Multidrug resistance studies

TRANSPORT ACROSS BIOLOGICAL MEMBRANES Drug Efflux and Multidrug Resistance Studies... 

Dearden JC, AI-Noobi A, Scott AC, Thomson SA. QSAR studies on P-glycoprotein-regulated multidrug resistance and on its reversal by phenothia-zines. SAR QSAR Environ Res 2003 14 447-54. 

A rational approach to problems such as drug targeting to regions protected by P-gp, inhibition or even prevention of multidrug resistance in different organisms, and prediction of drug-drug interactions due to P-gp should become possible with reliable structure-activity relationship (SAR) studies. 

The presence at the BBB of members of the multidrug resistance-associated protein (MRPs) family, whose members preferentially transport anionic compounds, is still controversial. The seven members of the MRP family belong, like P-gp, to the ATP-binding cassette (ABC) protein superfamily. Mrpl has been found at the BBB in isolated rat brain capillaries, primary cultures of brain capillary endothelial cells and in immortalized capillary endothelial cells, but not in human brain capillaries [59]. Another member, MRP2 has been found at the luminal membrane of the brain endothelial cells [60]. However, further studies are required to show that there are MRP transporters at the BBB (Figure 15.5). As for P-gp, a functional Mrpl was found in primary cultured rat astrocytes [56] and it has been shown to take part in the release of glutathione disulfide from brain astrocytes under oxidative stress [61]. 

Chemical Synthesis and Biological Studies of the Epothilones - Microtubule Stabilizing Agents with Enhanced Activity Against Multidrug-Resistant Cell Lines and Tumors. 

Jason Kindrachuk is a postdoctoral fellow at the University of British Columbia (UBC) in the laboratory of Professor R. E. W. Hancock. Jason received his Ph.D. from the University of Saskatchewan in 2007 where his research focused on host and pathogen sensory systems. During his study he specially focused on TLR-9 receptor—ligand interactions and the interactions between host defense peptides and the PhoPQ two-component sensory system of Salmonella typhimurium. In 2008 Jason received the Canadian Cystic Fibrosis Foundation Kin Canada Fellowship for his research in the area of alternative therapies for treatment of antibiotic- and multidrug-resistant bacteria. Currently his research is focused on the investigation of structure-activity relationships amongst natural and synthetic host defense peptides from the perspective of associated immunomodulatory activities and as well as vaccine formulation strategies. 

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