This old version of Proteopedia is provided for student assignments while the new version is undergoing repairs. Content and edits done in this old version of Proteopedia after March 1, 2026 will eventually be lost when it is retired in about June of 2026.
Apply for new accounts at the new Proteopedia. Your logins will work in both the old and new versions.
5a27
From Proteopedia
(Difference between revisions)
(New page: '''Unreleased structure''' The entry 5a27 is ON HOLD Authors: Rackham, M.D., Yu, Z., Brannigan, J.A., Heal, W.P., Paape, D., Barker, K.V., Wilkinson, A.J., Smith, D.F., Tate, E.W., Leat...) |
|||
| (6 intermediate revisions not shown.) | |||
| Line 1: | Line 1: | ||
| - | '''Unreleased structure''' | ||
| - | + | ==Leishmania major N-myristoyltransferase in complex with a chlorophenyl 1,2,4-oxadiazole inhibitor.== | |
| + | <StructureSection load='5a27' size='340' side='right'caption='[[5a27]], [[Resolution|resolution]] 1.37Å' scene=''> | ||
| + | == Structural highlights == | ||
| + | <table><tr><td colspan='2'>[[5a27]] is a 1 chain structure with sequence from [https://en.wikipedia.org/wiki/Leishmania_major Leishmania major]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=5A27 OCA]. For a <b>guided tour on the structure components</b> use [https://proteopedia.org/fgij/fg.htm?mol=5A27 FirstGlance]. <br> | ||
| + | </td></tr><tr id='method'><td class="sblockLbl"><b>[[Empirical_models|Method:]]</b></td><td class="sblockDat" id="methodDat">X-ray diffraction, [[Resolution|Resolution]] 1.37Å</td></tr> | ||
| + | <tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat" id="ligandDat"><scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene>, <scene name='pdbligand=TUT:5-CHLORANYL-N-[2-(3-METHOXYPHENYL)ETHANIMIDOYL]-2-PIPERIDIN-4-YLOXY-BENZAMIDE'>TUT</scene></td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[https://proteopedia.org/fgij/fg.htm?mol=5a27 FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=5a27 OCA], [https://pdbe.org/5a27 PDBe], [https://www.rcsb.org/pdb/explore.do?structureId=5a27 RCSB], [https://www.ebi.ac.uk/pdbsum/5a27 PDBsum], [https://prosat.h-its.org/prosat/prosatexe?pdbcode=5a27 ProSAT]</span></td></tr> | ||
| + | </table> | ||
| + | == Function == | ||
| + | [https://www.uniprot.org/uniprot/Q4Q5S8_LEIMA Q4Q5S8_LEIMA] Adds a myristoyl group to the N-terminal glycine residue of certain cellular proteins (By similarity). | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | N-Myristoyltransferase (NMT) is a potential drug target in Leishmania parasites. Scaffold-hopping from published inhibitors yielded the serendipitous discovery of a chemotype selective for Leishmania donovani NMT; development led to high affinity inhibitors with excellent ligand efficiency. The binding mode was characterised by crystallography and provides a structural rationale for selectivity. | ||
| - | + | Discovery of high affinity inhibitors of -myristoyltransferase.,Rackham MD, Yu Z, Brannigan JA, Heal WP, Paape D, Barker KV, Wilkinson AJ, Smith DF, Leatherbarrow RJ, Tate EW Medchemcomm. 2015 Oct 8;6(10):1761-1766. Epub 2015 Aug 19. PMID:26962429<ref>PMID:26962429</ref> | |
| - | + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | |
| - | [[Category: | + | </div> |
| - | [[Category: | + | <div class="pdbe-citations 5a27" style="background-color:#fffaf0;"></div> |
| - | [[Category: | + | == References == |
| - | [[Category: | + | <references/> |
| - | [[Category: Leatherbarrow | + | __TOC__ |
| - | [[Category: | + | </StructureSection> |
| - | [[Category: Rackham | + | [[Category: Large Structures]] |
| - | [[Category: | + | [[Category: Leishmania major]] |
| - | [[Category: Tate | + | [[Category: Barker KV]] |
| - | [[Category: | + | [[Category: Brannigan JA]] |
| - | [[Category: | + | [[Category: Heal WP]] |
| + | [[Category: Leatherbarrow RJ]] | ||
| + | [[Category: Paape D]] | ||
| + | [[Category: Rackham MD]] | ||
| + | [[Category: Smith DF]] | ||
| + | [[Category: Tate EW]] | ||
| + | [[Category: Wilkinson AJ]] | ||
| + | [[Category: Yu Z]] | ||
Current revision
Leishmania major N-myristoyltransferase in complex with a chlorophenyl 1,2,4-oxadiazole inhibitor.
| |||||||||||
Categories: Large Structures | Leishmania major | Barker KV | Brannigan JA | Heal WP | Leatherbarrow RJ | Paape D | Rackham MD | Smith DF | Tate EW | Wilkinson AJ | Yu Z
