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Microbial pathogenesis v.112, 2017년, pp.221 - 229   SCI SCIE
본 등재정보는 저널의 등재정보를 참고하여 보여주는 베타서비스로 정확한 논문의 등재여부는 등재기관에 확인하시기 바랍니다.

Prevention of OprD regulated antibiotic resistance in Pseudomonas aeruginosa biofilm

Raavi (Applied Science Department, Indian Institute of Information Technology, Allahabad, 211012, India ) ; Mishra, Swechha (Department of Applied Sciences and Bioinformatics, India ) ; Singh, Sangeeta (Department of Applied Sciences and Bioinformatics, India ) ;
  • 초록  

    Abstract In P.aeruginosa biofilms, the issue of antibiotic resistance is of particular importance due to increasing number of infections being reported in medical implants. The current study is focused on CzcR and CopR proteins which are part of two-component signal transduction systems (TCSs) - CzcR–CzcS and CopR–CopS respectively in P.aeruginosa . They both negatively regulate OprD porin expression which affects the intake of antibiotics like carbapenems. These two proteins can be treated as targets to combat antibiotic resistance in P.aeruginosa. Docking was performed on these proteins in search of inhibitors against the CzcR–CzcS and CopR–CopS TCSs. Efficient inhibitory ligands were evaluated on the basis of least binding energy, human oral absorption and ADME properties using a four-tier structure based virtual screening. The resulting ligands displayed high effective inhibitory property and satisfactory pharmacokinetics as compared to inhibitors which have been identified before for two-component signal transduction systems for gram negative bacteria. These potential inhibitors can now be used further in wet lab by performing selectivity assays to determine their inhibition rate against P.aeruginosa biofilms. Identification of potential leads may enable the development of new therapeutic strategies aimed at disrupting P.aeruginosa biofilms. Highlights The effectiveness of various ligands against the protein structure of CzcR and CopR. Insilico screening against these proteins. Simulation studies for stability check.


  • 주제어

    Antibiotic resistance .   Biofilms .   Carbapenems .   P.   aeruginosa .   Two component signal transduction systems.  

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