2oqi

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{{Seed}}
 
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[[Image:2oqi.png|left|200px]]
 
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==Human Dipeptidyl Peptidase IV (DPP4) with Piperidinone-constrained phenethylamine==
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The line below this paragraph, containing "STRUCTURE_2oqi", creates the "Structure Box" on the page.
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<StructureSection load='2oqi' size='340' side='right'caption='[[2oqi]], [[Resolution|resolution]] 2.80&Aring;' scene=''>
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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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'>[[2oqi]] 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=2OQI OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=2OQI 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]] 2.8&#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=GGO:(4R,5R)-5-AMINO-1-[2-(1,3-BENZODIOXOL-5-YL)ETHYL]-4-(2,4,5-TRIFLUOROPHENYL)PIPERIDIN-2-ONE'>GGO</scene></td></tr>
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{{STRUCTURE_2oqi| PDB=2oqi | 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=2oqi FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2oqi OCA], [https://pdbe.org/2oqi PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=2oqi RCSB], [https://www.ebi.ac.uk/pdbsum/2oqi PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=2oqi 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/oq/2oqi_consurf.spt"</scriptWhenChecked>
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<scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.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=2oqi 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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Dipeptidyl peptidase IV (DPP4) inhibitors are emerging as a new class of therapeutic agents for the treatment of type 2 diabetes. They exert their beneficial effects by increasing the levels of active glucagon-like peptide-1 and glucose-dependent insulinotropic peptide, which are two important incretins for glucose homeostasis. Starting from a high-throughput screening hit, we were able to identify a series of piperidinone- and piperidine-constrained phenethylamines as novel DPP4 inhibitors. Optimized compounds are potent, selective, and have good pharmacokinetic profiles.
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===Human Dipeptidyl Peptidase IV (DPP4) with Piperidinone-constrained phenethylamine===
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Discovery and structure-activity relationships of piperidinone- and piperidine-constrained phenethylamines as novel, potent, and selective dipeptidyl peptidase IV inhibitors.,Pei Z, Li X, von Geldern TW, Longenecker K, Pireh D, Stewart KD, Backes BJ, Lai C, Lubben TH, Ballaron SJ, Beno DW, Kempf-Grote AJ, Sham HL, Trevillyan JM J Med Chem. 2007 Apr 19;50(8):1983-7. Epub 2007 Mar 17. PMID:17367123<ref>PMID:17367123</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 2oqi" style="background-color:#fffaf0;"></div>
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==See Also==
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The line below this paragraph, {{ABSTRACT_PUBMED_17367123}}, 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 17367123 is the PubMed ID number.
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== References ==
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<references/>
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{{ABSTRACT_PUBMED_17367123}}
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__TOC__
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</StructureSection>
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==About this Structure==
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2OQI is a 4 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=2OQI OCA].
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==Reference==
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<ref group="xtra">PMID:17367123</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: Backes, B J.]]
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[[Category: Large Structures]]
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[[Category: Ballaron, S J.]]
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[[Category: Backes BJ]]
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[[Category: Beno, D W.]]
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[[Category: Ballaron SJ]]
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[[Category: Geldern, T W.von.]]
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[[Category: Beno DW]]
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[[Category: Kempf-Grote, A J.]]
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[[Category: Kempf-Grote AJ]]
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[[Category: Lai, C.]]
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[[Category: Lai C]]
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[[Category: Li, X.]]
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[[Category: Li X]]
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[[Category: Longenecker, K L.]]
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[[Category: Longenecker KL]]
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[[Category: Lubben, T H.]]
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[[Category: Lubben TH]]
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[[Category: Pei, Z.]]
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[[Category: Pei Z]]
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[[Category: Pireh, D.]]
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[[Category: Pireh D]]
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[[Category: Sham, H L.]]
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[[Category: Sham HL]]
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[[Category: Stewart, K D.]]
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[[Category: Stewart KD]]
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[[Category: Trevillyan, J M.]]
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[[Category: Trevillyan JM]]
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[[Category: Inhibitor]]
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[[Category: Von Geldern TW]]
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[[Category: Serine-peptidase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Feb 18 00:13:16 2009''
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Current revision

Human Dipeptidyl Peptidase IV (DPP4) with Piperidinone-constrained phenethylamine

PDB ID 2oqi

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