Exploring Enzyme Activity

Early Nineteenth Century engraving of a black rat similar to that which carried the fleas that spread the bubonic plague in crowded urban areas during the Great Plague of London, an outbreak which killed some 70, 000 persons.

Source: Google Arts & Culture

In today’s session the students explored enzyme activity in more mathematical depth, including specific activity and dissociation constants.

They then learned about types of inhibitors and drug design. Though the example of methotrexate (MTX) for use in inhibiting the enzyme dihydrofolate reductase in treating anthrax, we discussed how MTX functions as an inhibitor. We have also identified important differences between MTX and the substrate that allows for tighter binding in the active site. Using the program ChimeraX, the students then looked at the structure of DHFR from anthrax bound to MTX in order to propose changes to MTX to generate a more effective drug for treatment.