Description
Fasentin (392721-37-8) is a novel inhibitor of glucose uptake which acts via inhibition of the glucose transporter GluT1 and GluT4 (IC50=68 μM).1?Inhibition of glucose uptake is cell type specific2?and is a promising approach to new cancer therapeutics3. Rescues cardiac progenitor cell dysfunction and mitochondrial fission induced by high glucose.4?Sensitizes cells to FAS-induced cell death.5,6
Uses
Fasentin has been used as a glucose transporter (GLUT1) inhibitor to assess its effects on the vulnerability of a wide range of triple-negative breast cancer (TNBC) cell lines and to study its effects on cytotoxic drugs induced by hydrocortisone (HC).
Uses
Fasentin is a novel glucose transport inhibitor that blocks glucose uptake and is also a chemical sensitizer to the death receptor stimuli FAS and tumor necrosis factor apoptosis-inducing ligand.
Biochem/physiol Actions
Fasentin is a novel inhibitor of glucose uptake, GluT1 inhibitor. Fasentin is a novel inhibitor of glucose uptake that sensitizes cells to FAS-induced cell death. Fasentin selectively sensitized to death ligands, but did not decrease FLIP expression. It alters expression of genes associated with nutrient and glucose deprivation. Fasentin interacted with a unique site in the intracellular channel of the glucose transport protein GLUT1.
References
1) Granchi?et al.?(2016),?Anticancer agents interacting with membrane glucose transporters; Med. Chem. Comm.,?7?1716
2) Kraus?et al. (2018),?Targeting glucose transport and the NAD pathway in tumor cells with STF-31: a re-evaluation; Cell. Oncol. (Dordr),?41?485
3) Adekola?et al. (2012),?Glucose transporters in cancer metabolism; Curr. Opin. Oncol.,?24?650
4) Choi?et al.?(2016),?High Glucose Causes Human Cardiac Progenitor Cell Dysfunction by Promoting Mitochondrial Fission: Role of a GLUT1 Blocker; Prog. Biomol. Ther. (Seoul),?24?363
5) Schimmer?et al.?(2006),?Identification of small molecules that sensitize resistant tumor cells to tumor necrosis factor-family death receptors; Cancer Res.,?66?2367
6) Wood?et al.?(2008),?A novel inhibitor of glucose uptake sensitizes cells to FAS-induced cell death; Mol. Cancer Ther.,?7?3546
