P-Gb-In-1

P-gb-IN-1 (compound Ⅲ-8), a 2,5-disubstituted furan derivative, is a highly effective, broadspectrum P-glycoprotein (P-gp) inhibitor. P-gb-IN-1 displayed the reversal activity by inhibiting P-gp efflux. P-gb-IN-1 has a potent affinity to P-gp by forming H-bond interactions with residues Asn 721 and Met 986. P-gb-IN-1 possesses broad-spectrum reversal activity and low toxicity in MCF-7/ADR cells[1].

Research Areas >> Cancer

Signaling Pathways >> Membrane Transporter/Ion Channel >> P-glycoprotein

[1]. Zhikun Yang, et al. Discovery of 2,5-disubstituted furan derivatives featuring a benzamide motif for overcoming P-glycoprotein mediated multidrug resistance in MCF-7/ADR cell. Eur J Med Chem. 2023 Sep 5;257:115462.