4bbh: Difference between revisions
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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=4bbh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bbh OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4bbh RCSB], [http://www.ebi.ac.uk/pdbsum/4bbh 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=4bbh FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=4bbh OCA], [http://www.rcsb.org/pdb/explore.do?structureId=4bbh RCSB], [http://www.ebi.ac.uk/pdbsum/4bbh PDBsum]</span></td></tr> | ||
</table> | </table> | ||
== Function == | |||
[[http://www.uniprot.org/uniprot/A5K1A2_PLAVS A5K1A2_PLAVS]] Adds a myristoyl group to the N-terminal glycine residue of certain cellular proteins (By similarity).[RuleBase:RU000586] | |||
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== Publication Abstract from PubMed == | == Publication Abstract from PubMed == |
Revision as of 17:53, 24 December 2014
Plasmodium vivax N-myristoyltransferase with a bound benzothiophene inhibitorPlasmodium vivax N-myristoyltransferase with a bound benzothiophene inhibitor
Structural highlights
Function[A5K1A2_PLAVS] Adds a myristoyl group to the N-terminal glycine residue of certain cellular proteins (By similarity).[RuleBase:RU000586] Publication Abstract from PubMedN-Myristoyltransferase (NMT) is an attractive anti-protozoan drug target. A lead-hopping approach was utilized in the design and synthesis of novel benzo[b]thiophene-containing inhibitors of Plasmodium falciparum (Pf) and Plasmodium vivax (Pv) NMT. These inhibitors are selective against Homo sapiens NMT1 (HsNMT), have excellent ligand efficiency (LE) and display anti-parasitic activity in vitro. The binding mode of this series was determined by crystallography and shows a novel binding mode for the benzothiophene ring. Discovery of Novel and Ligand-Efficient Inhibitors of Plasmodium falciparum and Plasmodium vivax N-Myristoyltransferase.,Rackham MD, Brannigan JA, Moss DK, Yu Z, Wilkinson AJ, Holder AA, Tate EW, Leatherbarrow RJ J Med Chem. 2012 Nov 22. PMID:23170970[1] From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. References
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