Literature summary for 3.4.17.21 extracted from

Kozikowski, A.P.; Nan, F.; Conti, P.; Zhang, J.; Ramadan, E.; Bzdega, T.; Wroblewska, B.; Neale, J.H.; Pshenichkin, S.; Wroblewski, J.T.
Design of remarkably simple, yet potent urea-based inhibitors of glutamate carboxypeptidase II (NAALADase) (2001), J. Med. Chem., 44, 298-301.

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Application

Application	Comment	Organism
medicine	design of inhibitors may lead to effective neuroprotective agents, possibility to employ GCPII inhibitors in stroke therapy	Rattus norvegicus

Inhibitors

Inhibitors	Comment	Organism	Structure
(t-Bu)Cys-PSI[C-O]-Glu	IC50: 29 nM	Rattus norvegicus
2-(phosphonomethyl)pentanedioic acid	IC50: 5.1 nM	Rattus norvegicus
Asp-Glu	-	Rattus norvegicus
Asp-PSI[C-O-S]-Glu	IC50: 0.0461 mM	Rattus norvegicus
Asp-PSI[C-O]-Asp	IC50: 0.0038 mM	Rattus norvegicus
Asp-PSI[S]-Asp	0.1 mM, 42% inhibition	Rattus norvegicus
Cys-PSI[C-O-S]-Glu	IC50: 6.9 nM	Rattus norvegicus
D-Glu-PSI[C-O]-D-Glu	0.1 mM, 67% inhibition	Rattus norvegicus
D-Glu-PSI[C-O]-Glu	0.001 mM, 25% inhibition	Rattus norvegicus
Glu-Glu	-	Rattus norvegicus
Glu-PSI[C-O-C-O]-Glu	0.001 mM, 9% inhibition	Rattus norvegicus
Glu-PSI[C-O]-Glu	IC50: 47 nM	Rattus norvegicus
Gly-PSI[C-O-S]-Glu	0.001 mM, 46% inhibition	Rattus norvegicus
t-BuNHC(O)-Glu	0.001 mM, 10% inhibition	Rattus norvegicus
[HO2C(CH2)2CH(CO2H)CH2]2P(O)(OH)	-	Rattus norvegicus

Organism

Organism	UniProt	Comment	Textmining
Rattus norvegicus	-	-	-

IC50 Value

IC50 Value	IC50 Value Maximum	Comment	Organism	Inhibitor	Structure
0.0000051	-	IC50: 5.1 nM	Rattus norvegicus	2-(phosphonomethyl)pentanedioic acid
0.0000069	-	IC50: 6.9 nM	Rattus norvegicus	Cys-PSI[C-O-S]-Glu
0.000029	-	IC50: 29 nM	Rattus norvegicus	(t-Bu)Cys-PSI[C-O]-Glu
0.000047	-	IC50: 47 nM	Rattus norvegicus	Glu-PSI[C-O]-Glu
0.0038	-	IC50: 0.0038 mM	Rattus norvegicus	Asp-PSI[C-O]-Asp
0.0461	-	IC50: 0.0461 mM	Rattus norvegicus	Asp-PSI[C-O-S]-Glu

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Release 2023.1 (January 2023)