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Functionalized analogues of 5,8,10-trideazafolate: Development of an enzyme-assembled tight binding inhibitor of GAR Tfase and a potential irreversible inhibitor of AICAR Tfase

Academic Article
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Overview

related to degree

  • Haynes, Nancy-Ellen, Ph.D. in Organic Chemistry, Scripps Research 1991 - 1996

authors

  • Boger, Dale
  • Haynes, Nancy-Ellen
  • Warren, M. S.
  • Ramcharan, J.
  • Kitos, P. A.
  • Benkovic, S. J.

publication date

  • September 1997

journal

  • Bioorganic & Medicinal Chemistry  Journal

abstract

  • A set of inhibitors 3 and 4 of GAR and AICAR Tfase based on the TDAF core which contain an sp2 C-10 carbon atom replacing N-10 of the natural cofactor are detailed. Both possess electrophilic olefins and the potential of trapping the reacting amine of the substrates GAR and AICAR by a Michael addition at the enzyme active site to provide an enzyme-assembled tight binding inhibitor. While these agents did not display such characteristics and served as simple competitive inhibitors of GAR Tfase and AICAR Tfase, inhibitor 15 prepared in the conversion of 3 to 4 may provide an enzyme-assembled tight binding inhibitor of GAR Tfase upon reaction with the substrate GAR and may inactivate AICAR Tfase by virtue of alkylation of an active site residue.

subject areas

  • Cell Division
  • Enzyme Inhibitors
  • Glutamates
  • Hydroxymethyl and Formyl Transferases
  • Magnetic Resonance Spectroscopy
  • Molecular Structure
  • Phosphoribosylaminoimidazolecarboxamide Formyltransferase
  • Phosphoribosylglycinamide Formyltransferase
  • Protein Binding
  • Quinazolines
  • Spectrometry, Mass, Fast Atom Bombardment
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Identity

International Standard Serial Number (ISSN)

  • 0968-0896

Digital Object Identifier (DOI)

  • 10.1016/s0968-0896(97)00122-3

PubMed ID

  • 9354239
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Additional Document Info

start page

  • 1839

end page

  • 1846

volume

  • 5

issue

  • 9

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