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Unless otherwise stated all data on this page refer to the human proteins. Gene information is provided for human (Hs), mouse (Mm) and rat (Rn).
Detailed characterisation of members of the hexose transporter family is limited to SGLT1, 2 and 3, which are all inhibited in a competitive manner by phlorizin, a natural dihydrocholine glucoside, that exhibits modest selectivity towards SGLT2 (see  for an extensive review). SGLT1 is predominantly expressed in the small intestine, mediating the absorption of glucose (e.g. D-glucose), but also occurs in the brain, heart and in the late proximal straight tubule of the kidney. The expression of SGLT2 is almost exclusively restricted to the early proximal convoluted tubule of the kidney, where it is largely responsible for the renal reabsorption of glucose. SGLT3 is not a transporter but instead acts as a glucosensor generating an inwardly directed flux of Na+ that causes membrane depolarization .
1. Chao EC, Henry RR. (2010) SGLT2 inhibition--a novel strategy for diabetes treatment. Nat Rev Drug Discov, 9 (7): 551-9. [PMID:20508640]
2. Diez-Sampedro A, Hirayama BA, Osswald C, Gorboulev V, Baumgarten K, Volk C, Wright EM, Koepsell H. (2003) A glucose sensor hiding in a family of transporters. Proc. Natl. Acad. Sci. U.S.A., 100 (20): 11753-8. [PMID:13130073]
3. Fujimori Y, Katsuno K, Nakashima I, Ishikawa-Takemura Y, Fujikura H, Isaji M. (2008) Remogliflozin etabonate, in a novel category of selective low-affinity sodium glucose cotransporter (SGLT2) inhibitors, exhibits antidiabetic efficacy in rodent models. J. Pharmacol. Exp. Ther., 327 (1): 268-76. [PMID:18583547]
4. Grempler R, Thomas L, Eckhardt M, Himmelsbach F, Sauer A, Sharp DE, Bakker RA, Mark M, Klein T, Eickelmann P. (2012) Empagliflozin, a novel selective sodium glucose cotransporter-2 (SGLT-2) inhibitor: characterisation and comparison with other SGLT-2 inhibitors. Diabetes Obes Metab, 14 (1): 83-90. [PMID:21985634]
5. Hummel CS, Lu C, Loo DD, Hirayama BA, Voss AA, Wright EM. (2011) Glucose transport by human renal Na+/D-glucose cotransporters SGLT1 and SGLT2. Am. J. Physiol., Cell Physiol., 300 (1): C14-21. [PMID:20980548]
6. Kanai Y, Lee WS, You G, Brown D, Hediger MA. (1994) The human kidney low affinity Na+/glucose cotransporter SGLT2. Delineation of the major renal reabsorptive mechanism for D-glucose. J. Clin. Invest., 93 (1): 397-404. [PMID:8282810]
7. Kang SY, Song KS, Lee J, Lee SH, Lee J. (2010) Synthesis of pyridazine and thiazole analogs as SGLT2 inhibitors. Bioorg. Med. Chem., 18 (16): 6069-79. [PMID:20637636]
8. Katsuno K, Fujimori Y, Takemura Y, Hiratochi M, Itoh F, Komatsu Y, Fujikura H, Isaji M. (2007) Sergliflozin, a novel selective inhibitor of low-affinity sodium glucose cotransporter (SGLT2), validates the critical role of SGLT2 in renal glucose reabsorption and modulates plasma glucose level. J. Pharmacol. Exp. Ther., 320 (1): 323-30. [PMID:17050778]
9. Li AR, Zhang J, Greenberg J, Lee T, Liu J. (2011) Discovery of non-glucoside SGLT2 inhibitors. Bioorg. Med. Chem. Lett., 21 (8): 2472-5. [PMID:21398124]
10. Liang Y, Arakawa K, Ueta K, Matsushita Y, Kuriyama C, Martin T, Du F, Liu Y, Xu J, Conway B et al.. (2012) Effect of canagliflozin on renal threshold for glucose, glycemia, and body weight in normal and diabetic animal models. PLoS ONE, 7 (2): e30555. [PMID:22355316]
11. Voss AA, Díez-Sampedro A, Hirayama BA, Loo DD, Wright EM. (2007) Imino sugars are potent agonists of the human glucose sensor SGLT3. Mol. Pharmacol., 71 (2): 628-34. [PMID:17110502]
12. Wright EM, Loo DD, Hirayama BA. (2011) Biology of human sodium glucose transporters. Physiol. Rev., 91 (2): 733-94. [PMID:21527736]
13. Zambrowicz B, Freiman J, Brown PM, Frazier KS, Turnage A, Bronner J, Ruff D, Shadoan M, Banks P, Mseeh F et al.. (2012) LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. Clin. Pharmacol. Ther., 92 (2): 158-69. [PMID:22739142]
Database page citation:
Hexose transporter family. Accessed on 23/03/2017. IUPHAR/BPS Guide to PHARMACOLOGY, http://www.guidetopharmacology.org/GRAC/FamilyDisplayForward?familyId=173.
Concise Guide to PHARMACOLOGY citation:
Alexander SPH, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, Pawson AJ, Sharman JL, Southan C, Davies JA and CGTP Collaborators (2015) The Concise Guide to PHARMACOLOGY 2015/16: Transporters. Br J Pharmacol. 172: 6110-6202.