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LIFE 210 (38)

Drug resistant cancer, ATP-dependent transporters, PGP

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Colorado State University
Life Science
LIFE 210
Paul Laybourn

23 September Introduction/Overview Blood cancers and malignant/metastatic cancers (~50%) are treated with chemotherapy (not localized) Some patients are cured, but some do not respond due to drug resistant cancers Drug resistant cancer arises through a range of mechanisms Drug target changes, like Bcr-Abl protein catalytic site changes that affect Gleevec binding affinity More general multidrug resistant (MDR), conferring resistance to several drugs Impaired drug delivery – concentration in blood and tumor Cellular changes, include Increased DNA repair rate Blockage of programmed cell death Detoxifying system (cyt P45) activation Decreased cell uptake by transporters (polar drugs) Increased cell export by ATP-dependent pumps (ABC family of transporters of nonpolar drugs) ATP-Dependent Transporters (ABC family) Multidrug transporter P-glycoprotein (PGP) Encoded by MDR1 gene Binds hydrophobic, neutral or positively charged drugs The binding site is in the lipid bilayer hydrophobic core Has broad nonpolar substrate specificity Its normal functions are protective, keeping toxins out Blood-brain barrier and blood-cerebrospinal fluid barrier Testicular tissues Developing fetus (placenta) Stem cells Liver, intestinal tract and kidney Excrete toxins from body Stem Cells Exclude Fluoresce
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