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PDBsum entry 5of0
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PDB id:
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Hydrolase
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Title:
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X-ray structure of human glutamate carboxypeptidase ii (gcpii), the e424m inactive mutant, in complex with a inhibitor cfbzog
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Structure:
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Glutamate carboxypeptidase 2. Chain: a. Synonym: cell growth-inhibiting gene 27 protein,folate hydrolase 1, folylpoly-gamma-glutamate carboxypeptidase,fgcp,glutamate carboxypeptidase ii,gcpii,membrane glutamate carboxypeptidase,mgcp,n- acetylated-alpha-linked acidic dipeptidase i,naaladase i,prostate- specific membrane antigen,psma,pteroylpoly-gamma-glutamate carboxypeptidase. Engineered: yes.
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Source:
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Homo sapiens. Human. Organism_taxid: 9606. Gene: folh1, folh, naalad1, psm, psma, gig27. Expressed in: drosophila melanogaster. Expression_system_taxid: 7227. Expression_system_cell_line: schneiders s2 cells.
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Resolution:
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1.48Å
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R-factor:
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0.157
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R-free:
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0.172
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Authors:
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Z.Novakova,L.Motlova,C.Barinka
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Key ref:
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R.Nakajima
et al.
(2018).
2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics.
ACS Med Chem Lett,
9,
1099-1104.
PubMed id:
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Date:
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10-Jul-17
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Release date:
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01-Aug-18
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PROCHECK
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Headers
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References
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Q04609
(FOLH1_HUMAN) -
Glutamate carboxypeptidase 2 from Homo sapiens
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Seq:
Struc:
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750 a.a.
692 a.a.*
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Key: |
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PfamA domain |
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Secondary structure |
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*
PDB and UniProt seqs differ
at 1 residue position (black
cross)
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Enzyme class:
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E.C.3.4.17.21
- glutamate carboxypeptidase Ii.
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Reaction:
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Release of an unsubstituted, C-terminal glutamyl residue, typically from Ac-Asp-Glu or folylpoly-gamma-glutamates.
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Cofactor:
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Zn(2+)
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ACS Med Chem Lett
9:1099-1104
(2018)
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PubMed id:
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2-Aminoadipic Acid-C(O)-Glutamate Based Prostate-Specific Membrane Antigen Ligands for Potential Use as Theranostics.
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R.Nakajima,
Z.Nováková,
W.Tueckmantel,
L.Motlová,
C.Bařinka,
A.P.Kozikowski.
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ABSTRACT
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The design and synthesis of prostate specific membrane antigen (PSMA) ligands
derived from 2-aminoadipic acid, a building block that has not previously been
used to construct PSMA ligands, are reported. The effects of both the linker
length and of an N-substituent of our PSMA ligands were probed, and X-ray
structures of five of these ligands bound to PSMA were obtained. Among the
ligands disclosed herein, 13b showed the highest inhibitory activity for
PSMA. As ligand 13b can readily be radiolabeled since its fluorine atom
is adjacent to the nitrogen atom of its pyridine ring, the use of this and
related compounds as theranostics can be pursued.
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