3hab

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{{Seed}}
 
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[[Image:3hab.jpg|left|200px]]
 
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==The structure of DPP4 in complex with piperidine fused benzimidazole 25==
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The line below this paragraph, containing "STRUCTURE_3hab", creates the "Structure Box" on the page.
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<StructureSection load='3hab' size='340' side='right'caption='[[3hab]], [[Resolution|resolution]] 2.10&Aring;' scene=''>
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== Structural highlights ==
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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<table><tr><td colspan='2'>[[3hab]] is a 2 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=3HAB OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=3HAB FirstGlance]. <br>
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or leave the SCENE parameter empty for the default display.
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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]] 2.1&#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=677:(2R,3R)-7-(METHYLSULFONYL)-3-(2,4,5-TRIFLUOROPHENYL)-1,2,3,4-TETRAHYDROPYRIDO[1,2-A]BENZIMIDAZOL-2-AMINE'>677</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>, <scene name='pdbligand=NAG:N-ACETYL-D-GLUCOSAMINE'>NAG</scene></td></tr>
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{{STRUCTURE_3hab| PDB=3hab | SCENE= }}
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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=3hab FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3hab OCA], [https://pdbe.org/3hab PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=3hab RCSB], [https://www.ebi.ac.uk/pdbsum/3hab PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=3hab 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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== Evolutionary Conservation ==
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[[Image:Consurf_key_small.gif|200px|right]]
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Check<jmol>
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<jmolCheckbox>
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<scriptWhenChecked>; select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/ha/3hab_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview03.spt</scriptWhenUnchecked>
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<text>to colour the structure by Evolutionary Conservation</text>
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</jmolCheckbox>
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</jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/main_output.php?pdb_ID=3hab ConSurf].
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<div style="clear:both"></div>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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A new series of DPP-4 inhibitors derived from piperidine-fused benzimidazoles and imidazopyridines is described. Optimization of this class of DPP-4 inhibitors led to the discovery of imidazopyridine 34. The potency, selectivity, cross-species DMPK profiles, and in vivo efficacy of 34 is reported.
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===The structure of DPP4 in complex with piperidine fused benzimidazole 25===
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Aminopiperidine-fused imidazoles as dipeptidyl peptidase-IV inhibitors.,Edmondson SD, Mastracchio A, Cox JM, Eiermann GJ, He H, Lyons KA, Patel RA, Patel SB, Petrov A, Scapin G, Wu JK, Xu S, Zhu B, Thornberry NA, Roy RS, Weber AE Bioorg Med Chem Lett. 2009 Aug 1;19(15):4097-101. Epub 2009 Jun 6. PMID:19539471<ref>PMID:19539471</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 3hab" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_19539471}}, adds the Publication Abstract to the page
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*[[Dipeptidyl peptidase 3D structures|Dipeptidyl peptidase 3D structures]]
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(as it appears on PubMed at http://www.pubmed.gov), where 19539471 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_19539471}}
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__TOC__
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</StructureSection>
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==About this Structure==
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3HAB is a 2 chains structure of sequences from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3HAB OCA].
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==Reference==
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<ref group="xtra">PMID:19539471</ref><references group="xtra"/>
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[[Category: Dipeptidyl-peptidase IV]]
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[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Scapin, G.]]
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[[Category: Large Structures]]
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[[Category: Alpha/beta]]
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[[Category: Scapin G]]
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[[Category: Aminopeptidase]]
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[[Category: Beta-propeller]]
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[[Category: Cell membrane]]
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[[Category: Diabetes]]
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[[Category: Dimer]]
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[[Category: Disulfide bond]]
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[[Category: Glycoprotein]]
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[[Category: Hydrolase]]
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[[Category: Hydrolase/hydrolase inhibitor complex]]
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[[Category: Membrane]]
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[[Category: Protease]]
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[[Category: Secreted]]
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[[Category: Serine protease]]
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[[Category: Signal-anchor]]
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[[Category: Transmembrane]]
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[[Category: X-ray diffraction]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jul 22 20:42:12 2009''
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Current revision

The structure of DPP4 in complex with piperidine fused benzimidazole 25

PDB ID 3hab

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