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Glutamine transporters as pharmacological targets: From function to drug design

Asian Journal of Pharmaceutical Sciences 2020年第2期15卷 207-219页

作者： Mariafrancesca Scalise Lorena Pochini Michele Galluccio lara console Cesare Indiveri Department of DiBEST(Biologia Ecologia e Scienze della Terra)University of CalabriaArcavacata di Rende(CS)87036Italy

Among the different targets of administered drugs,there are membrane transporters that play also a role in drug delivery and ***,drug-transporter interactions are responsible for off-target effects of drugs underlying their *** improvement of the drug design process is subjected to the identification of those membrane transporters mostly relevant for drug absorption,delivery and side effect production.A peculiar group of proteins with great relevance to pharmacology is constituted by the membrane transporters responsible for managing glutamine traffic in different body *** interest around glutamine metabolism lies in its physio-pathological role;glutamine is considered a conditionally essential amino acid because highly proliferative cells have an increased request of glutamine that cannot be satisfied only by endogenous ***,glutamine transporters provide cells with this special *** the glutamine transporters,SLC1A5,SLC6A14,SLC6A19,SLC7A5,SLC7A8 and some members of SLC38 family are the best characterized,so far,in both physiological and pathological *** 3D structures have been solved by CryoEM;other structural data on these transporters have been obtained by computational *** with drugs have been described for several transporters of this *** some of them,the studies are at an advanced stage,for others,the studies are still in nuce and novel biochemical findings open intriguing perspectives.

关键词： Glutamine transporters Drug delivery Pharmacokinetics Screening Proteoliposome

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