentanecarboxylic acid
-
Cucurbita moschata
2-(nonylsulfonamido)benzoic acid
-
Cucurbita moschata
2-(nonylsulfonamido)benzoic acid 97% inhibition at 40 microg/ml Homo sapiens
additional information cyclopentyl and cyclohexyl scaffolds may be occluded from the enzyme active site by two protein loops that sterically guard the phosphate binding region Homo sapiens

Organism

Organism UniProt Comment Textmining
Cucurbita moschata P10349
-
-
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
glycerol 3-phosphate + palmitoyl-CoA
-
Homo sapiens CoA + 1-palmitoyl-sn-glycerol 3-phosphate
-
?
glycerol 3-phosphate + palmitoyl-CoA
-
Cucurbita moschata CoA + 1-palmitoyl-sn-glycerol 3-phosphate
-
?

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0247
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens 2-(nonylsulfonamido)benzoic acid
0.164
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (+-)-2-hydroxy-3-(octylsulfonamido)-cyclohexanecarboxylic acid
0.255
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (+-)-2-hydroxy-3-(octylsulfonamido)-cyclopentane carboxylic acid
0.295
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (+-)-2-(2-hydroxy-3-(octylsulfonamido)-cyclopentyl)acetic acid
0.324
-
pH not specified in the publication, temperature not specified in the publication Homo sapiens (+-)-2-hydroxy-3-(octylsulfonamido)-cyclopentanecarboxylic acid