Multidrug resistance remains a major obstacle to effective chemotherapy of colon cancer. ABCG2, as a half-transporter of the G subfamily of ATP-binding cassette transporter genes (ABC transporters), is known to play a crucial role in multidrug resistance. However, the molecular mechanism of controlling ABCG2 expression in drug resistance of colon cancer is unclear and scarcely reported. In the ...

Multidrug resistance (MDR) is considered multifactorial and has been associated with overexpression of the multidrug resistance protein (MRP). However, effective compounds for reversal of MRP-related MDR are limited. In the present study, the modulatory activity of the novel pyridine analogue PAK-104P on MRP-mediated resistance to doxorubicin and paclitaxel was investigated in two doxorubicin-s...

The effects of dietary supplementation of garlic (Allium sativum) extract on the growth and disease resistance of African catfish, Clarias gariepinus was evaluated. Also in-vitro evaluation of susceptibility of fish-borne multidrug resistant (MDR) pathogenic bacteria to aqueous extract of garlic was done. Aqueous garlic extract exhibited inhibitory activity against MDR bacteria and the degree o...

Fumitremorgin C (FTC) is a potent and specific chemosensitizing agent in cell lines selected for resistance to mitoxantrone that do not overexpress P-glycoprotein or multidrug resistance protein. The gene encoding a novel transporter, the breast cancer resistance protein (BCRP), was recently found to be overexpressed in a mitoxantrone-selected human colon cell line, S1-M1-3.2, which was used to...

Abstract Multidrug and toxic compound extrusion (MATE) transport proteins confer multidrug resistance on pathogenic microorganisms affect pharmacokinetics in mammals. Our understanding of how MATE transporters work, has mostly relied protein structures MD simulations. However, the energetics drug not been studied detail. Many utilise electrochemical H + or Na gradient to drive substrate efflux,...

Multidrug resistance proteins (MRPs) are members of the C family of a group of proteins named ATP-binding cassette (ABC) transporters. These ABC transporters together form the largest branch of proteins within the human body. The MRP family comprises of 13 members, of which MRP1 to MRP9 are the major transporters indicated to cause multidrug resistance in tumor cells by extruding anticancer dru...

Human hepatoma cells may represent a valuable alternative to the use of human hepatocytes for studying hepatic drug transporters, which is now a regulatory issue during drug development. In the present work, we have characterized hepatic drug transporter expression, activity and regulation in human hepatoma HuH-7 cells, in order to determine the potential relevance of these cells for drug trans...

An overexpression of plasma membrane glycoprotein with a relative molecular mass (Mr) of 170,000-180,000 is consistently found in different multidrug-resistant human and animal cell lines, although the functional role of the protein in multidrug resistance is not fully understood. It has been reported previously that the Mr 170,000-180,000 glycoprotein is involved, directly or indirectly, in th...