4g1f

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(New page: '''Unreleased structure''' The entry 4g1f is ON HOLD Authors: Skene, Robert J., Gwaltney, Stephen L. Description: Crystal Structure of human Dipeptidyl Peptidase IV in complex with a p...)
Current revision (10:52, 6 November 2024) (edit) (undo)
 
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'''Unreleased structure'''
 
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The entry 4g1f is ON HOLD
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==Crystal Structure of human Dipeptidyl Peptidase IV in complex with a pyridopyrimidinedione analogue==
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<StructureSection load='4g1f' size='340' side='right'caption='[[4g1f]], [[Resolution|resolution]] 2.90&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4g1f]] is a 4 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4G1F OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4G1F FirstGlance]. <br>
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</td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 2.9&#8491;</td></tr>
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<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=0WG:7-AMINO-6-(AMINOMETHYL)-5-(2-BROMOPHENYL)-1,3-DIMETHYLPYRIDO[2,3-D]PYRIMIDINE-2,4(1H,3H)-DIONE'>0WG</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></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=4g1f FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4g1f OCA], [https://pdbe.org/4g1f PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4g1f RCSB], [https://www.ebi.ac.uk/pdbsum/4g1f PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4g1f ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/DPP4_HUMAN DPP4_HUMAN] Cell surface glycoprotein receptor involved in the costimulatory signal essential for T-cell receptor (TCR)-mediated T-cell activation. Acts as a positive regulator of T-cell coactivation, by binding at least ADA, CAV1, IGF2R, and PTPRC. Its binding to CAV1 and CARD11 induces T-cell proliferation and NF-kappa-B activation in a T-cell receptor/CD3-dependent manner. Its interaction with ADA also regulates lymphocyte-epithelial cell adhesion. In association with FAP is involved in the pericellular proteolysis of the extracellular matrix (ECM), the migration and invasion of endothelial cells into the ECM. May be involved in the promotion of lymphatic endothelial cells adhesion, migration and tube formation. When overexpressed, enhanced cell proliferation, a process inhibited by GPC3. Acts also as a serine exopeptidase with a dipeptidyl peptidase activity that regulates various physiological processes by cleaving peptides in the circulation, including many chemokines, mitogenic growth factors, neuropeptides and peptide hormones. Removes N-terminal dipeptides sequentially from polypeptides having unsubstituted N-termini provided that the penultimate residue is proline.<ref>PMID:10951221</ref> <ref>PMID:17549790</ref> <ref>PMID:10570924</ref> <ref>PMID:10900005</ref> <ref>PMID:11772392</ref> <ref>PMID:14691230</ref> <ref>PMID:16651416</ref> <ref>PMID:17287217</ref> <ref>PMID:18708048</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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Dipeptidyl peptidase IV (DPP-4) inhibitors have been shown to enhance GLP-1 levels and thereby improve hyperglycemia in type II diabetes. From a small fragment hit, using structure-based design, we have discovered a new class of non-covalent, potent and selective DPP-4 inhibitors.
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Authors: Skene, Robert J., Gwaltney, Stephen L.
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Structure-based design of pyridopyrimidinediones as dipeptidyl peptidase IV inhibitors.,Lam B, Zhang Z, Stafford JA, Skene RJ, Shi L, Gwaltney SL 2nd Bioorg Med Chem Lett. 2012 Nov 1;22(21):6628-31. doi: 10.1016/j.bmcl.2012.08.110., Epub 2012 Sep 7. PMID:23025999<ref>PMID:23025999</ref>
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Description: Crystal Structure of human Dipeptidyl Peptidase IV in complex with a pyridopyrimidinedione analogue
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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 4g1f" style="background-color:#fffaf0;"></div>
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==See Also==
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*[[Dipeptidyl peptidase 3D structures|Dipeptidyl peptidase 3D structures]]
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== References ==
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<references/>
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__TOC__
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</StructureSection>
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[[Category: Homo sapiens]]
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[[Category: Large Structures]]
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[[Category: Gwaltney SL]]
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[[Category: Skene RJ]]

Current revision

Crystal Structure of human Dipeptidyl Peptidase IV in complex with a pyridopyrimidinedione analogue

PDB ID 4g1f

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