7nee
From Proteopedia
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==Inhibitor Complex with Thrombin Activatable Fibrinolysis inhibitor (TAFIa)== | ==Inhibitor Complex with Thrombin Activatable Fibrinolysis inhibitor (TAFIa)== | ||
| - | <StructureSection load='7nee' size='340' side='right'caption='[[7nee]]' scene=''> | + | <StructureSection load='7nee' size='340' side='right'caption='[[7nee]], [[Resolution|resolution]] 2.55Å' scene=''> |
== Structural highlights == | == Structural highlights == | ||
| - | <table><tr><td colspan='2'>Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7NEE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7NEE FirstGlance]. <br> | + | <table><tr><td colspan='2'>[[7nee]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Human Human]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=7NEE OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=7NEE FirstGlance]. <br> |
| - | </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=7nee FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7nee OCA], [https://pdbe.org/7nee PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7nee RCSB], [https://www.ebi.ac.uk/pdbsum/7nee PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7nee ProSAT]</span></td></tr> | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=U9B:(1R,3S)-3-(4-ammoniobutyl)-1-benzyl-1,4-azaphosphinan-1-ium-3-carboxylate+4,4-dioxide'>U9B</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr> |
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">CPB2 ([https://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 HUMAN])</td></tr> | ||
| + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[https://en.wikipedia.org/wiki/Carboxypeptidase_U Carboxypeptidase U], with EC number [https://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.17.20 3.4.17.20] </span></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=7nee FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=7nee OCA], [https://pdbe.org/7nee PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=7nee RCSB], [https://www.ebi.ac.uk/pdbsum/7nee PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=7nee ProSAT]</span></td></tr> | ||
</table> | </table> | ||
| + | == Function == | ||
| + | [[https://www.uniprot.org/uniprot/CBPB2_HUMAN CBPB2_HUMAN]] Cleaves C-terminal arginine or lysine residues from biologically active peptides such as kinins or anaphylatoxins in the circulation thereby regulating their activities. Down-regulates fibrinolysis by removing C-terminal lysine residues from fibrin that has already been partially degraded by plasmin.<ref>PMID:10574983</ref> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Selective and potent inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) have the potential to increase endogenous and therapeutic fibrinolysis and to behave like profibrinolytic agents without the risk of major hemorrhage, since they do not interfere either with platelet activation or with coagulation during blood hemostasis. Therefore, TAFIa inhibitors could be used in at-risk patients for the treatment, prevention, and secondary prevention of stroke, venous thrombosis, and pulmonary embolisms. In this paper, we describe the design, the structure-activity relationship (SAR), and the synthesis of novel, potent, and selective phosphinanes and azaphosphinanes as TAFIa inhibitors. Several highly active azaphosphinanes display attractive properties suitable for further in vivo efficacy studies in thrombosis models. | ||
| + | |||
| + | Phosphinanes and Azaphosphinanes as Potent and Selective Inhibitors of Activated Thrombin-Activatable Fibrinolysis Inhibitor (TAFIa).,Schaffner AP, Sansilvestri-Morel P, Despaux N, Ruano E, Persigand T, Rupin A, Mennecier P, Vallez MO, Raimbaud E, Desos P, Gloanec P J Med Chem. 2021 Mar 25. doi: 10.1021/acs.jmedchem.0c02072. PMID:33764059<ref>PMID:33764059</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | <div class="pdbe-citations 7nee" style="background-color:#fffaf0;"></div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
| + | [[Category: Carboxypeptidase U]] | ||
| + | [[Category: Human]] | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
| - | [[Category: Brown | + | [[Category: Brown, D G]] |
| - | [[Category: Gloanec P]] | + | [[Category: Gloanec, P]] |
| - | [[Category: Raimbaud E]] | + | [[Category: Raimbaud, E]] |
| - | [[Category: Schaffner | + | [[Category: Schaffner, A P]] |
| - | [[Category: Vuillard | + | [[Category: Vuillard, L M]] |
| + | [[Category: Complex]] | ||
| + | [[Category: Hydrolase]] | ||
| + | [[Category: Inhibitor]] | ||
Revision as of 08:35, 21 April 2021
Inhibitor Complex with Thrombin Activatable Fibrinolysis inhibitor (TAFIa)
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