Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.17.21 extracted from

  • Tykvart, J.; Schimer, J.; Jankarik, A.; Barinkova, J.; Navratil, V.; Starkova, J.; Sramkova, K.; Konvalinka, J.; Majer, P.; Sacha, P.
    Design of highly potent urea-based, exosite-binding inhibitors selective for glutamate carboxypeptidase II (2015), J. Med. Chem., 58, 4357-4363 .
    View publication on PubMed
Search for more literature for 3.4.17.21

Application

Application Comment Organism
diagnostics the enzyme is a prostate cancer marker Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
(S)-2-(3-((S)-1-carboxy-(4-iodobenzamido)pentyl)ureido)pentanedioic acid 830fold selectivity compared to glutamate carboxypeptidase III Homo sapiens
(S)-2-(3-((S)-5-(6-(4-(4-(4-acetylpiperazin-1-yl)phenyl)piperazin-1-yl)-N-(4-bromobenzyl)nicotinamido)-1-carboxypentyl)ureido)-pentanedioic acid 4200fold selectivity compared to glutamate carboxypeptidase III Homo sapiens
(S)-2-(3-((S)-5-(6-(4-(4-(4-acetylpiperazin-1-yl)phenyl)piperazin-1-yl)nicotinamido)-1-carboxypentyl)ureido)pentanedioic acid 1400fold selectivity compared to glutamate carboxypeptidase III Homo sapiens
(S)-2-(3-((S)-5-(N-(4-bromobenzyl)-6-(4-(4-(4-(4-carboxy-3-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoyl)piperazin-1-yl)phenyl)-piperazin-1-yl)nicotinamido)-1-carboxypentyl)ureido)pentanedioic acid 1900fold selectivity compared to glutamate carboxypeptidase III Homo sapiens
(S)-2-(3-((S)-5-(N-(4-bromobenzyl)-6-(4-(4-(4-(41-oxo-45-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10,13,16,19,22,25,28,31,34,37-dodecaoxa-40-azapentatetracontan-1-oyl)piperazin-1-yl)phenyl)piperazin-1-yl)nicotinamido)-1-carboxypentyl)ureido)pentanedioic acid 6600fold selectivity compared to glutamate carboxypeptidase III Homo sapiens
2-(phosphonomethyl)pentandioic acid 10fold selectivity compared to glutamate carboxypeptidase III Homo sapiens
DKFZ-PSMA-11 720fold selectivity compared to glutamate carboxypeptidase III Homo sapiens
N-[[[(1S)-1-carboxy-3-methylbutyl]amino]carbonyl]-L-glutamic acid i.e. ZJ-43. 160fold selectivity compared to glutamate carboxypeptidase III Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q04609
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Synonyms

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

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000000003
-
 (S)-2-(3-((S)-1-carboxy-(4-iodobenzamido)pentyl)ureido)pentanedioic acid pH and temperature not specified in the publication Homo sapiens
0.0000000086
-
 (S)-2-(3-((S)-5-(N-(4-bromobenzyl)-6-(4-(4-(4-(4-carboxy-3-(6-hydroxy-3-oxo-3H-xanthen-9-yl)benzoyl)piperazin-1-yl)phenyl)-piperazin-1-yl)nicotinamido)-1-carboxypentyl)ureido)pentanedioic acid pH and temperature not specified in the publication Homo sapiens
0.000000018
-
 DKFZ-PSMA-11 pH and temperature not specified in the publication Homo sapiens
0.000000049
-
 (S)-2-(3-((S)-5-(6-(4-(4-(4-acetylpiperazin-1-yl)phenyl)piperazin-1-yl)-N-(4-bromobenzyl)nicotinamido)-1-carboxypentyl)ureido)-pentanedioic acid pH and temperature not specified in the publication Homo sapiens
0.000000071
-
 (S)-2-(3-((S)-5-(6-(4-(4-(4-acetylpiperazin-1-yl)phenyl)piperazin-1-yl)nicotinamido)-1-carboxypentyl)ureido)pentanedioic acid pH and temperature not specified in the publication Homo sapiens
0.00000011
-
 (S)-2-(3-((S)-5-(N-(4-bromobenzyl)-6-(4-(4-(4-(41-oxo-45-((3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl)-4,7,10,13,16,19,22,25,28,31,34,37-dodecaoxa-40-azapentatetracontan-1-oyl)piperazin-1-yl)phenyl)piperazin-1-yl)nicotinamido)-1-carboxypentyl)ureido)pentanedioic acid pH and temperature not specified in the publication Homo sapiens
0.00000028
-
 2-(phosphonomethyl)pentandioic acid pH and temperature not specified in the publication Homo sapiens
0.00000058
-
 N-[[[(1S)-1-carboxy-3-methylbutyl]amino]carbonyl]-L-glutamic acid pH and temperature not specified in the publication Homo sapiens