1H-NMR relaxometric study of pancreatic serine (pro)enzyme inhibition by a Gd(III) chelate bearing boronic functionalities

Silvio Aime, Mauro Fasano, Silvia Paoletti, Franca Viola, Cataldo Tarricone, Paolo Ascenzi

Research output: Contribution to journalArticle

3 Citations (Scopus)

Abstract

Binding of the paramagnetic N,N'-bis(m-boroxyphenylcarbamoylmethyl)- diethylenetriamine-N,N',N'-triacetic acid Gd(III) complex (GdBB) to chymotrypsin, chymotrypsinogen, trypsin, typsinogen and pancreatic elastase has been investigated by 1H-NMR relaxometry, between pH 6.0 and 8.5, at 25.0°C. Values of Ki for the competitive inhibition of serine proteinases by GdBB are in excellent agreement with values of Kd obtained by 1H-NMR relaxometry, suggesting that the substrate and the paramagnetic complex bind to the same region. Moreover, 1H-NMR relaxometry allowed to determine values of Kd for GdBB binding to chymotrypsinogen and trypsinogen, both devoid of catalytic activity. The increase of the water proton relaxation rate upon GdBB binding to serine (pro)enzymes may be useful in the design of novel functional contrast agents for magnetic resonance imaging.

Original languageEnglish
Pages (from-to)741-746
Number of pages6
JournalBiochemistry and Molecular Biology International
Volume39
Issue number4
Publication statusPublished - 1996

Fingerprint

Bearings (structural)
Enzyme inhibition
Chymotrypsinogen
Serine
Nuclear magnetic resonance
Enzymes
Trypsinogen
Pancreatic Elastase
Chymotrypsin
Serine Proteases
Magnetic resonance
Trypsin
Contrast Media
Protons
Catalyst activity
Magnetic Resonance Imaging
Imaging techniques
Acids
Water
Substrates

Keywords

  • (Pro)enzyme inhibition
  • H-NMR relaxometry
  • Gd(III) complex
  • Serine proteinases
  • Zymogens

ASJC Scopus subject areas

  • Biochemistry
  • Genetics
  • Molecular Biology

Cite this

1H-NMR relaxometric study of pancreatic serine (pro)enzyme inhibition by a Gd(III) chelate bearing boronic functionalities. / Aime, Silvio; Fasano, Mauro; Paoletti, Silvia; Viola, Franca; Tarricone, Cataldo; Ascenzi, Paolo.

In: Biochemistry and Molecular Biology International, Vol. 39, No. 4, 1996, p. 741-746.

Research output: Contribution to journalArticle

Aime, Silvio ; Fasano, Mauro ; Paoletti, Silvia ; Viola, Franca ; Tarricone, Cataldo ; Ascenzi, Paolo. / 1H-NMR relaxometric study of pancreatic serine (pro)enzyme inhibition by a Gd(III) chelate bearing boronic functionalities. In: Biochemistry and Molecular Biology International. 1996 ; Vol. 39, No. 4. pp. 741-746.
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