Development of surrogate substrates for neuropathy target esterase

Babak Borhan, Ying Ko, Chris Mackay, Barry W. Wilson, Mark J. Kurth, Bruce D. Hammock

Research output: Contribution to journalArticle

3 Scopus citations

Abstract

Seventeen substrates were synthesized and their activities as surrogate substrates for Neuropathy Target Esterase were tested. Substrates investigated are carbon analogs of phenylvalerate (1) with oxygen and sulfur substituted at the α, β and γ positions. Phenol and thiophenol esters of these analogs constitute two series of compounds tested. The ratio of catalytic hydrolysis to background hydrolysis increased at lower pH values with all substrates tested including phenylvalerate (1). There was more than a 2.5-fold increase in specific activity with phenylthiopropylethanoate (6) at pH of 6.75 compared to phenylvalerate (1). Furthermore, a 19-fold decrease in Km is reported with compound 6. This and related compounds can be used as the basis of more sensitive assays for neuropathy target esterase. Thiophenyl esters in this series are sufficiently good substrates to hold promise in continuous assays.

Original languageEnglish (US)
Pages (from-to)171-182
Number of pages12
JournalBiochimica et Biophysica Acta (BBA)/Protein Structure and Molecular
Volume1250
Issue number2
DOIs
StatePublished - Jul 19 1995

Keywords

  • Colorimetric substrate
  • Esterase
  • Neuropathy target esterase
  • Surrogate substrate

ASJC Scopus subject areas

  • Biochemistry
  • Biophysics
  • Molecular Biology
  • Structural Biology

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