FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W1996335718> ?p ?o ?g. }

• W1996335718 endingPage "588" @default.
• W1996335718 startingPage "579" @default.
• W1996335718 abstract "Penicillin-binding proteins (PBPs) are ubiquitous bacterial enzymes involved in cell wall biosynthesis. The development of new PBP inhibitors is a potentially viable strategy for developing new antibacterial agents. Several potential transition state analogue inhibitors for the PBPs were synthesized, including peptide chloromethyl ketones, trifluoromethyl ketones, aldehydes, and boronic acids. These agents were characterized chemically, stereochemically, and as inhibitors of a set of low molecular mass PBPs: Escherichia coli (EC) PBP 5, Neisseria gonorrhoeae (NG) PBP 3, and NG PBP 4. A peptide boronic acid was the most effective PBP inhibitor in the series, with a preference observed for a d-boroAla-based over an l-boroAla-based inhibitor, as expected given that physiological PBP substrates are based on d-Ala at the cleavage site. The lowest K(I) of 370 nM was obtained for NG PBP 3 inhibition by Boc-l-Lys(Cbz)-d-boroAla (10b). Competitive inhibition was observed for this enzyme-inhibitor pair, as expected for an active site-directed inhibitor. For the three PBPs included in this study, an inverse correlation was observed between the values for log K(I) with 10b and the values for log(k(cat)/K(m)) for activity against the analogous substrate, and K(m)/K(I) ratios were 90, 1900, and 9600 for NG PBP 4, EC PBP 5, and NG PBP 3, respectively. These results demonstrate that peptide boronic acids can be effective transition state analogue inhibitors for the PBPs and provide a basis for the use of these agents as probes of PBP structure, function, and mechanism, as well as a possible basis for the development of new PBP-targeted antibacterial agents." @default.
• W1996335718 created "2016-06-24" @default.
• W1996335718 creator A5011107963 @default.
• W1996335718 creator A5012455309 @default.
• W1996335718 creator A5075589181 @default.
• W1996335718 creator A5078141025 @default.
• W1996335718 creator A5089479395 @default.
• W1996335718 date "2002-12-21" @default.
• W1996335718 modified "2023-10-09" @default.
• W1996335718 title "Potential Transition State Analogue Inhibitors for the Penicillin-Binding Proteins" @default.
• W1996335718 cites W1567678817 @default.
• W1996335718 cites W1571433223 @default.
• W1996335718 cites W1588598829 @default.
• W1996335718 cites W1770472858 @default.
• W1996335718 cites W1789135509 @default.
• W1996335718 cites W1816216527 @default.
• W1996335718 cites W1986810946 @default.
• W1996335718 cites W1986924706 @default.
• W1996335718 cites W1988294842 @default.
• W1996335718 cites W2032077456 @default.
• W1996335718 cites W2055237918 @default.
• W1996335718 cites W2066946595 @default.
• W1996335718 cites W2079537385 @default.
• W1996335718 cites W2094871139 @default.
• W1996335718 cites W2109793735 @default.
• W1996335718 cites W2111516721 @default.
• W1996335718 cites W2115069651 @default.
• W1996335718 cites W2128577323 @default.
• W1996335718 cites W2130752141 @default.
• W1996335718 cites W2151020563 @default.
• W1996335718 cites W2151496242 @default.
• W1996335718 cites W2163279482 @default.
• W1996335718 cites W2172007292 @default.
• W1996335718 cites W2178936247 @default.
• W1996335718 cites W2342867733 @default.
• W1996335718 cites W2352447739 @default.
• W1996335718 cites W2400800015 @default.
• W1996335718 cites W2949448151 @default.
• W1996335718 doi "https://doi.org/10.1021/bi026726k" @default.
• W1996335718 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/12525187" @default.
• W1996335718 hasPublicationYear "2002" @default.
• W1996335718 type Work @default.
• W1996335718 sameAs 1996335718 @default.
• W1996335718 citedByCount "42" @default.
• W1996335718 countsByYear W19963357182012 @default.
• W1996335718 countsByYear W19963357182013 @default.
• W1996335718 countsByYear W19963357182014 @default.
• W1996335718 countsByYear W19963357182016 @default.
• W1996335718 countsByYear W19963357182020 @default.
• W1996335718 countsByYear W19963357182021 @default.
• W1996335718 countsByYear W19963357182022 @default.
• W1996335718 countsByYear W19963357182023 @default.
• W1996335718 crossrefType "journal-article" @default.
• W1996335718 hasAuthorship W1996335718A5011107963 @default.
• W1996335718 hasAuthorship W1996335718A5012455309 @default.
• W1996335718 hasAuthorship W1996335718A5075589181 @default.
• W1996335718 hasAuthorship W1996335718A5078141025 @default.
• W1996335718 hasAuthorship W1996335718A5089479395 @default.
• W1996335718 hasConcept C104317684 @default.
• W1996335718 hasConcept C13053905 @default.
• W1996335718 hasConcept C174802600 @default.
• W1996335718 hasConcept C181199279 @default.
• W1996335718 hasConcept C185592680 @default.
• W1996335718 hasConcept C2776653525 @default.
• W1996335718 hasConcept C2779281246 @default.
• W1996335718 hasConcept C41183919 @default.
• W1996335718 hasConcept C501593827 @default.
• W1996335718 hasConcept C547475151 @default.
• W1996335718 hasConcept C55493867 @default.
• W1996335718 hasConcept C56856141 @default.
• W1996335718 hasConcept C71240020 @default.
• W1996335718 hasConceptScore W1996335718C104317684 @default.
• W1996335718 hasConceptScore W1996335718C13053905 @default.
• W1996335718 hasConceptScore W1996335718C174802600 @default.
• W1996335718 hasConceptScore W1996335718C181199279 @default.
• W1996335718 hasConceptScore W1996335718C185592680 @default.
• W1996335718 hasConceptScore W1996335718C2776653525 @default.
• W1996335718 hasConceptScore W1996335718C2779281246 @default.
• W1996335718 hasConceptScore W1996335718C41183919 @default.
• W1996335718 hasConceptScore W1996335718C501593827 @default.
• W1996335718 hasConceptScore W1996335718C547475151 @default.
• W1996335718 hasConceptScore W1996335718C55493867 @default.
• W1996335718 hasConceptScore W1996335718C56856141 @default.
• W1996335718 hasConceptScore W1996335718C71240020 @default.
• W1996335718 hasIssue "2" @default.
• W1996335718 hasLocation W19963357181 @default.
• W1996335718 hasLocation W19963357182 @default.
• W1996335718 hasOpenAccess W1996335718 @default.
• W1996335718 hasPrimaryLocation W19963357181 @default.
• W1996335718 hasRelatedWork W1852497695 @default.
• W1996335718 hasRelatedWork W1951830410 @default.
• W1996335718 hasRelatedWork W1991833505 @default.
• W1996335718 hasRelatedWork W2000610163 @default.
• W1996335718 hasRelatedWork W2071988704 @default.
• W1996335718 hasRelatedWork W2078293238 @default.
• W1996335718 hasRelatedWork W2091078308 @default.
• W1996335718 hasRelatedWork W2125229513 @default.
• W1996335718 hasRelatedWork W2395116299 @default.

• next