4x2u: Difference between revisions

From Proteopedia
Jump to navigationJump to search
← Older editNewer edit →
OCA (talk | contribs)
Bots, Bureaucrats, journal, Administrators
3,330,738 edits
No edit summary
OCA (talk | contribs)
Bots, Bureaucrats, journal, Administrators
3,330,738 edits
No edit summary
Line 1: Line 1:
'''Unreleased structure'''
==X-ray crystal structure of the orally available aminopeptidase inhibitor, Tosedostat, bound to the M1 Alanyl Aminopeptidase from P. falciparum==
<StructureSection load='4x2u' size='340' side='right' caption='[[4x2u]], [[Resolution|resolution]] 1.60&Aring;' scene=''>
== Structural highlights ==
<table><tr><td colspan='2'>[[4x2u]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4X2U OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4X2U FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=GOL:GLYCEROL'>GOL</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=TOD:(2S)-({(2R)-2-[(1S)-1-HYDROXY-2-(HYDROXYAMINO)-2-OXOETHYL]-4-METHYLPENTANOYL}AMINO)(PHENYL)ETHANOIC+ACID'>TOD</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene></td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3ebg|3ebg]], [[3ebh|3ebh]], [[4x2t|4x2t]]</td></tr>
<tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4x2u FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4x2u OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4x2u RCSB], [http://www.ebi.ac.uk/pdbsum/4x2u PDBsum]</span></td></tr>
</table>
== Function ==
[[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> 
<div style="background-color:#fffaf0;">
== Publication Abstract from PubMed ==
New antimalarial treatments are desperately required to face the spread of drug resistant parasites. Inhibition of metalloaminopeptidases PfA-M1 and PfA-M17 is a validated therapeutic strategy for treatment of Plasmodium falciparum malaria. Here we describe the crystal structures of PfA-M1 and PfA-M17 bound to chemotherapeutic agent Tosedostat. The inhibitor occupies the enzymes' putative product egress channels in addition to the substrate binding pockets; however, adopts different binding poses when bound to PfA-M1 and PfA-M17. These findings will be valuable for the continued development of selective inhibitors of PfA-M1 and PfA-M17. This article is protected by copyright. All rights reserved.


The entry 4x2u is ON HOLD  until Paper Publication
X-ray crystal structures of an orally available aminopeptidase inhibitor, Tosedostat, bound to anti-malarial drug targets PfA-M1 and PfA-M17.,Drinkwater N, Bamert RS, Kannan Sivaraman K, Paiardini A, McGowan S Proteins. 2015 Feb 2. doi: 10.1002/prot.24771. PMID:25645579<ref>PMID:25645579</ref>


Authors: Drinkwater, N., McGowan, S.
From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
 
</div>
Description:
== References ==
[[Category: Unreleased Structures]]
<references/>
__TOC__
</StructureSection>
[[Category: Drinkwater, N]]
[[Category: Drinkwater, N]]
[[Category: Mcgowan, S]]
[[Category: McGowan, S]]
[[Category: Antimalarial]]
[[Category: Hydrolase-hydrolase inhibitor complex]]
[[Category: Inhibitor]]
[[Category: M1 alanyl-aminopeptidase]]
[[Category: Plasmodium falciparum]]
[[Category: Protease]]
[[Category: Tosedostat]]
Retrieved from "https://proteopedia.org/4x2u"