CHEM 437 Lecture Notes - Lecture 18: Chromogenic, Ic50, Chromophore
Document Summary
Repetition and reinforcement of lesson from gpcrs. Assays drug + target not at equilibrium. Vmax changes with longer exposure to i (bc less enzyme around to do run) Determine vmax at di erent amounts of time with i this gives: rate inactive = kinactive not a good way to drive drug development bc it takes a long time to determine for each and every drug. Excellent science but slow: pre-incubations (screening) just add irreversible inhibitor then determine ic50 chromogenic substrates. R-oh = weaker push look for structural features that look like the enzymes wants to bind and process. Four classes of proteases serine proteases cysteine proteases soft electrophiles, vinyl sulfones or epoxides metalloproteases make a single water nucelophilic aspartic proteases. Proteases select and bind their substrates prior to cleaving them. Add electrophilic group to react with nucleophilic residue (warhead) > selective covalent inhibitor typically a peptide with a di erent head on it.
