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Lecture 18

CHEM 437 Lecture Notes - Lecture 18: Chromogenic, Ic50, Chromophore


Department
Chemistry
Course Code
CHEM 437
Professor
Hoff
Lecture
18

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Chem 437!
March 14/2017!
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5.3 Nuclear receptors!
"- repetition and reinforcement of lesson from gPCRs!
5.4 Penicillin Binding proteins!
"-PBPs from irreversible drug target interactions!
"- Assays drug + target not at equilibrium!
"- How to measure?!
1) Enzymology!
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"E+S <-Km-> ES -kcat-> E+P!
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"E+I <-Ki-> EI -Kinactive-> EI* (DEAD)!
Vmax changes with longer exposure to I (bc less enzyme around to do run)!
Determine Vmax at dierent 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!
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2) Pre-incubations (screening)!
just add irreversible inhibitor then determine IC50!
chromogenic substrates!
PNP!
Characteristics of a good one:!
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""""""""""strong absorber!
"""""""""""Push pull chromophore!
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"""Donor!
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Low energy excited states. Homo lumo has much charge transfer character!
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