7bfz

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==X-ray structure of human prostate-specific membrane antigen(PSMA) in complex with a inhibitor Glu-490==
==X-ray structure of human prostate-specific membrane antigen(PSMA) in complex with a inhibitor Glu-490==
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<StructureSection load='7bfz' size='340' side='right'caption='[[7bfz]]' scene=''>
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<StructureSection load='7bfz' size='340' side='right'caption='[[7bfz]], [[Resolution|resolution]] 1.73&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7BFZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7BFZ FirstGlance]. <br>
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<table><tr><td colspan='2'>[[7bfz]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7BFZ OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7BFZ FirstGlance]. <br>
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</td></tr><tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7bfz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7bfz OCA], [https://pdbe.org/7bfz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7bfz RCSB], [https://www.ebi.ac.uk/pdbsum/7bfz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7bfz ProSAT]</span></td></tr>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=BMA:BETA-D-MANNOSE'>BMA</scene>, <scene name='pdbligand=CA:CALCIUM+ION'>CA</scene>, <scene name='pdbligand=CL:CHLORIDE+ION'>CL</scene>, <scene name='pdbligand=EDO:1,2-ETHANEDIOL'>EDO</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene>, <scene name='pdbligand=PEG:DI(HYDROXYETHYL)ETHER'>PEG</scene>, <scene name='pdbligand=TKZ:(((S)-1-carboxy-5-((E)-2-cyano-3-(5-(1-(3-methoxy-3-oxopropyl)-1,2,3,4-tetrahydroquinolin-6-yl)thiophen-2-yl)acrylamido)pentyl)carbamoyl)-L-glutamic+acid'>TKZ</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>, <scene name='pdbligand=FUC:ALPHA-L-FUCOSE'>FUC</scene>, <scene name='pdbligand=MAN:ALPHA-D-MANNOSE'>MAN</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Glutamate_carboxypeptidase_II Glutamate carboxypeptidase II], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.17.21 3.4.17.21] </span></td></tr>
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<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=7bfz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7bfz OCA], [https://pdbe.org/7bfz PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7bfz RCSB], [https://www.ebi.ac.uk/pdbsum/7bfz PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7bfz ProSAT]</span></td></tr>
</table>
</table>
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== Function ==
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[[https://www.uniprot.org/uniprot/FOLH1_HUMAN FOLH1_HUMAN]] Has both folate hydrolase and N-acetylated-alpha-linked-acidic dipeptidase (NAALADase) activity. Has a preference for tri-alpha-glutamate peptides. In the intestine, required for the uptake of folate. In the brain, modulates excitatory neurotransmission through the hydrolysis of the neuropeptide, N-aceylaspartylglutamate (NAAG), thereby releasing glutamate. Isoform PSM-4 and isoform PSM-5 would appear to be physiologically irrelevant. Involved in prostate tumor progression. Also exhibits a dipeptidyl-peptidase IV type activity. In vitro, cleaves Gly-Pro-AMC.
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Surgery is an efficient way to treat localized prostate cancer (PCa), however, it is challenging to demarcate rapidly and accurately the tumor boundary intraoperatively, as existing tumor detection methods are seldom performed in real-time. To overcome those limitations, we develop a fluorescent molecular rotor that specifically targets the prostate-specific membrane antigen (PSMA), an established marker for PCa. The probes have picomolar affinity (IC50 = 63-118 pM) for PSMA and generate virtually instantaneous onset of robust fluorescent signal proportional to the concentration of the PSMA-probe complex. In vitro and ex vivo experiments using PCa cell lines and clinical samples, respectively, indicate the utility of the probe for biomedical applications, including real-time monitoring of endocytosis and tumor staging. Experiments performed in a PCa xenograft model reveal suitability of the probe for imaging applications in vivo.
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A prostate-specific membrane antigen activated molecular rotor for real-time fluorescence imaging.,Zhang J, Rakhimbekova A, Duan X, Yin Q, Foss CA, Fan Y, Xu Y, Li X, Cai X, Kutil Z, Wang P, Yang Z, Zhang N, Pomper MG, Wang Y, Barinka C, Yang X Nat Commun. 2021 Sep 15;12(1):5460. doi: 10.1038/s41467-021-25746-6. PMID:34526506<ref>PMID:34526506</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 7bfz" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Glutamate carboxypeptidase II]]
[[Category: Large Structures]]
[[Category: Large Structures]]
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[[Category: Barinka C]]
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[[Category: Barinka, C]]
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[[Category: Motlova L]]
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[[Category: Motlova, L]]
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[[Category: Rakhimbekova A]]
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[[Category: Rakhimbekova, A]]
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[[Category: Hydrolase]]
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[[Category: Inhibitor]]
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[[Category: Naaladase]]

Revision as of 06:41, 31 August 2022

X-ray structure of human prostate-specific membrane antigen(PSMA) in complex with a inhibitor Glu-490

PDB ID 7bfz

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