FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3014077166> ?p ?o ?g. }

• W3014077166 abstract "Bacterial resistance to β-lactamantibiotics is largely mediated by β-lactamases, which catalyzethe hydrolysis of these drugs and continue to emerge in response toantibiotic use. β-Lactamases that hydrolyze the last resortcarbapenem class of β-lactam antibiotics (carbapenemases) area growing global health threat. Inhibitors have been developed toprevent β-lactamase-mediated hydrolysis and restore the efficacyof these antibiotics. However, there are few inhibitors availablefor problematic carbapenemases such as oxacillinase-48 (OXA-48). ADNA-encoded chemical library approach was used to rapidly screen forcompounds that bind and potentially inhibit OXA-48. Using this approach,a hit compound, CDD-97, was identified with submicromolar potency(Ki = 0.53 ± 0.08μM) against OXA-48. X-ray crystallography showed that CDD-97binds noncovalently in the active site of OXA-48. Synthesis and testingof derivatives of CDD-97 revealed structure–activity relationshipsand informed the design of a compound with a 2-fold increase in potency.CDD-97, however, synergizes poorly with β-lactam antibioticsto inhibit the growth of bacteria expressing OXA-48 due to poor accumulationinto E. coli. Despite the low in vivo activity, CDD-97 provides new insights into OXA-48 inhibition anddemonstrates the potential of using DNA-encoded chemistry technologyto rapidly identify β-lactamase binders and to study β-lactamaseinhibition, leading to clinically useful inhibitors." @default.
• W3014077166 created "2020-04-03" @default.
• W3014077166 creator A5000105829 @default.
• W3014077166 creator A5007728137 @default.
• W3014077166 creator A5014232188 @default.
• W3014077166 creator A5019024121 @default.
• W3014077166 creator A5049547614 @default.
• W3014077166 creator A5050107484 @default.
• W3014077166 creator A5050632280 @default.
• W3014077166 creator A5050804010 @default.
• W3014077166 creator A5050982810 @default.
• W3014077166 creator A5051089170 @default.
• W3014077166 creator A5052532604 @default.
• W3014077166 creator A5054094467 @default.
• W3014077166 creator A5071359121 @default.
• W3014077166 creator A5078548892 @default.
• W3014077166 creator A5080515384 @default.
• W3014077166 creator A5082943207 @default.
• W3014077166 creator A5087102144 @default.
• W3014077166 date "2020-03-17" @default.
• W3014077166 modified "2023-09-27" @default.
• W3014077166 title "Identifying Oxacillinase-48 Carbapenemase InhibitorsUsing DNA-Encoded Chemical Libraries" @default.
• W3014077166 doi "https://doi.org/10.1021/acsinfecdis.0c00015.s001" @default.
• W3014077166 hasPublicationYear "2020" @default.
• W3014077166 type Work @default.
• W3014077166 sameAs 3014077166 @default.
• W3014077166 citedByCount "0" @default.
• W3014077166 crossrefType "component" @default.
• W3014077166 hasAuthorship W3014077166A5000105829 @default.
• W3014077166 hasAuthorship W3014077166A5007728137 @default.
• W3014077166 hasAuthorship W3014077166A5014232188 @default.
• W3014077166 hasAuthorship W3014077166A5019024121 @default.
• W3014077166 hasAuthorship W3014077166A5049547614 @default.
• W3014077166 hasAuthorship W3014077166A5050107484 @default.
• W3014077166 hasAuthorship W3014077166A5050632280 @default.
• W3014077166 hasAuthorship W3014077166A5050804010 @default.
• W3014077166 hasAuthorship W3014077166A5050982810 @default.
• W3014077166 hasAuthorship W3014077166A5051089170 @default.
• W3014077166 hasAuthorship W3014077166A5052532604 @default.
• W3014077166 hasAuthorship W3014077166A5054094467 @default.
• W3014077166 hasAuthorship W3014077166A5071359121 @default.
• W3014077166 hasAuthorship W3014077166A5078548892 @default.
• W3014077166 hasAuthorship W3014077166A5080515384 @default.
• W3014077166 hasAuthorship W3014077166A5082943207 @default.
• W3014077166 hasAuthorship W3014077166A5087102144 @default.
• W3014077166 hasBestOaLocation W30140771661 @default.
• W3014077166 hasConcept C181199279 @default.
• W3014077166 hasConcept C185592680 @default.
• W3014077166 hasConcept C202751555 @default.
• W3014077166 hasConcept C207001950 @default.
• W3014077166 hasConcept C2776685102 @default.
• W3014077166 hasConcept C41183919 @default.
• W3014077166 hasConcept C501593827 @default.
• W3014077166 hasConcept C523546767 @default.
• W3014077166 hasConcept C54355233 @default.
• W3014077166 hasConcept C552990157 @default.
• W3014077166 hasConcept C55493867 @default.
• W3014077166 hasConcept C57992300 @default.
• W3014077166 hasConcept C86803240 @default.
• W3014077166 hasConcept C89423630 @default.
• W3014077166 hasConceptScore W3014077166C181199279 @default.
• W3014077166 hasConceptScore W3014077166C185592680 @default.
• W3014077166 hasConceptScore W3014077166C202751555 @default.
• W3014077166 hasConceptScore W3014077166C207001950 @default.
• W3014077166 hasConceptScore W3014077166C2776685102 @default.
• W3014077166 hasConceptScore W3014077166C41183919 @default.
• W3014077166 hasConceptScore W3014077166C501593827 @default.
• W3014077166 hasConceptScore W3014077166C523546767 @default.
• W3014077166 hasConceptScore W3014077166C54355233 @default.
• W3014077166 hasConceptScore W3014077166C552990157 @default.
• W3014077166 hasConceptScore W3014077166C55493867 @default.
• W3014077166 hasConceptScore W3014077166C57992300 @default.
• W3014077166 hasConceptScore W3014077166C86803240 @default.
• W3014077166 hasConceptScore W3014077166C89423630 @default.
• W3014077166 hasLocation W30140771661 @default.
• W3014077166 hasOpenAccess W3014077166 @default.
• W3014077166 hasPrimaryLocation W30140771661 @default.
• W3014077166 hasRelatedWork W1872459886 @default.
• W3014077166 hasRelatedWork W1968310807 @default.
• W3014077166 hasRelatedWork W2095666577 @default.
• W3014077166 hasRelatedWork W2308144791 @default.
• W3014077166 hasRelatedWork W2536200613 @default.
• W3014077166 hasRelatedWork W2565816470 @default.
• W3014077166 hasRelatedWork W2594606023 @default.
• W3014077166 hasRelatedWork W2609950920 @default.
• W3014077166 hasRelatedWork W2778580813 @default.
• W3014077166 hasRelatedWork W2780486542 @default.
• W3014077166 hasRelatedWork W2899913067 @default.
• W3014077166 hasRelatedWork W2972794119 @default.
• W3014077166 hasRelatedWork W2972820440 @default.
• W3014077166 hasRelatedWork W2995743119 @default.
• W3014077166 hasRelatedWork W3034560589 @default.
• W3014077166 hasRelatedWork W3087950656 @default.
• W3014077166 hasRelatedWork W3120999347 @default.
• W3014077166 hasRelatedWork W4210487041 @default.
• W3014077166 hasRelatedWork W2407375057 @default.
• W3014077166 hasRelatedWork W2774636508 @default.
• W3014077166 isParatext "false" @default.
• W3014077166 isRetracted "false" @default.
• W3014077166 magId "3014077166" @default.

• next