Chem 219 Perturbing Biomolecules in Cells Questions with Correct Solutions

Chem 219 Perturbing Biomolecules in Cells Questions with Correct Solutions What is a tight or weak binder for small molecule inhibitors - Answer -tight binder: KD < 1nm weak binder KD > 1mM Rules for drug candidates for SM - Answer -if compounds have two+ will not be a good uptake into cell - MW >500 (now 750) - 5+ H-bond donors (too polar) - Sum of N's and O' > 10 (too polar) - C*log P > 5 (too greasy) Draw reaction coordinate diagram of how enzyme changes reaction. What does it stabilize? - Answer - check drawing stabilizes TS Draw case study and TS inhibitor for SM - Answer -check drawing Draw how fragment-based drug discovery is done - Answer -check drawing draw the general strategy for regulating protein expression/activity - Answer -check drawing