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Literature summary for 3.4.17.21 extracted from

  • Pavlicek, J.; Ptacek, J.; Cerny, J.; Byun, Y.; Skultetyova, L.; Pomper, M.G.; Lubkowski, J.; Barinka, C.
    Structural characterization of P1-diversified urea-based inhibitors of glutamate carboxypeptidase II (2014), Bioorg. Med. Chem. Lett., 24, 2340-2345.
    View publication on PubMedView publication on EuropePMC

Crystallization (Commentary)

Crystallization (Comment) Organism
in complex with inhibitors N-2-([(1S)-1-carboxy-2-(furan-2-yl)ethyl]carbamoyl)-N-6-(4-iodobenzoyl)-L-lysine, N-2-([(1S)-1-carboxybut-3-yn-1-yl]carbamoyl)-N-6-(4-iodobenzoyl)-L-lysine, and N-([(1S)-1-carboxy-5-([(4-iodophenyl)carbonyl]amino)pentyl]carbamoyl)-L-glutamic acid, PDB entries 4OC2, 4OC3, and 3D7H, respectively Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
N-([(1S)-1-carboxy-5-([(4-iodophenyl)carbonyl]amino)pentyl]carbamoyl)-L-glutamic acid P1'-diversified urea-based inhibitor, in complex with enzyme PDB entry 3D7H Homo sapiens
N-2-([(1S)-1-carboxy-2-(furan-2-yl)ethyl]carbamoyl)-N-6-(4-iodobenzoyl)-L-lysine P1'-diversified urea-based inhibitor, in complex with enzyme PDB entry 4OC3 Homo sapiens
N-2-([(1S)-1-carboxybut-3-yn-1-yl]carbamoyl)-N-6-(4-iodobenzoyl)-L-lysine P1'-diversified urea-based inhibitor, in complex with enzyme PDB entry 4OC2 Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens Q04609
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-

Source Tissue

Source Tissue Comment Organism Textmining

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00000001
-
N-([(1S)-1-carboxy-5-([(4-iodophenyl)carbonyl]amino)pentyl]carbamoyl)-L-glutamic acid pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.0000053
-
N-2-([(1S)-1-carboxy-2-(furan-2-yl)ethyl]carbamoyl)-N-6-(4-iodobenzoyl)-L-lysine pH not specified in the publication, temperature not specified in the publication Homo sapiens
0.0000053
-
N-2-([(1S)-1-carboxybut-3-yn-1-yl]carbamoyl)-N-6-(4-iodobenzoyl)-L-lysine pH not specified in the publication, temperature not specified in the publication Homo sapiens