FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1966207966> ?p ?o ?g. }

• W1966207966 endingPage "e56926" @default.
• W1966207966 startingPage "e56926" @default.
• W1966207966 abstract "The worldwide dissemination of CTX-M type β-lactamases is a threat to human health. Previously, we have reported the spread of bla(CTX-M-15) gene in different clinical strains of Enterobacteriaceae from the hospital settings of Aligarh in north India. In view of the varying resistance pattern against cephalosporins and other β-lactam antibiotics, we intended to understand the correlation between MICs and catalytic activity of CTX-M-15. In this study, steady-state kinetic parameters and MICs were determined on E. coli DH5α transformed with bla(CTX-M-15) gene that was cloned from Enterobacter cloacae (EC-15) strain of clinical background. The effect of conventional β-lactamase inhibitors (clavulanic acid, sulbactam and tazobactam) on CTX-M-15 was also studied. We have found that tazobactam is the best among these inhibitors against CTX-M-15. The inhibition characteristic of tazobactam is defined by its very low IC(50) value (6 nM), high affinity (K(i) = 0.017 µM) and better acylation efficiency (k(+2)/K' = 0.44 µM(-1)s(-1)). It forms an acyl-enzyme covalent complex, which is quite stable (k(+3) = 0.0057 s(-1)). Since increasing resistance has been reported against conventional β-lactam antibiotic-inhibitor combinations, we aspire to design a non-β-lactam core containing β-lactamase inhibitor. For this, we screened ZINC database and performed molecular docking to identify a potential non-β-lactam based inhibitor (ZINC03787097). The MICs of cephalosporin antibiotics in combination with this inhibitor gave promising results. Steady-state kinetics and molecular docking studies showed that ZINC03787097 is a reversible inhibitor which binds non-covalently to the active site of the enzyme through hydrogen bonds and hydrophobic interactions. Though, it's IC(50) (180 nM) is much higher than tazobactam, it has good affinity for CTX-M-15 (K(i) = 0.388 µM). This study concludes that ZINC03787097 compound can be used as seed molecule to design more efficient non-β-lactam containing β-lactamase inhibitor that could evade pre-existing bacterial resistance mechanisms." @default.
• W1966207966 created "2016-06-24" @default.
• W1966207966 creator A5001487177 @default.
• W1966207966 creator A5044713051 @default.
• W1966207966 creator A5052778864 @default.
• W1966207966 creator A5055895921 @default.
• W1966207966 date "2013-02-21" @default.
• W1966207966 modified "2023-09-25" @default.
• W1966207966 title "Biochemical Characterization of CTX-M-15 from Enterobacter cloacae and Designing a Novel Non-β-Lactam-β-Lactamase Inhibitor" @default.
• W1966207966 cites W1966015663 @default.
• W1966207966 cites W1985202881 @default.
• W1966207966 cites W2047709322 @default.
• W1966207966 cites W2069017848 @default.
• W1966207966 cites W2071605785 @default.
• W1966207966 cites W2097041258 @default.
• W1966207966 cites W2153848674 @default.
• W1966207966 cites W2222312033 @default.
• W1966207966 cites W44466508 @default.
• W1966207966 doi "https://doi.org/10.1371/journal.pone.0056926" @default.
• W1966207966 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/3875596" @default.
• W1966207966 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/23437273" @default.
• W1966207966 hasPublicationYear "2013" @default.
• W1966207966 type Work @default.
• W1966207966 sameAs 1966207966 @default.
• W1966207966 citedByCount "47" @default.
• W1966207966 countsByYear W19662079662013 @default.
• W1966207966 countsByYear W19662079662014 @default.
• W1966207966 countsByYear W19662079662015 @default.
• W1966207966 countsByYear W19662079662016 @default.
• W1966207966 countsByYear W19662079662017 @default.
• W1966207966 countsByYear W19662079662018 @default.
• W1966207966 countsByYear W19662079662019 @default.
• W1966207966 countsByYear W19662079662020 @default.
• W1966207966 countsByYear W19662079662021 @default.
• W1966207966 countsByYear W19662079662022 @default.
• W1966207966 countsByYear W19662079662023 @default.
• W1966207966 crossrefType "journal-article" @default.
• W1966207966 hasAuthorship W1966207966A5001487177 @default.
• W1966207966 hasAuthorship W1966207966A5044713051 @default.
• W1966207966 hasAuthorship W1966207966A5052778864 @default.
• W1966207966 hasAuthorship W1966207966A5055895921 @default.
• W1966207966 hasBestOaLocation W19662079661 @default.
• W1966207966 hasConcept C104317684 @default.
• W1966207966 hasConcept C185592680 @default.
• W1966207966 hasConcept C2776124114 @default.
• W1966207966 hasConcept C2777402170 @default.
• W1966207966 hasConcept C2777406300 @default.
• W1966207966 hasConcept C2778266534 @default.
• W1966207966 hasConcept C2778478555 @default.
• W1966207966 hasConcept C2778910516 @default.
• W1966207966 hasConcept C2778983983 @default.
• W1966207966 hasConcept C2779454058 @default.
• W1966207966 hasConcept C2779489039 @default.
• W1966207966 hasConcept C2779631663 @default.
• W1966207966 hasConcept C2779708577 @default.
• W1966207966 hasConcept C2910641391 @default.
• W1966207966 hasConcept C501593827 @default.
• W1966207966 hasConcept C523546767 @default.
• W1966207966 hasConcept C54355233 @default.
• W1966207966 hasConcept C547475151 @default.
• W1966207966 hasConcept C55493867 @default.
• W1966207966 hasConcept C64778159 @default.
• W1966207966 hasConcept C86803240 @default.
• W1966207966 hasConcept C89423630 @default.
• W1966207966 hasConcept C94665300 @default.
• W1966207966 hasConceptScore W1966207966C104317684 @default.
• W1966207966 hasConceptScore W1966207966C185592680 @default.
• W1966207966 hasConceptScore W1966207966C2776124114 @default.
• W1966207966 hasConceptScore W1966207966C2777402170 @default.
• W1966207966 hasConceptScore W1966207966C2777406300 @default.
• W1966207966 hasConceptScore W1966207966C2778266534 @default.
• W1966207966 hasConceptScore W1966207966C2778478555 @default.
• W1966207966 hasConceptScore W1966207966C2778910516 @default.
• W1966207966 hasConceptScore W1966207966C2778983983 @default.
• W1966207966 hasConceptScore W1966207966C2779454058 @default.
• W1966207966 hasConceptScore W1966207966C2779489039 @default.
• W1966207966 hasConceptScore W1966207966C2779631663 @default.
• W1966207966 hasConceptScore W1966207966C2779708577 @default.
• W1966207966 hasConceptScore W1966207966C2910641391 @default.
• W1966207966 hasConceptScore W1966207966C501593827 @default.
• W1966207966 hasConceptScore W1966207966C523546767 @default.
• W1966207966 hasConceptScore W1966207966C54355233 @default.
• W1966207966 hasConceptScore W1966207966C547475151 @default.
• W1966207966 hasConceptScore W1966207966C55493867 @default.
• W1966207966 hasConceptScore W1966207966C64778159 @default.
• W1966207966 hasConceptScore W1966207966C86803240 @default.
• W1966207966 hasConceptScore W1966207966C89423630 @default.
• W1966207966 hasConceptScore W1966207966C94665300 @default.
• W1966207966 hasIssue "2" @default.
• W1966207966 hasLocation W19662079661 @default.
• W1966207966 hasLocation W19662079662 @default.
• W1966207966 hasLocation W19662079663 @default.
• W1966207966 hasLocation W19662079664 @default.
• W1966207966 hasLocation W19662079665 @default.
• W1966207966 hasOpenAccess W1966207966 @default.
• W1966207966 hasPrimaryLocation W19662079661 @default.
• W1966207966 hasRelatedWork W1965256508 @default.
• W1966207966 hasRelatedWork W1966207966 @default.

• next