Direct interaction of a cftr potentiator and a cftr corrector with phospholipid bilayers (Articolo in rivista)

Type

• Articolo in rivista (Classe)
• Prodotto della ricerca (Classe)

Label

• Direct interaction of a cftr potentiator and a cftr corrector with phospholipid bilayers (Articolo in rivista) (literal)

Anno

• 2014-01-01T00:00:00+01:00 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#doi

• 10.1007/s00249-014-0956-y (literal)

Alternative label

• Baroni D.; Zegarra-Moran O.; Svensson A.; Moran O. (2014)
  Direct interaction of a cftr potentiator and a cftr corrector with phospholipid bilayers
  in European biophysics journal
  (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#autori

• Baroni D.; Zegarra-Moran O.; Svensson A.; Moran O. (literal)

Pagina inizio

• 341 (literal)

Pagina fine

• 346 (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#url

• http://www.scopus.com/inward/record.url?eid=2-s2.0-84905719391&partnerID=q2rCbXpz (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroVolume

• 43 (literal)

Rivista

• European biophysics journal (Rivista)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#numeroFascicolo

• 6-7 (literal)

Note

• Scopu (literal)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#affiliazioni

• Istituto di Biofisica, CNR, via De Marini, 6, 16149 Genoa, Italy; Laboratorio di Genetica Molecolare, Istituto Giannina Gaslini, via Gerolamo Gaslini, 5, 16148 Genoa, Italy; Cells-Alba, 08290 Cerdanyola del Valle?s, Barcelona, Spain (literal)

Titolo

• Direct interaction of a cftr potentiator and a cftr corrector with phospholipid bilayers (literal)

Abstract

• Cystic fibrosis transmembrane conductance regulator (CFTR) potentiators and correctors are new drugs that target the basic CFTR protein defect and are expected to benefit cystic fibrosis patients. To optimize the substances so far proposed for human use, and to minimise unwanted side effects, it is essential to investigate possible interactions between the drugs and cell components. We used small-angle X-ray scattering with synchrotron radiation to analyse the effects of two representative drugs, the potentiator VX-770 (Ivacaftor), approved for human use, and the corrector VX-809 (Lumacaftor), on a model phospholipid membrane. By reconstruction of the electron density profile of unilamellar vesicles treated with VX-770 or VX-809 we found that these drugs penetrate the phospholipid bilayer. VX-809 becomes homogeneously distributed throughout the bilayer whereas VX-770 accumulates predominantly in the internal leaflet, behaviour probably favoured by the asymmetry of the bilayer, because of vesicle curvature. Penetration of the bilayer by these drugs, probably as part of the mechanisms of permeation, causes destabilization of the membrane; this must be taken into account during future drug development. © European Biophysical Societies'Association 2014. (literal)

Prodotto di

• Meccanismi molecolari della permeabilità di membrana (MD.P01.009.001) (Modulo)
• Istituto di biofisica (IBF) (Istituto)

Autore CNR

• OSCAR SANTIAGO MORAN ALBONICO GASPAROTTO (Unità di personale interno)
• DEBORA BARONI (Unità di personale esterno)

Insieme di parole chiave

• Keywords of "Direct interaction of a cftr potentiator and a cftr corrector with phospholipid bilayers" (Insieme di parole chiave)

Incoming links:

Autore CNR di

• OSCAR SANTIAGO MORAN ALBONICO GASPAROTTO (Unità di personale interno)
• DEBORA BARONI (Unità di personale esterno)

Prodotto

• Istituto di biofisica (IBF) (Istituto)
• Meccanismi molecolari della permeabilità di membrana (MD.P01.009.001) (Modulo)

Http://www.cnr.it/ontology/cnr/pubblicazioni.owl#rivistaDi

• European biophysics journal (Rivista)

Insieme di parole chiave di

• Keywords of "Direct interaction of a cftr potentiator and a cftr corrector with phospholipid bilayers" (Insieme di parole chiave)