| Structural highlights
2y1o is a 1 chain structure with sequence from [alpha Escherichia coli dh5[alpha]]. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance.
| | Ligands: | , , |
| NonStd Res: | |
| Related: | 2wjp, 2vtd, 2uuo, 2jfg, 1uag, 4uag, 2uag, 2jfh, 3uag, 2uup, 1e0d, 2vte, 2jff, 2x5o, 1eeh |
| Activity: | UDP-N-acetylmuramoyl-L-alanine--D-glutamate ligase, with EC number 6.3.2.9 |
| Resources: | FirstGlance, OCA, PDBe, RCSB, PDBsum, ProSAT |
Function
[MURD_ECOLI] Cell wall formation. Catalyzes the addition of glutamate to the nucleotide precursor UDP-N-acetylmuramoyl-L-alanine (UMA).[HAMAP-Rule:MF_00639]
Publication Abstract from PubMed
MurD and MurE ligases, consecutive enzymes participating in the intracellular steps of bacterial peptidoglycan biosynthesis, are important targets for antibacterial drug discovery. We have designed, synthesized, and evaluated the first d-glutamic acid-containing dual inhibitor of MurD and MurE ligases from Escherichia coli and Staphylococcus aureus (IC50 values between 6.4 and 180 muM) possessing antibacterial activity against Gram-positive S. aureus and its methicillin-resistant strain (MRSA) with minimal inhibitory concentration (MIC) values of 8 mug/mL. The inhibitor was also found to be noncytotoxic for human HepG2 cells at concentrations below 200 muM.
Dual Inhibitor of MurD and MurE Ligases from Escherichia coli and Staphylococcus aureus.,Tomasic T, Sink R, Zidar N, Fic A, Contreras-Martel C, Dessen A, Patin D, Blanot D, Muller-Premru M, Gobec S, Zega A, Kikelj D, Masic LP ACS Med Chem Lett. 2012 Jun 27;3(8):626-30. doi: 10.1021/ml300047h. eCollection, 2012 Aug 9. PMID:24900523[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Tomasic T, Sink R, Zidar N, Fic A, Contreras-Martel C, Dessen A, Patin D, Blanot D, Muller-Premru M, Gobec S, Zega A, Kikelj D, Masic LP. Dual Inhibitor of MurD and MurE Ligases from Escherichia coli and Staphylococcus aureus. ACS Med Chem Lett. 2012 Jun 27;3(8):626-30. doi: 10.1021/ml300047h. eCollection, 2012 Aug 9. PMID:24900523 doi:http://dx.doi.org/10.1021/ml300047h
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