4pnc
From Proteopedia
(Difference between revisions)
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== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4pnc]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4PNC OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4PNC FirstGlance]. <br> | <table><tr><td colspan='2'>[[4pnc]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4PNC OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4PNC FirstGlance]. <br> | ||
| - | </td></tr><tr><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7NP:(2S)-7-METHOXY-2-METHYL-3,4-DIHYDRONAPHTHALEN-1(2H)-ONE'>7NP</scene>, <scene name='pdbligand=CO:COBALT+(II)+ION'>CO</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene>< | + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=7NP:(2S)-7-METHOXY-2-METHYL-3,4-DIHYDRONAPHTHALEN-1(2H)-ONE'>7NP</scene>, <scene name='pdbligand=CO:COBALT+(II)+ION'>CO</scene>, <scene name='pdbligand=NA:SODIUM+ION'>NA</scene></td></tr> |
| - | <tr><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3mat|3mat]], [[1xnz|1xnz]], [[1yvm|1yvm]]</td></tr> | + | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[3mat|3mat]], [[1xnz|1xnz]], [[1yvm|1yvm]]</td></tr> |
| - | <tr><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Methionyl_aminopeptidase Methionyl aminopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.11.18 3.4.11.18] </span></td></tr> | + | <tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Methionyl_aminopeptidase Methionyl aminopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.11.18 3.4.11.18] </span></td></tr> |
| - | <tr><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4pnc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4pnc OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4pnc RCSB], [http://www.ebi.ac.uk/pdbsum/4pnc PDBsum]</span></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=4pnc FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4pnc OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4pnc RCSB], [http://www.ebi.ac.uk/pdbsum/4pnc PDBsum]</span></td></tr> |
| - | <table> | + | </table> |
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | We identified and characterized beta-aminoketones as prodrugs for irreversible MetAP inhibitors that are selective for the MetAP-1 subtype. beta-Aminoketones with certain structural features form alpha,beta-unsaturated ketones under physiological conditions, which bind covalently and selectively to cysteines in the S1 pocket of MetAP-1. The binding mode was confirmed by X-ray crystallography and assays with the MetAPs from Escherichia coli, Staphylococcus aureus and both human isoforms. The initially identified tetralone derivatives showed complete selectivity for E. coli MetAP versus human MetAP-1 and MetAP-2. Rational design of indanone analogs yielded compounds with selectivity for the human type-1 versus the human type-2 MetAP. | ||
| + | |||
| + | Beta-aminoketones as prodrugs for selective irreversible inhibitors of type-1 methionine aminopeptidases.,Altmeyer M, Amtmann E, Heyl C, Marschner A, Scheidig AJ, Klein CD Bioorg Med Chem Lett. 2014 Sep 23. pii: S0960-894X(14)00990-1. doi:, 10.1016/j.bmcl.2014.09.047. PMID:25293447<ref>PMID:25293447</ref> | ||
| + | |||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
| + | == References == | ||
| + | <references/> | ||
__TOC__ | __TOC__ | ||
</StructureSection> | </StructureSection> | ||
[[Category: Methionyl aminopeptidase]] | [[Category: Methionyl aminopeptidase]] | ||
[[Category: Altmeyer, M.]] | [[Category: Altmeyer, M.]] | ||
| - | [[Category: Klein, C | + | [[Category: Klein, C D.]] |
| - | [[Category: Scheidig, A | + | [[Category: Scheidig, A J.]] |
[[Category: 1-tetralone]] | [[Category: 1-tetralone]] | ||
[[Category: Covalent inhibitor]] | [[Category: Covalent inhibitor]] | ||
Revision as of 06:48, 5 November 2014
E. COLI METHIONINE AMINOPEPTIDASE IN COMPLEX WITH INHIBITOR 7-METHOXY-2-METHYLEN-3,4-DIHYDRONAPHTHALEN-1(2H)-ONE
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