Abstract

Proteoliposomes represent a suitable and up to date tool for studying membranetransporters which physiologically mediate absorption, excretion, trafficking andreabsorption of nutrients and metabolites. Using recently developed reconstitutionstrategies, transporters can be inserted in artificial bilayers with the same orientation as inthe cell membranes and in the absence of other interfering molecular systems. Thesemethodologies are very suitable for studying kinetic parameters and molecularmechanisms. After the first applications on mitochondrial transporters, in the last decade,proteoliposomes obtained with optimized methodologies have been used for studyingplasma membrane transporters and defining their functional and kinetic properties andstructure/function relationships. A lot of information has been obtained which has clarifiedand completed the knowledge on several transporters among which the OCTN sub-familymembers, transporters for neutral amino acid, B0AT1 and ASCT2, and others.Transporters can mediate absorption of substrate-like derivatives or drugs, improving theirbioavailability or can interact with these compounds or other xenobiotics, leading toside/toxic effects. Therefore, proteoliposomes have recently been used for studying theinteraction of some plasma membrane and mitochondrial transporters with toxiccompounds, such as mercurials, H2O2 and some drugs. Several mechanisms have beendefined and in some cases the amino acid residues responsible for the interaction have been identified. The data obtained indicate proteoliposomes as a novel and potentially importanttool in drug discovery.

Autore Pugliese

• Tonazzi Annamaria , Giangregorio Nicola

Tutti gli autori

• M. Scalise; L. Pochini; N. Giangregorio; A. Tonazzi; C. Indiveri

Titolo volume/Rivista

Pharmaceutics

Anno di pubblicazione

2013

ISSN

1999-4923

ISBN

Non Disponibile

Numero di citazioni Wos

Nessuna citazione

Ultimo Aggiornamento Citazioni

Non Disponibile

Numero di citazioni Scopus

Non Disponibile

Ultimo Aggiornamento Citazioni

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Settori ERC

Non Disponibile

Codici ASJC

Non Disponibile