Introduction of SLC47A2
SLC47A2 encoded by SLC47A2 gene, also known as MATE2, is a member of the MATE (multidrug and toxic compound extrusion) family of transporters. It is responsible for the solute transport and its substrates are diverse including tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methyl nicotinamide, metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acyclovir, and ganciclovir. SLC47A2 is primarily expressed in the kidney.
|Basic Information of SLC47A2|
|Protein Name||Multidrug and toxin extrusion protein 2|
|Aliases||MATE2, MATE2K, MATE2-B, MATE2-K|
|Organism||Homo sapiens (Human)|
Function of SLC47A2 Membrane Protein
SLC47A2/MATE2 is an organic cation/proton exchanger that plays an important role in the renal elimination of toxic electrolytes including endogenous and exogenous, through urine and bile. Its substrates are diverse including many cationic drugs and endogenous compounds. Many studies have indicated that SLC47A2 plays an important role in metformin (a drug for diabetes treatment) pharmacokinetics. It is associated with metformin disposition and response through mediating the transport and excretion of metformin into the urine and bile. A gain-of-function promoter polymorphism (rs12943590 G>A) of SLC47A2 gene is associated with glucose-lowering effects of metformin in type 2 diabetes patients. In addition, compared to the paired adjacent nontumor tissues, the expression of SLC47A2 is significantly decreased in the renal cell carcinoma (RCC) tissue at low tumor node metastasis stage, suggesting that SLC47A2 inhibition may enhance the risk of RCC.
Fig.1 The structural model of human MATE2-K is presented: side view (A) and top view (B). (Nishimura, 2014)
Application of SLC47A2 Membrane Protein in Literature
The article reports that the high MATE2 expression may result in resistance to the anti-proliferative effect of metformin and should be considered as a negative predictive biomarker in clinical trials.
In the study, results show that the expression of SLC47A2 is significantly decreased in the renal cell carcinoma (RCC) tissue compared to the paired adjacent nontumor tissues at low tumor node metastasis stage. Thus, it is proposed that the inhibition of SLC47A2 may increase the susceptibility of RCC.
The investigation reveals that MATE2-K is involved in the poor response to metformin in patients with diabetes.
Results of the study show that heterozygous MATE variants have little effect on the disposition of metformin in diabetic patients.
This metformin pharmacokinetic study determines the association between MATE2-K promoter haplotypes and metformin pharmacokinetics.
SLC47A2 Preparation Options
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