4k5m

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{{STRUCTURE_4k5m| PDB=4k5m | SCENE= }}
 
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===Phosphonic Arginine Mimetics as Inhibitors of the M1 Aminopeptidases from Plasmodium falciparum===
 
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{{ABSTRACT_PUBMED_23713488}}
 
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==Function==
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==Phosphonic Arginine Mimetics as Inhibitors of the M1 Aminopeptidases from Plasmodium falciparum==
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[[http://www.uniprot.org/uniprot/AMP1_PLAFQ AMP1_PLAFQ]] Displays aminopeptidase activity with a broad substrate specificity. Preferentially hydrolyzes L-Lys-AMC but also shows strong activity against L-Ala-AMC, L-Arg-AMC and L-Leu-AMC.<ref>PMID:12166515</ref> <ref>PMID:19196988</ref>
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<StructureSection load='4k5m' size='340' side='right'caption='[[4k5m]], [[Resolution|resolution]] 1.75&Aring;' scene=''>
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== Structural highlights ==
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<table><tr><td colspan='2'>[[4k5m]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Plasmodium_falciparum_FcB1/Columbia Plasmodium falciparum FcB1/Columbia]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4K5M OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4K5M 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]] 1.75&#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=1OV:[(1R)-1-AMINO-4-CARBAMIMIDAMIDOBUTYL]PHOSPHONIC+ACID'>1OV</scene>, <scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</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=4k5m FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4k5m OCA], [https://pdbe.org/4k5m PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4k5m RCSB], [https://www.ebi.ac.uk/pdbsum/4k5m PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4k5m ProSAT]</span></td></tr>
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</table>
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== Function ==
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[https://www.uniprot.org/uniprot/AMP1_PLAFQ AMP1_PLAFQ] Displays aminopeptidase activity with a broad substrate specificity. Preferentially hydrolyzes L-Lys-AMC but also shows strong activity against L-Ala-AMC, L-Arg-AMC and L-Leu-AMC.<ref>PMID:12166515</ref> <ref>PMID:19196988</ref>
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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The malaria parasite &lt;i&gt;Plasmodium falciparum&lt;/i&gt; employs two metallo-aminopeptidases, P&lt;i&gt;f&lt;/i&gt;A-M1 and P&lt;I&gt;f&lt;/i&gt;A-M17, which are essential for parasite survival. Compounds that inhibit the activity of either enzyme represent leads for the development of new anti-malarial drugs. Here we report the synthesis and structure-activity-relationships of a small library of phosphonic acid arginine mimetics that probe the S1 pocket of both enzymes, and map the necessary interactions that would be important for a dual inhibitor.
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==About this Structure==
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Synthesis and Structure-Activity Relationships of Phosphonic Arginine Mimetics as Inhibitors of the M1 and M17 Aminopeptidases from &lt;i&gt;Plasmodium falciparum&lt;/i&gt;,Kannan Sivaraman K, Paiardini A, Sienczyk M, Ruggeri C, Oellig CA, Dalton JP, Scammells PJ, Drag M, McGowan S J Med Chem. 2013 May 28. PMID:23713488<ref>PMID:23713488</ref>
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[[4k5m]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Plasmodium_falciparum_fcb1/columbia Plasmodium falciparum fcb1/columbia]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4K5M OCA].
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==Reference==
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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<ref group="xtra">PMID:023713488</ref><references group="xtra"/><references/>
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</div>
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[[Category: Plasmodium falciparum fcb1/columbia]]
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<div class="pdbe-citations 4k5m" style="background-color:#fffaf0;"></div>
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[[Category: McGowan, S.]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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==See Also==
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[[Category: M1 alanyl-aminopeptidase]]
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*[[Aminopeptidase 3D structures|Aminopeptidase 3D structures]]
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[[Category: Protease]]
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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: Large Structures]]
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[[Category: Plasmodium falciparum FcB1/Columbia]]
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[[Category: McGowan S]]

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Phosphonic Arginine Mimetics as Inhibitors of the M1 Aminopeptidases from Plasmodium falciparum

PDB ID 4k5m

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