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Literature summary for 3.4.17.21 extracted from

  • Novakova, Z.; Cerny, J.; Choy, C.J.; Nedrow, J.R.; Choi, J.K.; Lubkowski, J.; Berkman, C.E.; Barinka, C.
    Design of composite inhibitors targeting glutamate carboxypeptidase II the importance of effector functionalities (2016), FEBS J., 283, 130-143 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.17.21

Crystallization (Commentary)

Crystallization (Comment) Organism
hanging-drop vapor-diffusion method, crystal structures of human glutamate carboxypeptidase II in complex with a series of phosphoramidate-based inhibitors harboring effector functions of diverse physicochemical characteristics Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-(4-fluorobenzoyl)-L-isoleucyl-O-[[[(1S)-1,3-dicarboxypropyl]amino](hydroxy)phosphoryl]-L-serine
-
 Homo sapiens
N-(4-fluorobenzoyl)-L-valyl-O-[[[(1S)-1,3-dicarboxypropyl]amino](hydroxy)phosphoryl]-L-serine
-
 Homo sapiens
N-[(2-benzamidoethoxy)(hydroxy)phosphoryl]-L-glutamic acid
-
 Homo sapiens
N-[hydroxy(4-phenylbutoxy)phosphoryl]-L-glutamic acid
-
 Homo sapiens
N-[[(2R)-2-benzamido-2-carboxyethoxy](hydroxy)phosphoryl]-L-glutamic acid
-
 Homo sapiens
N-[[(2S)-2-benzamido-2-carboxyethoxy](hydroxy)phosphoryl]-L-glutamic acid
-
 Homo sapiens
N-[[(2S)-2-[[(6S)-6-amino-6-carboxy-3-oxohexyl]amino]-2-carboxyethoxy](hydroxy)phosphoryl]-L-glutamic acid
-
 Homo sapiens
N-[[([1,1'-biphenyl]-4-yl)methoxy](hydroxy)phosphoryl]-L-glutamic acid
-
 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q04609
-
-

Synonyms

Synonyms Comment Organism
GCPII
-
 Homo sapiens
glutamate carboxypeptidase II
-
 Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000014
-
 37°C, pH 7.4 Homo sapiens N-[[(2S)-2-[[(6S)-6-amino-6-carboxy-3-oxohexyl]amino]-2-carboxyethoxy](hydroxy)phosphoryl]-L-glutamic acid
0.000016
-
 37°C, pH 7.4 Homo sapiens N-(4-fluorobenzoyl)-L-valyl-O-[[[(1S)-1,3-dicarboxypropyl]amino](hydroxy)phosphoryl]-L-serine
0.000016
-
 37°C, pH 7.4 Homo sapiens N-(4-fluorobenzoyl)-L-isoleucyl-O-[[[(1S)-1,3-dicarboxypropyl]amino](hydroxy)phosphoryl]-L-serine
0.000035
-
 37°C, pH 7.4 Homo sapiens N-[[(2S)-2-benzamido-2-carboxyethoxy](hydroxy)phosphoryl]-L-glutamic acid
0.000168
-
 37°C, pH 7.4 Homo sapiens N-[[([1,1'-biphenyl]-4-yl)methoxy](hydroxy)phosphoryl]-L-glutamic acid
0.00018
-
 37°C, pH 7.4 Homo sapiens N-[hydroxy(4-phenylbutoxy)phosphoryl]-L-glutamic acid
0.0007
-
 37°C, pH 7.4 Homo sapiens N-[[(2R)-2-benzamido-2-carboxyethoxy](hydroxy)phosphoryl]-L-glutamic acid
0.0018
-
 37°C, pH 7.4 Homo sapiens N-[(2-benzamidoethoxy)(hydroxy)phosphoryl]-L-glutamic acid