4eox

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==X-ray Structure of Polypeptide Deformylase Bound to a Acylprolinamide inhibitor==
==X-ray Structure of Polypeptide Deformylase Bound to a Acylprolinamide inhibitor==
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<StructureSection load='4eox' size='340' side='right' caption='[[4eox]], [[Resolution|resolution]] 1.78&Aring;' scene=''>
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<StructureSection load='4eox' size='340' side='right'caption='[[4eox]], [[Resolution|resolution]] 1.78&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
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<table><tr><td colspan='2'>[[4eox]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Strr6 Strr6]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EOX OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4EOX FirstGlance]. <br>
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<table><tr><td colspan='2'>[[4eox]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Streptococcus_pneumoniae_R6 Streptococcus pneumoniae R6]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4EOX OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=4EOX FirstGlance]. <br>
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</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=0S5:N-BENZOYL-1-[(2R)-3-CYCLOPENTYL-2-{[FORMYL(HYDROXY)AMINO]METHYL}PROPANOYL]-L-PROLINAMIDE'>0S5</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene></td></tr>
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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]] 1.783&#8491;</td></tr>
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<tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">def, spr1310 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=171101 STRR6])</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=0S5:N-BENZOYL-1-[(2R)-3-CYCLOPENTYL-2-{[FORMYL(HYDROXY)AMINO]METHYL}PROPANOYL]-L-PROLINAMIDE'>0S5</scene>, <scene name='pdbligand=NI:NICKEL+(II)+ION'>NI</scene></td></tr>
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<tr id='activity'><td class="sblockLbl"><b>Activity:</b></td><td class="sblockDat"><span class='plainlinks'>[http://en.wikipedia.org/wiki/Peptide_deformylase Peptide deformylase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.5.1.88 3.5.1.88] </span></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=4eox FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4eox OCA], [https://pdbe.org/4eox PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=4eox RCSB], [https://www.ebi.ac.uk/pdbsum/4eox PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=4eox ProSAT]</span></td></tr>
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<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=4eox FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4eox OCA], [http://pdbe.org/4eox PDBe], [http://www.rcsb.org/pdb/explore.do?structureId=4eox RCSB], [http://www.ebi.ac.uk/pdbsum/4eox PDBsum], [http://prosat.h-its.org/prosat/prosatexe?pdbcode=4eox ProSAT]</span></td></tr>
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</table>
</table>
== Function ==
== Function ==
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[[http://www.uniprot.org/uniprot/DEF_STRR6 DEF_STRR6]] Removes the formyl group from the N-terminal Met of newly synthesized proteins. Requires at least a dipeptide for an efficient rate of reaction. N-terminal L-methionine is a prerequisite for activity but the enzyme has broad specificity at other positions (By similarity).
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[https://www.uniprot.org/uniprot/DEF_STRR6 DEF_STRR6] Removes the formyl group from the N-terminal Met of newly synthesized proteins. Requires at least a dipeptide for an efficient rate of reaction. N-terminal L-methionine is a prerequisite for activity but the enzyme has broad specificity at other positions (By similarity).
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<div style="background-color:#fffaf0;">
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== Publication Abstract from PubMed ==
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A new class of PDF inhibitor with potent, broad spectrum antibacterial activity is described. Optimization of blood stability and potency provided compounds with improved pharmacokinetics that were suitable for in vivo experiments. Compound 5c, which has robust antibacterial activity, demonstrated efficacy in two respiratory tract infection models.
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Acylprolinamides: A new class of peptide deformylase inhibitors with in vivo antibacterial activity.,Axten JM, Medina JR, Blackledge CW, Duquenne C, Grant SW, Bobko MA, Peng T, Miller WH, Pinckney T, Gallagher TF, Kulkarni S, Lewandowski T, Van Aller GS, Zonis R, Ward P, Campobasso N Bioorg Med Chem Lett. 2012 Jun 15;22(12):4028-32. Epub 2012 Apr 25. PMID:22579486<ref>PMID:22579486</ref>
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From MEDLINE&reg;/PubMed&reg;, a database of the U.S. National Library of Medicine.<br>
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</div>
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<div class="pdbe-citations 4eox" style="background-color:#fffaf0;"></div>
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== References ==
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<references/>
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__TOC__
__TOC__
</StructureSection>
</StructureSection>
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[[Category: Peptide deformylase]]
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[[Category: Large Structures]]
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[[Category: Strr6]]
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[[Category: Streptococcus pneumoniae R6]]
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[[Category: Campobasso, N]]
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[[Category: Campobasso N]]
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[[Category: Ward, P]]
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[[Category: Ward P]]
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[[Category: Alpha-beta]]
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[[Category: Hydrolase-hydrolase inhibitor complex]]
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[[Category: Peptide deformylase metal ion binding]]
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Current revision

X-ray Structure of Polypeptide Deformylase Bound to a Acylprolinamide inhibitor

PDB ID 4eox

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