1. Academic Validation
  2. Oxime-based inhibitors of glucose transporter 1 displaying antiproliferative effects in cancer cells

Oxime-based inhibitors of glucose transporter 1 displaying antiproliferative effects in cancer cells

  • Bioorg Med Chem Lett. 2013 Dec 15;23(24):6923-7. doi: 10.1016/j.bmcl.2013.09.037.
Tiziano Tuccinardi 1 Carlotta Granchi Jessica Iegre Ilaria Paterni Simone Bertini Marco Macchia Adriano Martinelli Yanrong Qian Xiaozhuo Chen Filippo Minutolo
Affiliations

Affiliation

  • 1 Dipartimento di Farmacia, Università di Pisa, Via Bonanno 6, 56126 Pisa, Italy.
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

Cancer; Glucose transporter; Glycolysis; Modeling; Warburg effect.

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