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Literature DB >> 24900523

Dual Inhibitor of MurD and MurE Ligases from Escherichia coli and Staphylococcus aureus.

Tihomir Tomašić¹, Roman Sink¹, Nace Zidar¹, Anja Fic¹, Carlos Contreras-Martel², Andréa Dessen², Delphine Patin³, Didier Blanot³, Manica Müller-Premru⁴, Stanislav Gobec¹, Anamarija Zega¹, Danijel Kikelj¹, Lucija Peterlin Mašič¹.

Abstract

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 μM) possessing antibacterial activity against Gram-positive S. aureus and its methicillin-resistant strain (MRSA) with minimal inhibitory concentration (MIC) values of 8 μg/mL. The inhibitor was also found to be noncytotoxic for human HepG2 cells at concentrations below 200 μM.

Entities: Chemical Species

Keywords: 2-thioxothiazolidin-4-one; Mur ligase; antibacterial agent; inhibitor; peptidoglycan

Year: 2012 PMID： 24900523 PMCID： PMC4025807 DOI： 10.1021/ml300047h

Source DB: PubMed Journal: ACS Med Chem Lett ISSN： 1948-5875 Impact factor: 4.345

26 in total

1. Role of the ortholog and paralog amino acid invariants in the active site of the UDP-MurNAc-L-alanine:D-glutamate ligase (MurD).

Authors: A Bouhss; S Dementin; C Parquet; D Mengin-Lecreulx; J A Bertrand; D Le Beller; O Dideberg; J van Heijenoort; D Blanot
Journal: Biochemistry Date: 1999-09-21 Impact factor: 3.162

Review 2. The bacterial cell wall as a source of antibacterial targets.

Authors: David W Green
Journal: Expert Opin Ther Targets Date: 2002-02 Impact factor: 6.902

Review 3. Structure, function and dynamics in the mur family of bacterial cell wall ligases.

Authors: Clyde A Smith
Journal: J Mol Biol Date: 2006-08-01 Impact factor: 5.469

Review 4. Challenges of antibacterial discovery.

Authors: Lynn L Silver
Journal: Clin Microbiol Rev Date: 2011-01 Impact factor: 26.132

5. Invariant amino acids in the Mur peptide synthetases of bacterial peptidoglycan synthesis and their modification by site-directed mutagenesis in the UDP-MurNAc:L-alanine ligase from Escherichia coli.

Authors: A Bouhss; D Mengin-Lecreulx; D Blanot; J van Heijenoort; C Parquet
Journal: Biochemistry Date: 1997-09-30 Impact factor: 3.162

6. Determination of the MurD mechanism through crystallographic analysis of enzyme complexes.

Authors: J A Bertrand; G Auger; L Martin; E Fanchon; D Blanot; D Le Beller; J van Heijenoort; O Dideberg
Journal: J Mol Biol Date: 1999-06-11 Impact factor: 5.469

7. Kinetic mechanism of the Escherichia coli UDPMurNAc-tripeptide D-alanyl-D-alanine-adding enzyme: use of a glutathione S-transferase fusion.

Authors: M S Anderson; S S Eveland; H R Onishi; D L Pompliano
Journal: Biochemistry Date: 1996-12-17 Impact factor: 3.162

8. NMR and molecular dynamics study of the binding mode of naphthalene-N-sulfonyl-D-glutamic acid derivatives: novel MurD ligase inhibitors.

Authors: Mihael Simcic; Milan Hodoscek; Jan Humljan; Katja Kristan; Uros Urleb; Darko Kocjan; Simona Golic Grdadolnik
Journal: J Med Chem Date: 2009-05-14 Impact factor: 7.446

9. Discovery of novel benzene 1,3-dicarboxylic acid inhibitors of bacterial MurD and MurE ligases by structure-based virtual screening approach.

Authors: Andrej Perdih; Andreja Kovac; Gerhard Wolber; Didier Blanot; Stanislav Gobec; Tom Solmajer
Journal: Bioorg Med Chem Lett Date: 2009-04-01 Impact factor: 2.823

10. Phosphorylated hydroxyethylamines as novel inhibitors of the bacterial cell wall biosynthesis enzymes MurC to MurF.

Authors: Matej Sova; Andreja Kovac; Samo Turk; Martina Hrast; Didier Blanot; Stanislav Gobec
Journal: Bioorg Chem Date: 2009-09-10 Impact factor: 5.275

9 in total

1. Furan-based benzene mono- and dicarboxylic acid derivatives as multiple inhibitors of the bacterial Mur ligases (MurC-MurF): experimental and computational characterization.

Authors: Andrej Perdih; Martina Hrast; Kaja Pureber; Hélène Barreteau; Simona Golič Grdadolnik; Darko Kocjan; Stanislav Gobec; Tom Solmajer; Gerhard Wolber
Journal: J Comput Aided Mol Des Date: 2015-04-08 Impact factor: 3.686

Review 2. Potential Inhibitors Targeting Escherichia coli UDP-N-Acetylglucosamine Enolpyruvyl Transferase (MurA): An Overview.

Authors: Diksha Raina; Chetan Kumar; Vinod Kumar; Inshad Ali Khan; Saurabh Saran
Journal: Indian J Microbiol Date: 2021-10-29 Impact factor: 2.461

3. Conformational ensemble of a multidomain protein explored by Gd³⁺ electron paramagnetic resonance.

Authors: Tomohide Saio; Soya Hiramatsu; Mizue Asada; Hiroshi Nakagawa; Kazumi Shimizu; Hiroyuki Kumeta; Toshikazu Nakamura; Koichiro Ishimori
Journal: Biophys J Date: 2021-07-07 Impact factor: 3.699

Review 4. Computer-Aided Drug Discovery in Plant Pathology.

Authors: Gnanendra Shanmugam; Junhyun Jeon
Journal: Plant Pathol J Date: 2017-12-01 Impact factor: 1.795

5. Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligases.

Authors: Martina Hrast; Kaja Rožman; Iza Ogris; Veronika Škedelj; Delphine Patin; Matej Sova; Hélène Barreteau; Stanislav Gobec; Simona Golič Grdadolnik; Anamarija Zega
Journal: J Enzyme Inhib Med Chem Date: 2019-12 Impact factor: 5.051