Literature summary for 3.4.17.21 extracted from

Majer, P.; Jankarik, A.; Krecmerova, M.; Tichy, T.; Tenora, L.; Wozniak, K.; Wu, Y.; Pommier, E.; Ferraris, D.; Rais, R.; Slusher, B.
Discovery of orally available prodrugs of the glutamate carboxypeptidase II (GCPII) inhibitor 2-phosphonomethylpentanedioic acid (2-PMPA) (2016), J. Med. Chem., 59, 2810-2819 .

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Application

Application	Comment	Organism
medicine	inhibitors of glutamate carboxypeptidase II with distinct chemical scaffolds are efficacious in several neurological models wherein excess glutamatergic transmission is presumed pathogenic. These include animal models of neuropathic pain, peripheral neuropathy, stroke, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, epilepsy, traumatic brain injury, addiction, and cognition	Canis lupus familiaris
medicine	inhibitors of glutamate carboxypeptidase II with distinct chemical scaffolds are efficacious in several neurological models wherein excess glutamatergic transmission is presumed pathogenic. These include animal models of neuropathic pain, peripheral neuropathy, stroke, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, epilepsy, traumatic brain injury, addiction, and cognition	Mus musculus

Inhibitors

Inhibitors	Comment	Organism	Structure
2-(phosphonomethyl)pentanedioic acid	potent inhibitor, robust neuroprotective efficacy in many neurological disease models	Canis lupus familiaris
2-(phosphonomethyl)pentanedioic acid	potent inhibitor, robust neuroprotective efficacy in many neurological disease models	Mus musculus
4-[[bis[[(isopropoxycarbonyl)oxy]methoxy]phosphoryl]-methyl]-5-[[(isopropoxycarbonyl)oxy]methoxy]-5-oxopentanoic acid	the orally bioavailable prodrug affords excellent release of 2-phosphonomethylpentanedioic acid following oral administration in both mice and dog	Canis lupus familiaris
4-[[bis[[(isopropoxycarbonyl)oxy]methoxy]phosphoryl]-methyl]-5-[[(isopropoxycarbonyl)oxy]methoxy]-5-oxopentanoic acid	the orally bioavailable prodrug affords excellent release of 2-phosphonomethylpentanedioic acid following oral administration in both mice and dog	Mus musculus

Organism

Organism	UniProt	Comment	Textmining
Canis lupus familiaris	-	beagle	-
Mus musculus	O35409	-	-

Synonyms

Synonyms	Comment	Organism
GCPII	-	Canis lupus familiaris
GCPII	-	Mus musculus
glutamate carboxypeptidase II	-	Canis lupus familiaris
glutamate carboxypeptidase II	-	Mus musculus

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.0000003	-	2-(phosphonomethyl)pentanedioic acid	pH and temperature not specified in the publication	Canis lupus familiaris
0.0000003	-	2-(phosphonomethyl)pentanedioic acid	pH and temperature not specified in the publication	Mus musculus

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Release 2023.1 (January 2023)