Optical biosensor analysis in studying new synthesized bicalutamide analogs binding to androgen receptor (Articolo in rivista)

Type
Label
  • Optical biosensor analysis in studying new synthesized bicalutamide analogs binding to androgen receptor (Articolo in rivista) (literal)
Anno
  • 2014-01-01T00:00:00+01:00 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi
  • 10.1016/j.jpba.2014.03.002 (literal)
Alternative label
  • Fortugno, Cecilia; Varchi, Greta; Guerrini, Andrea; Carrupt, Pierre-Alain; Bertucci, Carlo (2014)
    Optical biosensor analysis in studying new synthesized bicalutamide analogs binding to androgen receptor
    in Journal of pharmaceutical and biomedical analysis (Print)
    (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori
  • Fortugno, Cecilia; Varchi, Greta; Guerrini, Andrea; Carrupt, Pierre-Alain; Bertucci, Carlo (literal)
Pagina inizio
  • 151 (literal)
Pagina fine
  • 157 (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume
  • 95 (literal)
Rivista
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#pagineTotali
  • 7 (literal)
Note
  • ISI Web of Science (WOS) (literal)
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni
  • University of Bologna; Consiglio Nazionale delle Ricerche (CNR); University of Geneva (literal)
Titolo
  • Optical biosensor analysis in studying new synthesized bicalutamide analogs binding to androgen receptor (literal)
Abstract
  • Bicalutamide (Casodex (R)) is a non-steroidal anti-androgen drug used in the treatment of prostate cancer, which represents the second most common malignancy diagnosed in men worldwide. In this work, we analyze the ability of some novel bicalutamide analogs to bind the androgen receptor, by using an optical biosensor. Androgen receptor was covalently immobilized on a carboxy methyl dextran matrix. The immobilized receptor chip was then used for the binding experiments of the bicalutamide analogs. The (R)-bicalutamide dissociation constant was in good agreement to the value reported in literature obtained by using radiolabeled targets. Most of the new synthesized compounds showed higher androgen receptor binding level, when compared to the reference. Our results clearly indicate that the surface plasmon resonance (SPR) technique offers many advantages with respect to other available technologies in terms of studying biomolecular interactions. Moreover, this study provides an effective methodology for determining the binding affinity of novel chemical entities for the isolated androgen receptor, thus excluding possible off-target interactions occurring in conventional cell-based techniques. (C) 2014 Elsevier B.V. All rights reserved. (literal)
Prodotto di
Autore CNR
Insieme di parole chiave

Incoming links:


Prodotto
Autore CNR di
Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi
Insieme di parole chiave di
data.CNR.it