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Oxime-based inhibitors of glucose transporter 1 displaying antiproliferative effects in cancer cells
Authors:Tiziano Tuccinardi  Carlotta Granchi  Jessica Iegre  Ilaria Paterni  Simone Bertini  Marco Macchia  Adriano Martinelli  Yanrong Qian  Xiaozhuo Chen  Filippo Minutolo
Affiliation:1. Dipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy;2. Edison Biotechnology Institute, Ohio University, the Ridges, Athens, OH 45701, USA
Abstract:An analysis of the main pharmacophoric features present in the still limited number of inhibitors of glucose transporter GLUT1 led to the identification of new oxime-based inhibitors, which proved to be able to efficiently hinder glucose uptake and cell growth in H1299 lung cancer cells. The most important interactions of a representative inhibitor were indicated by a novel computational model of GLUT1, which was purposely developed to explain these results and to provide useful indications for the design and the development of new and more efficient GLUT1 inhibitors.
Keywords:Glucose transporter  Glycolysis  Warburg effect  Cancer  Modeling
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