6zrv
From Proteopedia
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| - | '''Unreleased structure''' | ||
| - | + | ==Crystal Structure of Stabilized Active Plasminogen Activator Inhibitor-1 (PAI-1-W175F) in Complex with an Inhibitory Nanobody (VHH-s-a93, Nb93)== | |
| + | <StructureSection load='6zrv' size='340' side='right'caption='[[6zrv]], [[Resolution|resolution]] 1.88Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[6zrv]] is a 2 chain structure with sequence from [https://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] and [https://en.wikipedia.org/wiki/Vicugna_pacos Vicugna pacos]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=6ZRV OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=6ZRV FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.88Å</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=6zrv FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=6zrv OCA], [https://pdbe.org/6zrv PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=6zrv RCSB], [https://www.ebi.ac.uk/pdbsum/6zrv PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=6zrv ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | Plasminogen activator inhibitor-1 (PAI-1) is the main physiological inhibitor of tissue-type (tPA) and urokinase-type (uPA) plasminogen activators (PAs). Apart from being critically involved in fibrinolysis and wound healing, emerging evidence indicates that PAI-1 plays an important role in many diseases, including cardiovascular disease, tissue fibrosis, and cancer. Targeting PAI-1 is therefore a promising therapeutic strategy in PAI-1 related pathologies. Despite ongoing efforts no PAI-1 inhibitors were approved to date for therapeutic use in humans. A better understanding of the molecular mechanisms of PAI-1 inhibition is therefore necessary to guide the rational design of PAI-1 modulators. Here, we present a 1.9 A crystal structure of PAI-1 in complex with an inhibitory nanobody VHH-s-a93 (Nb93). Structural analysis in combination with biochemical characterization reveals that Nb93 directly interferes with PAI-1/PA complex formation and stabilizes the active conformation of the PAI-1 molecule. | ||
| - | + | Structural Insights into the Mechanism of a Nanobody That Stabilizes PAI-1 and Modulates Its Activity.,Sillen M, Weeks SD, Strelkov SV, Declerck PJ Int J Mol Sci. 2020 Aug 15;21(16):5859. doi: 10.3390/ijms21165859. PMID:32824134<ref>PMID:32824134</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: Declerck | + | <div class="pdbe-citations 6zrv" style="background-color:#fffaf0;"></div> |
| - | [[Category: Sillen | + | |
| - | [[Category: Strelkov | + | ==See Also== |
| - | [[Category: Weeks | + | *[[Plasminogen activator inhibitor|Plasminogen activator inhibitor]] |
| + | == References == | ||
| + | <references/> | ||
| + | __TOC__ | ||
| + | </StructureSection> | ||
| + | [[Category: Homo sapiens]] | ||
| + | [[Category: Large Structures]] | ||
| + | [[Category: Vicugna pacos]] | ||
| + | [[Category: Declerck PJ]] | ||
| + | [[Category: Sillen M]] | ||
| + | [[Category: Strelkov SV]] | ||
| + | [[Category: Weeks SD]] | ||
Current revision
Crystal Structure of Stabilized Active Plasminogen Activator Inhibitor-1 (PAI-1-W175F) in Complex with an Inhibitory Nanobody (VHH-s-a93, Nb93)
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