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MRP inhibitors block multidrug resistance-associated proteins, which export drugs and conjugates. Multidrug resistance-associated protein 1 (MRP1) was cloned in 1992 from a multidrug-resistant human lung cancer cell line. MRP1 and its relatives belong to subfamily C of the adenosine triphosphate-binding cassette (ABC) transporters. A 1994 study showed that MRP1 exports leukotriene C4 and related glutathione conjugates. Reversan was reported in 2009 as an MRP1 inhibitor and is also listed as a P-glycoprotein (P-gp) inhibitor. Biricodar modulates both P-gp and MRP1, and LY-402913, ZW-1226 and CPI1 are listed as MRP1 inhibitors. Ceefourin 1 and Ceefourin 2 were identified in 2014 as selective MRP4 inhibitors. PU 23 and DM-4107 are further compounds listed as MRP4 inhibitors.
Synonyms: VX-710 dicitrate; VX-710
Biricodar dicitrate (VX-710 dicitrate) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
Synonyms: VX-710
Biricodar (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells.
