Literature summary for 3.4.17.21 extracted from

Tsukamoto, T.; Majer, P.; Vitharana, D.; Ni, C.; Hin, B.; Lu, X.C.; Thomas, A.G.; Wozniak, K.M.; Calvin, D.C.; Wu, Y.; Slusher, B.S.; Scarpetti, D.; Bonneville, G.W.
Enantiospecificity of glutamate carboxypeptidase II inhibition (2005), J. Med. Chem., 48, 2319-2324.

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Inhibitors

Inhibitors	Comment	Organism	Structure
(R)-2-(3-mercaptopropyl)-pentanedioic acid	equally potent as the S-isomer, 0.000085 mM	Homo sapiens
(R)-2-(3-mercaptopropyl)-pentanedioic acid	antinociceptide effects in the chronic constriction injury model, cell culture model of cerebral ischemia	Rattus norvegicus
(R)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid	40fold less potent than the S-isomer, IC50: 0.0014 mM	Homo sapiens
(R)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid	neuroprotective effects in the middle cerebral artery occlusion model, cell culture model of cerebral ischemia	Rattus norvegicus
(R)-2-(phosphonomethyl)-pentanedioic acid	less potent than the S-isomer, IC50: 0.000030 mM	Homo sapiens
(R)-2-(phosphonomethyl)-pentanedioic acid	-	Rattus norvegicus
(S)-2-(3-mercaptopropyl)-pentanedioic acid	equally potent as the R-isomer, 0.000067 mM	Homo sapiens
(S)-2-(3-mercaptopropyl)-pentanedioic acid	antinociceptide effects in the chronic constriction injury model, cell culture model of cerebral ischemia	Rattus norvegicus
(S)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid	40fold more potent than the R-isomer, IC50: 0.000034 mM	Homo sapiens
(S)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid	neuroprotective effects in the middle cerebral artery occlusion model, cell culture model of cerebral ischemia	Rattus norvegicus
(S)-2-(phosphonomethyl)-pentanedioic acid	more potent than the R-isomer, IC50: 0.0000001 mM	Homo sapiens
(S)-2-(phosphonomethyl)-pentanedioic acid	-	Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates	Organism	Comment (Nat. Sub.)	Natural Products	Comment (Nat. Pro.)	Rev.	Reac.
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O	Homo sapiens	-	N-acetyl-alpha-L-aspartate + L-glutamate	-	?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O	Rattus norvegicus	-	N-acetyl-alpha-L-aspartate + L-glutamate	-	?

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	-	-	-
Rattus norvegicus	-	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
cell culture	cerebral ischemia cell culture model	Rattus norvegicus	-

Substrates and Products (Substrate)

Substrates	Comment Substrates	Organism	Products	Comment (Products)	Rev.	Reac.
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O	-	Homo sapiens	N-acetyl-alpha-L-aspartate + L-glutamate	-	?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O	-	Rattus norvegicus	N-acetyl-alpha-L-aspartate + L-glutamate	-	?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O	enantiospecific reaction	Homo sapiens	N-acetyl-alpha-L-aspartate + L-glutamate	-	?
N-acetyl-alpha-L-aspartyl-L-glutamate + H2O	enantiospecific reaction	Rattus norvegicus	N-acetyl-alpha-L-aspartate + L-glutamate	-	?

Synonyms

Synonyms	Comment	Organism
GCP II	-	Homo sapiens
GCP II	-	Rattus norvegicus

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000001	-	more potent than the R-isomer, IC50: 0.0000001 mM	Homo sapiens	(S)-2-(phosphonomethyl)-pentanedioic acid
0.00003	-	less potent than the S-isomer, IC50: 0.000030 mM	Homo sapiens	(R)-2-(phosphonomethyl)-pentanedioic acid
0.000034	-	40fold more potent than the R-isomer, IC50: 0.000034 mM	Homo sapiens	(S)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid
0.0014	-	40fold less potent than the S-isomer, IC50: 0.0014 mM	Homo sapiens	(R)-2-(hydroxypentafluorophenylmethyl-phosphinoylmethyl)pentanedioic acid

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Release 2023.1 (January 2023)