4c7h: Difference between revisions
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==Leismania major N-myristoyltransferase in complex with a peptidomimetic (-NH2) molecule== | ==Leismania major N-myristoyltransferase in complex with a peptidomimetic (-NH2) molecule== | ||
<StructureSection load='4c7h' size='340' side='right' caption='[[4c7h]], [[Resolution|resolution]] 1.40Å' scene=''> | <StructureSection load='4c7h' size='340' side='right'caption='[[4c7h]], [[Resolution|resolution]] 1.40Å' scene=''> | ||
== Structural highlights == | == Structural highlights == | ||
<table><tr><td colspan='2'>[[4c7h]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4C7H OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4C7H FirstGlance]. <br> | <table><tr><td colspan='2'>[[4c7h]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Leima Leima]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4C7H OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4C7H FirstGlance]. <br> | ||
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=COA:COENZYME+A'>COA</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EN5:N-(10-AMINODECANOYL)-L-SERYL-N-(2-CYCLOHEXYLETHYL)-L-LYSINAMIDE'>EN5</scene>, <scene name='pdbligand=ENF:N-{(5E)-10-[(9E)-TETRADEC-9-ENOYLAMINO]DEC-5-ENOYL}-L-SERYL-N-(2-CYCLOHEXYLETHYL)-L-LYSINAMIDE'>ENF</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene></td></tr> | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=COA:COENZYME+A'>COA</scene>, <scene name='pdbligand=DMS:DIMETHYL+SULFOXIDE'>DMS</scene>, <scene name='pdbligand=EN5:N-(10-AMINODECANOYL)-L-SERYL-N-(2-CYCLOHEXYLETHYL)-L-LYSINAMIDE'>EN5</scene>, <scene name='pdbligand=ENF:N-{(5E)-10-[(9E)-TETRADEC-9-ENOYLAMINO]DEC-5-ENOYL}-L-SERYL-N-(2-CYCLOHEXYLETHYL)-L-LYSINAMIDE'>ENF</scene>, <scene name='pdbligand=MG:MAGNESIUM+ION'>MG</scene>, <scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene></td></tr> | ||
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4c68|4c68]], [[4c7i|4c7i]]</td></tr> | <tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4c68|4c68]], [[4c7i|4c7i]]</td></tr> | ||
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</StructureSection> | </StructureSection> | ||
[[Category: Glycylpeptide N-tetradecanoyltransferase]] | [[Category: Glycylpeptide N-tetradecanoyltransferase]] | ||
[[Category: Large Structures]] | |||
[[Category: Leima]] | |||
[[Category: Brannigan, J A]] | [[Category: Brannigan, J A]] | ||
[[Category: Goncalves, V]] | [[Category: Goncalves, V]] | ||
Revision as of 12:31, 20 March 2019
Leismania major N-myristoyltransferase in complex with a peptidomimetic (-NH2) moleculeLeismania major N-myristoyltransferase in complex with a peptidomimetic (-NH2) molecule
Structural highlights
Function[Q4Q5S8_LEIMA] Adds a myristoyl group to the N-terminal glycine residue of certain cellular proteins (By similarity). Publication Abstract from PubMedN-Myristoyltransferase (NMT) has been shown to be essential in Leishmania and subsequently validated as a drug target in Plasmodium. Herein, we discuss the use of antifungal NMT inhibitors as a basis for inhibitor development resulting in the first sub-micromolar peptidomimetic inhibitors of Plasmodium and Leishmania NMTs. High-resolution structures of these inhibitors with Plasmodium and Leishmania NMTs permit a comparative analysis of binding modes, and provide the first crystal structure evidence for a ternary NMT-Coenzyme A/myristoylated peptide product complex. Peptidomimetic inhibitors of N-myristoyltransferase from human malaria and leishmaniasis parasites.,Olaleye TO, Brannigan JA, Roberts SM, Leatherbarrow RJ, Wilkinson AJ, Tate EW Org Biomol Chem. 2014 Sep 18. PMID:25230674[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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