LIFE 210 Study Guide - Quiz Guide: High-Throughput Screening, Combinatorial Chemistry, Salix Alba
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The original source white willow tree bark tea. New drugs derived by redesign of aspirin to form new analgesics. New variants ampicillin, oxacillin, cloxacillin, penicillin o and amoxicillin. Searched for a magic bullet to cure syphilis. Approach now known as a structure activity relationship study . Bind through their specific shape/fit and functional group non covalent interactions. Function through binding in place of the normal ligand (hormone, &c. ) Active area incorporate into a simpler, more easily synthesized molecule demerol. Computer modeling is now used, based on these same principles, to design potential new drugs. Use high throughput screening for most effective molecules. Have defined actives site cleft for drug binding site. 518 in human kinome , 90 are tyrosine kinases. Ras gtpase site is not a good candidate, inhibitory drug would promote cancer. Tyrosine kinases are very similar structurally and are particularly involved in cancer. Rational drug design to target kinases malfunctioning in cancer cells.
