4ucm: Difference between revisions

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==CRYSTAL STRUCTURE OF LEISHMANIA MAJOR N-MYRISTOYLTRANSFERASE (NMT) WITH BOUND MYRISTOYL-COA AND A FRAGMENT==
==CRYSTAL STRUCTURE OF LEISHMANIA MAJOR N-MYRISTOYLTRANSFERASE (NMT) WITH BOUND MYRISTOYL-COA AND A FRAGMENT==
<StructureSection load='4ucm' size='340' side='right' caption='[[4ucm]], [[Resolution|resolution]] 2.32&Aring;' scene=''>
<StructureSection load='4ucm' size='340' side='right'caption='[[4ucm]], [[Resolution|resolution]] 2.32&Aring;' scene=''>
== Structural highlights ==
== Structural highlights ==
<table><tr><td colspan='2'>[[4ucm]] is a 1 chain structure. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=4UCM OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4UCM FirstGlance]. <br>
<table><tr><td colspan='2'>[[4ucm]] 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=4UCM OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=4UCM FirstGlance]. <br>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene>, <scene name='pdbligand=X6W:METHYL-3-METHYL-5-PHENYL-2H-PYRAZOL-4-METHYL+AMINE'>X6W</scene></td></tr>
</td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=MYA:TETRADECANOYL-COA'>MYA</scene>, <scene name='pdbligand=X6W:METHYL-3-METHYL-5-PHENYL-2H-PYRAZOL-4-METHYL+AMINE'>X6W</scene></td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4ucn|4ucn]], [[4ucp|4ucp]]</td></tr>
<tr id='related'><td class="sblockLbl"><b>[[Related_structure|Related:]]</b></td><td class="sblockDat">[[4ucn|4ucn]], [[4ucp|4ucp]]</td></tr>
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</StructureSection>
</StructureSection>
[[Category: Glycylpeptide N-tetradecanoyltransferase]]
[[Category: Glycylpeptide N-tetradecanoyltransferase]]
[[Category: Large Structures]]
[[Category: Leima]]
[[Category: Robinson, D A]]
[[Category: Robinson, D A]]
[[Category: Wyatt, P G]]
[[Category: Wyatt, P G]]

Revision as of 11:38, 21 May 2019

CRYSTAL STRUCTURE OF LEISHMANIA MAJOR N-MYRISTOYLTRANSFERASE (NMT) WITH BOUND MYRISTOYL-COA AND A FRAGMENTCRYSTAL STRUCTURE OF LEISHMANIA MAJOR N-MYRISTOYLTRANSFERASE (NMT) WITH BOUND MYRISTOYL-COA AND A FRAGMENT

Structural highlights

4ucm is a 1 chain structure with sequence from Leima. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
Ligands:,
Activity:Glycylpeptide N-tetradecanoyltransferase, with EC number 2.3.1.97
Resources:FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT

Function

[Q4Q5S8_LEIMA] Adds a myristoyl group to the N-terminal glycine residue of certain cellular proteins (By similarity).

Publication Abstract from PubMed

Trypanosoma brucei N-myristoyltransferase (TbNMT) is an attractive therapeutic target for the treatment of human African trypanosomiasis. Pyrazole sulfonamide (DDD85646), a potent inhibitor of TbNMT, has been identified in previous studies; however, poor central nervous system exposure restricts its use to the haemolymphatic form (stage 1) of the disease. In order to identify new chemical matter, a fragment screen was carried out by ligand-observed NMR spectroscopy, identifying hits that occupy the DDD85646 binding site. Crystal structures of hits from this assay have been obtained in complex with the closely related NMT from Leishmania major, providing a structural starting point for the evolution of novel chemical matter.

Identification and structure solution of fragment hits against kinetoplastid N-myristoyltransferase.,Robinson DA, Wyatt PG Acta Crystallogr F Struct Biol Commun. 2015 May;71(Pt 5):586-93. doi:, 10.1107/S2053230X15003040. Epub 2015 Apr 21. PMID:25945713[1]

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

References

  1. Robinson DA, Wyatt PG. Identification and structure solution of fragment hits against kinetoplastid N-myristoyltransferase. Acta Crystallogr F Struct Biol Commun. 2015 May;71(Pt 5):586-93. doi:, 10.1107/S2053230X15003040. Epub 2015 Apr 21. PMID:25945713 doi:http://dx.doi.org/10.1107/S2053230X15003040

4ucm, resolution 2.32Å

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OCA