Discovery of inhibitors of bacterial histidine kinases

N.R. Velikova

Research output: Thesisinternal PhD, WU

Abstract

Discovery of Inhibitors of Bacterial Histidine Kinases Summary

The thesis is on novel antibacterial drug discovery (http://youtu.be/NRMWOGgeysM). Using structure-based and fragment-based drug discovery approach, we have identified small-molecule histidine-kinase inhibitors with antibacterial effect against multi-drug resistant strains, including clinical isolates of multi-drug resistant bacteria such as MRSA. Furthermore, we have shown broadening of the antibacterial spectrum and lowering the toxicity of the histidine-kinase inhibitors using nanoparticles. The results open up exciting possibilities for development of novel antibacterial(nano)medicines.

 

Original languageEnglish
QualificationDoctor of Philosophy
Awarding Institution
  • Wageningen University
Supervisors/Advisors
  • Wells, Jerry, Promotor
  • Marina, A., Co-promotor, External person
Award date7 Nov 2014
Place of PublicationWageningen
Publisher
Print ISBNs9789462571112
Publication statusPublished - 2014

Fingerprint

Drug Discovery
Methicillin-Resistant Staphylococcus aureus
Pharmaceutical Preparations
Nanoparticles
Bacteria
Histidine Kinase

Keywords

  • host pathogen interactions
  • bacteria
  • kinases
  • histidine
  • drug resistance
  • antibiotics
  • microbiology

Cite this

Velikova, N. R. (2014). Discovery of inhibitors of bacterial histidine kinases. Wageningen: Wageningen University.
Velikova, N.R.. / Discovery of inhibitors of bacterial histidine kinases. Wageningen : Wageningen University, 2014. 225 p.
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author = "N.R. Velikova",
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Velikova, NR 2014, 'Discovery of inhibitors of bacterial histidine kinases', Doctor of Philosophy, Wageningen University, Wageningen.

Discovery of inhibitors of bacterial histidine kinases. / Velikova, N.R.

Wageningen : Wageningen University, 2014. 225 p.

Research output: Thesisinternal PhD, WU

TY - THES

T1 - Discovery of inhibitors of bacterial histidine kinases

AU - Velikova, N.R.

N1 - WU thesis 5902

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Y1 - 2014

N2 - Discovery of Inhibitors of Bacterial Histidine Kinases Summary The thesis is on novel antibacterial drug discovery (http://youtu.be/NRMWOGgeysM). Using structure-based and fragment-based drug discovery approach, we have identified small-molecule histidine-kinase inhibitors with antibacterial effect against multi-drug resistant strains, including clinical isolates of multi-drug resistant bacteria such as MRSA. Furthermore, we have shown broadening of the antibacterial spectrum and lowering the toxicity of the histidine-kinase inhibitors using nanoparticles. The results open up exciting possibilities for development of novel antibacterial(nano)medicines.  

AB - Discovery of Inhibitors of Bacterial Histidine Kinases Summary The thesis is on novel antibacterial drug discovery (http://youtu.be/NRMWOGgeysM). Using structure-based and fragment-based drug discovery approach, we have identified small-molecule histidine-kinase inhibitors with antibacterial effect against multi-drug resistant strains, including clinical isolates of multi-drug resistant bacteria such as MRSA. Furthermore, we have shown broadening of the antibacterial spectrum and lowering the toxicity of the histidine-kinase inhibitors using nanoparticles. The results open up exciting possibilities for development of novel antibacterial(nano)medicines.  

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KW - bacteriën

KW - kinasen

KW - histidine

KW - geneesmiddelresistentie

KW - antibiotica

KW - microbiologie

KW - host pathogen interactions

KW - bacteria

KW - kinases

KW - histidine

KW - drug resistance

KW - antibiotics

KW - microbiology

M3 - internal PhD, WU

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Velikova NR. Discovery of inhibitors of bacterial histidine kinases. Wageningen: Wageningen University, 2014. 225 p.