4k5o: Difference between revisions
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<StructureSection load='4k5o' size='340' side='right'caption='[[4k5o]], [[Resolution|resolution]] 1.90Å' scene=''> | <StructureSection load='4k5o' size='340' side='right'caption='[[4k5o]], [[Resolution|resolution]] 1.90Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4k5o]] is a 1 chain structure with sequence from [ | <table><tr><td colspan='2'>[[4k5o]] 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=4K5O OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4K5O FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=1OT:{(R)-AMINO[4-(1H-PYRAZOL-1-YL)PHENYL]METHYL}PHOSPHONIC+ACID'>1OT</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><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.9Å</td></tr> | ||
<tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=1OT:{(R)-AMINO[4-(1H-PYRAZOL-1-YL)PHENYL]METHYL}PHOSPHONIC+ACID'>1OT</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> | |||
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[ | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=4k5o FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4k5o OCA], [https://pdbe.org/4k5o PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4k5o RCSB], [https://www.ebi.ac.uk/pdbsum/4k5o PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4k5o ProSAT]</span></td></tr> | ||
</table> | </table> | ||
== Function == | == Function == | ||
[ | [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> | ||
<div style="background-color:#fffaf0;"> | <div style="background-color:#fffaf0;"> | ||
== Publication Abstract from PubMed == | == Publication Abstract from PubMed == | ||
| Line 27: | Line 27: | ||
</StructureSection> | </StructureSection> | ||
[[Category: Large Structures]] | [[Category: Large Structures]] | ||
[[Category: | [[Category: Plasmodium falciparum FcB1/Columbia]] | ||
[[Category: McGowan | [[Category: McGowan S]] | ||
Latest revision as of 18:54, 20 September 2023
Phosphonic Arginine Mimetics as Inhibitors of the M1 Aminopeptidases from Plasmodium falciparumPhosphonic Arginine Mimetics as Inhibitors of the M1 Aminopeptidases from Plasmodium falciparum
Structural highlights
FunctionAMP1_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.[1] [2] Publication Abstract from PubMedThe malaria parasite <i>Plasmodium falciparum</i> employs two metallo-aminopeptidases, P<i>f</i>A-M1 and P<I>f</i>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. Synthesis and Structure-Activity Relationships of Phosphonic Arginine Mimetics as Inhibitors of the M1 and M17 Aminopeptidases from <i>Plasmodium falciparum</i>,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[3] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See AlsoReferences
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