Role of OCT1 in hepatocellular carcinoma

Figures & data

Table 1 Natural substrates and drugs transported by organic cation transporters (OCTs)

OCTs	Natural substrates	Drugs
OCT1	TEA, MPP, ASP, acetylcholine, choline, corticosterone, epinephrine, histamine, guanidine, salsolinol serotonin, thiamine, progesterone, prostaglandin E2/F2.^Citation9,Citation22,Citation96^–^Citation101	Acyclovir, atenolol, debrisoquine, furamidine, ganciclovir, lamivudine, lamotrigine, metformin, oxaliplatin, pentamidine, picoplatin, tropisetron, zalcitabine.^Citation102^–^Citation105
OCT2	TEA, MPP, ASP, N-methylnicotinamide, aminoguanidine, acetylcholine, dopamine, epinephrine, norepinephrine, serotonin, histamine, cyclo (His-Pro), salsolinol, agmatinepolyamine, putrescine, choline.^Citation22,Citation100,Citation101	Amantadine, amiloride, atenolol, cimetidine, cisplatin, famotidine, ifosfamide, lamivudine, memantine, metformin, oxaliplatin, picoplatin.^Citation102^–^Citation103,Citation106
OCT3	epinephrine, norepinephrine, histamine, agmatine, cyclo (His-Pro), salsolinol.^Citation101,	Cisplatin, etilefrine, lamivudine, lidocaine, metformin, oxaliplatin, pramipexole, quinidine.^Citation103,Citation107

Abbreviations: TEA, tetraethylammonium; MPP, 1-methyl-4-phenylpyridinium; ASP, 4-[4-(dimthylamino)-styryl]-Nmethylpyridinium.

Figure 1 Schemes of pathways/processes affecting OCT1 expression.

Notes: (A) The SLC22A1 gene tends to be suppressed by CDCA via interference of small heterodimer partner (SHP), which can co-repress HNF-4α transactivation. (B) PXR is activated by rifampicin to compete for SRC-1 with HNF-4α, and thus represses the HNF-4α-mediated transactivation of SLC22A1 gene. (C) The HNF-4α-mediated transactivation of SLC22A1 gene is activated by glucocorticoids binding glucocorticoids receptor via up-regulating HNF-4α.

Abbreviation: CDCA, chenodeoxycholic acid.

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