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The guanidiniocarbonylpyrrole-fluorophore conjugates as theragnostic tools for dipeptidyl peptidase III monitoring and inhibition.
Cehic, Mirsada; Suc Sajko, Josipa; Karacic, Zrinka; Piotrowski, Patryciusz; Smidlehner, Tamara; Jeric, Ivanka; Schmuck, Carsten; Piantanida, Ivo; Tomic, Sanja.
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  • Cehic M; Ruder BosKovic Institute, Zagreb, Croatia.
  • Suc Sajko J; Ruder BosKovic Institute, Zagreb, Croatia.
  • Karacic Z; Ruder BosKovic Institute, Zagreb, Croatia.
  • Piotrowski P; Institute of Organic Chemistry, University of Duisburg-Essen, Essen, Germany.
  • Smidlehner T; Ruder BosKovic Institute, Zagreb, Croatia.
  • Jeric I; Ruder BosKovic Institute, Zagreb, Croatia.
  • Schmuck C; Institute of Organic Chemistry, University of Duisburg-Essen, Essen, Germany.
  • Piantanida I; Ruder BosKovic Institute, Zagreb, Croatia.
  • Tomic S; Ruder BosKovic Institute, Zagreb, Croatia.
J Biomol Struct Dyn ; 38(13): 3790-3800, 2020 Aug.
Article en En | MEDLINE | ID: mdl-31496375
Study of seven new guanidiniocarbonylpyrrole (GCP)-fluorophore conjugates interactions with dipeptidyl peptidase III (DPP III) showed that all compounds bind strongly (Ks ≈ µM) to enzyme active site, but with very different fluorimetric response (varying from quenching to strong increase), dependent on the fluorophore type and intramolecular pre-organisation of molecule. Positively charged lysine side chain improved significantly compound solubility but diminished fluorescence increase upon DPP III binding and completely abolished inhibitory effect on DPP III activity, whereas linker-neutral analogues showed stronger emission increase and were efficient enzyme inhibitors. By far the best fluorimetric response and inhibitive properties showed cyanine-GCP analogue, thus being promising lead compound for both enzyme sensing and bio-activity inhibiting (theragnostic) studies of DPP III in the future.Communicated by Ramaswamy H. Sarma.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dipeptidil-Peptidasas y Tripeptidil-Peptidasas / Colorantes Fluorescentes Idioma: En Revista: J Biomol Struct Dyn Año: 2020 Tipo del documento: Article País de afiliación: Croacia Pais de publicación: Reino Unido
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Dipeptidil-Peptidasas y Tripeptidil-Peptidasas / Colorantes Fluorescentes Idioma: En Revista: J Biomol Struct Dyn Año: 2020 Tipo del documento: Article País de afiliación: Croacia Pais de publicación: Reino Unido