The large extracellular loop of organic cation transporter 1 influences substrate affinity and is pivotal for oligomerization
06.09.2011
Keller T, Egenberger B, Gorboulev V, Bernhard F, Uzelac Z, Gorbunov D, Wirth C, Koppatz S, Dötsch V, Hunte C, Sitte HH, Koepsell H.
J Biol Chem. 2011;286(43):37874-86.
Organic cation transporters (OCTs) play a pivotal role in absorption, distribution, and excretion of drugs. The study shows that the structural integrity of the large extracellular loop of rOct1 is critically dependent on disulfide bond formation and that this loop is pivotal for homo-oligomerization. Oligomerization increases membrane targeting of the transporter but OCT1 monomers can operate independently. The reported data are important to understand the transport mechanism of the medically relevant transporters.
