Molecular basis of polyspecific drug binding and transport by OCT1 and OCT2.

ABSTRACT: A wide range of endogenous and xenobiotic organic ions require facilitated transport systems to cross the plasma membrane for their disposition ^{1, 2} . In mammals, organic cation transporter subtypes 1 and 2 (OCT1 and OCT2, also known as SLC22A1 and SLC22A2, respectively) are polyspecific transporters responsible for the uptake and clearance of structurally diverse cationic compounds in the liver and kidneys, respectively ^{3, 4} . Notably, it is well established that human OCT1 and OCT2 play central roles in the pharmacokinetics, pharmacodynamics, and drug-drug interactions (DDI) of many prescription medications, including metformin ^{5, 6} . Despite their importance, the basis of polyspecific cationic drug recognition and the alternating access mechanism for OCT

SUBMITTER: Suo Y 

PROVIDER: S-EPMC10055046 | biostudies-literature | 2023 Mar

REPOSITORIES: biostudies-literature