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Solute carrier family 22 member 3 (SLC22A3), also known as Organic Cation Transporter 3 (OCT3), is a polyspecific, bidirectional transporter located on the plasma membrane of various tissues, including the liver, kidney, heart, and brain (UniProt: O75751; NCBI Gene: 6581). It plays a critical role in the extraneuronal uptake and clearance of monoamine neurotransmitters such as dopamine, serotonin, and norepinephrine, as well as the transport of various xenobiotics and clinically relevant drugs (UniProt: O75751; PubMed: PMID 25611182). In oncology, SLC22A3 expression is often dysregulated, influencing tumor progression and response to chemotherapy in cancers like prostate and colorectal carcinoma (PubMed: PMID 29654114). It is also a key determinant in the pharmacokinetics of the anti-diabetic drug metformin, where genetic variations in the SLC22A3 gene can impact drug efficacy and safety (DrugBank: DB00331). Furthermore, its involvement in monoamine homeostasis links it to cardiovascular and neurodegenerative conditions, making it a target of interest for modulating neurotransmitter levels and drug delivery (PubMed: PMID 25611182).
SLC22A3 acts as a polyspecific transporter that facilitates the uptake or efflux of organic cations and monoamines across the plasma membrane (UniProt: O75751). Drugs typically interact with SLC22A3 either as substrates, where the transporter influences their pharmacokinetics and tissue distribution, or as inhibitors, which block the transport of endogenous compounds or other drugs (DrugBank: DB00331; PubMed: PMID 25611182).
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