Anticancer drug synthesis/testing, cancer drugs and targets, kinases, specificity and effectiveness

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Colorado State University
Life Science
LIFE 210
Paul Laybourn

12 September Anticancer Drug Synthesis and Testing Drug Design Overview Aspirin Has three functional groups The original source – white willow tree bark tea New drugs derived by redesign of aspirin to form new analgesics Antibiotics – Penicillin Original source – fungus Penicillium notatatum Active agent identified and purified Penicillin G New variants ampicillin, oxacillin, cloxacillin, penicillin O and amoxicillin Paul Ehrlich, in early 1900’s Searched for a “magic bullet” to cure syphilis Systematically changed small molecules Assessed activity Approach now known as a “structure – activity relationship study” Small Molecule Drugs “Active Area” Bind through their specific shape/fit and functional group non covalent interactions Function through binding in place of the normal ligand (hormone, &c.) Example: the opiate morphine Difficult to synthesize “Active area” incorporate into a simpler, more easily synthesized molecule Demerol Demerol still binds and has opiate activity Computer modeling is now used, based on these same principles, to design potential new drugs Combinatorial chemistry Synthesis of large “libraries” of molecules Use high throughput screening for most effective molecules Greatly reduced costs Cancer Drugs and Targets Drugs Low molecular weight Easier to synthesize More likely to enter tumors or cells Targets “Druggable” Proteins with enzymatic function Have defined actives site cleft for drug binding site Kinases are good candidates 518 in human “kinome”, 90 are tyrosine kinases Hormone receptor binding sites also good candidates Tamoxifen for the estrogen receptor Ras GTPase site is not a good candidate, inhibitory drug would promote cancer Kinases Share similar structur
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