Multidrug & toxin extrusion protein 1 (MATE-1, hMATE-1, solute carrier family 47 member 1, SLC47A1, MATE1)
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Function
- solute transporter for tetraethylammonium (TEA), 1-methyl-4-phenylpyridinium (MPP), cimetidine, N-methylnicotinamide (NMN), metformin, creatinine, guanidine, procainamide, topotecan, estrone sulfate, acyclovir, ganciclovir & also the zwitterionic cephalosporin, cephalexin & cephradin
- role in the uptake of oxaliplatin (a new platinum anticancer agent)
- able to transport paraquat (PQ or N,N-dimethyl-4-4'-bipiridinium) a widely used herbicid
- responsible for the secretion of cationic drugs across brush border membranes
- KM=0.38 mM for TEA
- KM=0.10 mM for MPP
- KM=0.17 mM for cimetidine
- KM=0.78 mM for metformin
- KM=2.1 mM for guanidine
- KM=1.23 mM for procainamide
- KM=0.07 mM for topotecan
- KM=0.47 mM for estrone sulfate
- KM=2.64 mM for acyclovir
- KM=5.12 mM for ganciclovir
- Vmax=1.185 nmol/min/mg enzyme toward TEA
- Vmax=0.735 nmol/min/mg enzyme toward MPP
- Vmax=0.135 nmol/min/mg enzyme toward cimetidine
- Vmax=2.23 nmol/min/mg enzyme toward metformin
- Vmax=0.89 nmol/min/mg enzyme toward guanidine
- Vmax=3.78 nmol/min/mg enzyme toward procainamide
- Vmax=0.21 nmol/min/mg enzyme toward topotecan
- Vmax=0.265 nmol/min/mg enzyme toward estrone sulfate
- Vmax=0.62 nmol/min/mg enzyme toward acyclovir
- Vmax=1.08 nmol/min/mg enzyme toward ganciclovir
- Optimum pH is 8.5. active from pH 6 to 8.5
Structure
- belongs to the multi antimicrobial extrusion (MATE) (TC 2.A.66.1) family
Compartment
- cell membrane
- predominantly localized at the plasma membrane but also found in intracellular organelles
Alternative splicing
named isoforms=3
Expression
- expressed in liver, skeletal muscle & kidney (especially found in luminal membranes of the urinary tubules, bile caniculi & brush border membranes)