Matches in SemOpenAlex for { <https://semopenalex.org/work/W1970453912> ?p ?o ?g. }
- W1970453912 endingPage "175" @default.
- W1970453912 startingPage "167" @default.
- W1970453912 abstract "1-Bromo-2-[14C]pinacolone, (CH3)3C14COCH2Br ([14C]BrPin), was prepared from [1-14C]acetyl chloride and tert-butylmagnesium chloride with cuprous chloride catalyst, followed by bromination. It was examined as an active-site directed label for acetylcholinesterase (acetylcholine acetylhydrolase, EC 3.1.1.7) (AcChE). AcChE, isolated from Torpedo nobiliana, has kcat=(4.00±0.04)·103s−1, Km=0.055±0.008 mM in hydrolysis of acetylthiocholine, and kcat=(5.6±0.2)·103s−1, Km=0.051±0.003 mM in hydrolysis of acetylcholine. BrPin, binding in the trimethyl cavity, acts initially as a reversible competitive inhibitor, Ki=0.20±0.09 mM, and, with time, as an irreversible covalently bound inactivator. Introduction of 14C from [14C]BrPin into Torpedo AcChE at pH 7.0 was followed by SDS-PAGE, autoradiography and scintillation counting, in the absence and presence of 5-trimethylammonio-2-pentanone (TAP), a competitive inhibitor (Ki=0.075±0.001 mM) isosteric with acetylcholine; 1.8–1.914C was incorporated per inactivated enzyme unit at 50% inactivation. TAP retarded i of 0.9–1.114C per unit of enzyme protected. Prior inactivation of AcChE by BrPin prevents reaction with [3H]diisopropyl fluorophosphate ([3H]DFP). Prior inactivation by DFP or [3H]DFP does not prevent reaction with [14C]BrPin, and this subsequent reaction with BrPin does not displace the [3H] moiety. [14C]BrPin alkylates a nucleophile in the active site, and this reaction does not alkylate or utilize the serine-hydroxyl." @default.
- W1970453912 created "2016-06-24" @default.
- W1970453912 creator A5001034485 @default.
- W1970453912 creator A5001903645 @default.
- W1970453912 creator A5026583404 @default.
- W1970453912 creator A5057672280 @default.
- W1970453912 creator A5060274786 @default.
- W1970453912 creator A5073425838 @default.
- W1970453912 date "1989-08-01" @default.
- W1970453912 modified "2023-09-23" @default.
- W1970453912 title "Reactions of 1-bromo-2-[14C]pinacolone with acetylcholinesterase from Torpedo nobiliana. Effects of 5-trimethylammonio-2-pentanone and diisopropyl fluorophosphate" @default.
- W1970453912 cites W120458786 @default.
- W1970453912 cites W1526676880 @default.
- W1970453912 cites W1540879137 @default.
- W1970453912 cites W1555252779 @default.
- W1970453912 cites W1558203936 @default.
- W1970453912 cites W1567765570 @default.
- W1970453912 cites W1590152938 @default.
- W1970453912 cites W1765021352 @default.
- W1970453912 cites W1775749144 @default.
- W1970453912 cites W184960722 @default.
- W1970453912 cites W1966102999 @default.
- W1970453912 cites W1966419526 @default.
- W1970453912 cites W1967047630 @default.
- W1970453912 cites W1971048984 @default.
- W1970453912 cites W1981964291 @default.
- W1970453912 cites W1995041731 @default.
- W1970453912 cites W1995403265 @default.
- W1970453912 cites W1995864559 @default.
- W1970453912 cites W2000477613 @default.
- W1970453912 cites W2012384963 @default.
- W1970453912 cites W2013132270 @default.
- W1970453912 cites W2020605520 @default.
- W1970453912 cites W2020986390 @default.
- W1970453912 cites W2022718687 @default.
- W1970453912 cites W2022964379 @default.
- W1970453912 cites W2025380882 @default.
- W1970453912 cites W2026621849 @default.
- W1970453912 cites W2040095977 @default.
- W1970453912 cites W2054979333 @default.
- W1970453912 cites W2059000929 @default.
- W1970453912 cites W2063413595 @default.
- W1970453912 cites W2066361830 @default.
- W1970453912 cites W2067290235 @default.
- W1970453912 cites W2070497237 @default.
- W1970453912 cites W2071036683 @default.
- W1970453912 cites W2076300996 @default.
- W1970453912 cites W2100837269 @default.
- W1970453912 cites W219453556 @default.
- W1970453912 cites W2333083481 @default.
- W1970453912 cites W68267517 @default.
- W1970453912 cites W988479680 @default.
- W1970453912 doi "https://doi.org/10.1016/0167-4838(89)90182-9" @default.
- W1970453912 hasPubMedId "https://pubmed.ncbi.nlm.nih.gov/2765553" @default.
- W1970453912 hasPublicationYear "1989" @default.
- W1970453912 type Work @default.
- W1970453912 sameAs 1970453912 @default.
- W1970453912 citedByCount "18" @default.
- W1970453912 crossrefType "journal-article" @default.
- W1970453912 hasAuthorship W1970453912A5001034485 @default.
- W1970453912 hasAuthorship W1970453912A5001903645 @default.
- W1970453912 hasAuthorship W1970453912A5026583404 @default.
- W1970453912 hasAuthorship W1970453912A5057672280 @default.
- W1970453912 hasAuthorship W1970453912A5060274786 @default.
- W1970453912 hasAuthorship W1970453912A5073425838 @default.
- W1970453912 hasConcept C123419017 @default.
- W1970453912 hasConcept C155647269 @default.
- W1970453912 hasConcept C161790260 @default.
- W1970453912 hasConcept C170493617 @default.
- W1970453912 hasConcept C178790620 @default.
- W1970453912 hasConcept C178907741 @default.
- W1970453912 hasConcept C181199279 @default.
- W1970453912 hasConcept C185592680 @default.
- W1970453912 hasConcept C193557335 @default.
- W1970453912 hasConcept C2776568683 @default.
- W1970453912 hasConcept C2776873056 @default.
- W1970453912 hasConcept C2778816929 @default.
- W1970453912 hasConcept C2779059548 @default.
- W1970453912 hasConcept C2909509320 @default.
- W1970453912 hasConcept C41183919 @default.
- W1970453912 hasConcept C55493867 @default.
- W1970453912 hasConcept C56856141 @default.
- W1970453912 hasConcept C71240020 @default.
- W1970453912 hasConcept C80161118 @default.
- W1970453912 hasConcept C94412978 @default.
- W1970453912 hasConceptScore W1970453912C123419017 @default.
- W1970453912 hasConceptScore W1970453912C155647269 @default.
- W1970453912 hasConceptScore W1970453912C161790260 @default.
- W1970453912 hasConceptScore W1970453912C170493617 @default.
- W1970453912 hasConceptScore W1970453912C178790620 @default.
- W1970453912 hasConceptScore W1970453912C178907741 @default.
- W1970453912 hasConceptScore W1970453912C181199279 @default.
- W1970453912 hasConceptScore W1970453912C185592680 @default.
- W1970453912 hasConceptScore W1970453912C193557335 @default.
- W1970453912 hasConceptScore W1970453912C2776568683 @default.
- W1970453912 hasConceptScore W1970453912C2776873056 @default.
- W1970453912 hasConceptScore W1970453912C2778816929 @default.
- W1970453912 hasConceptScore W1970453912C2779059548 @default.