Title : Inhibitor binding in the human renal low- and high-affinity Na+/glucose cotransporters.

Pub. Date : 2008 Mar

PMID : 18063724






3 Functional Relationships(s)
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1 In this study, we examined the inhibition of alpha-methyl-d-glucopyranose transport by phlorizin and a new candidate drug, sergliflozin-A [(2-[4-methoxyphenyl]methyl)phenyl beta-d-glucopyranoside], in COS-7 cells expressing hSGLT1 and hSGLT2. sergliflozin-A solute carrier family 5 member 2 Homo sapiens
2 Inhibition by sergliflozin-A was also competitive, with K(i) values of 1 muM in hSGLT1 and 20 nM in hSGLT2. sergliflozin-A solute carrier family 5 member 2 Homo sapiens
3 In contrast, mutagenesis of the analogous Cys615 in hSGLT2 produced the opposite effect, a decrease in IC(50) for phlorizin and sergliflozin-A. sergliflozin-A solute carrier family 5 member 2 Homo sapiens