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Lecture 11 Web: pollev.com/ucibio Text: To: 37607 Type in: 169964 <your question> Lecture 11 objectives Understand irreversible enzyme inhibition Understand how enzyme kinetics relates to drug discovery Understand the differences between basic and applied research Apply enzyme kinetic principles to understand metabolic pathway regulation Enzyme kinetics Thermodynamics determine spontaneity and rate Enzymes change rate by lowering Ea Enzymes fold into precise 3D shapes MM equation approximates enzyme kinetics Enzymes can be regulated “Irreversible” regulation Covalent modification of enzymes Eg: Phosphorylation Kinase Active Inactive E1 E1-PO4 Phosphatas e Irreversible inhibitors Bind enzyme very tightly Very often at active site Very often covalently binds active site “Suicide” inhibitors Making new drugs Identify targets Find candidate drugs Effective concentration VS toxic concentration Phases of clinical trials Societal implications of discovery pipeline http://clinuity.com/blog/2009/11/chart-of-the-day-drug-approval-pipeline/ Societal implications of discovery pipeline Identify targets Find candidate drugs Effective concentration VS toxic concentration Phases of clinical trials Failure rates Time from discovery Market? Money, money, money What does basic research do for me? Identify targets Identify candidates Drives technological innovations Different approaches to curing disease Less worried about short term economic return Regulating pathways A E1 B E2 C E3 D E4 Convert A E ONLY when needed Intermediates have no role Therefore first COMMITTED step Regulate PATHWAY not necessarily reactions FEEDBACK INHIBITION E Complex pathways A E1 B E2 C E4 E3 D Can have many different regulation points Feedback + FEEDFORWARD E How to study a pathway? A E1 B E2 C E3 D E4 E Studying pathways Submit assignment to “Studying pathways” Midnight tonight Carbs - Isomers Carbohydrates = HUGE Diversity “Isomers” - Constitutional/Structural - Stereo - Enantiomers - Diastereomers - Epimers - Anomers Isomers Select best isomer description for the two molecules below: A. Epimers B. Anomers C. Enantiomers D. Diastereomers E. None/Other Carbohydrate diversity increased by cyclization! Carbohydrate diversity increased by cyclization!
