Great question! Basically, efflux pumps are features of the bacterial cell that allow it to jettison foreign materials or toxins. So if we were to test the brinzolamide alongside an efflux pump inhibitor, it might give us some clues as to whether the ineffectiveness of the brinzomalide that we observed was due to the bacteria’s ability to remove it from the cell.
I think versions of the experiment that would include an efflux pump inhibitor would be similar to the ones we conducted here–we would introduce an efflux pump inhibitor into all of our wells containing to bacteria and evaluate whether the brinzolamide plus the inhibitor had any measurable effect on bacterial growth.
This is a really good question and is a complex one! Generally, medicinal chemists alter the functional groups on a given compound to change properties that may facilitate its entry into the cell. As far as I know there’s no one specific way to do this, but involves a ton of trial and error for each specific compound that a chemist works with.
In the conclusion it states that it might be possible that the outer layer might have blocked the entry way into the cell, so if that is the case is there a way to get past that our would a new compound need to be used?
Thanks for this question! I think there are options for both, actually! Sometimes, researchers will make genetic modifications to the bacterial cells to make them hyperpermeable, making them extra sensitive to the effects of any potential antibiotics. We would definitely be interested in seeing how our compound worked in such cells. The other option would be to modify the structure of brinzolamide (e.g., making small changes to its functional groups), which might change its properties such that it would have an easier time entering the bacterial cells.
How would you conduct an experiment with brinzolamide and an efflux pump inhibitor to test the effectiveness of the drug?
Great question! Basically, efflux pumps are features of the bacterial cell that allow it to jettison foreign materials or toxins. So if we were to test the brinzolamide alongside an efflux pump inhibitor, it might give us some clues as to whether the ineffectiveness of the brinzomalide that we observed was due to the bacteria’s ability to remove it from the cell.
I think versions of the experiment that would include an efflux pump inhibitor would be similar to the ones we conducted here–we would introduce an efflux pump inhibitor into all of our wells containing to bacteria and evaluate whether the brinzolamide plus the inhibitor had any measurable effect on bacterial growth.
It’s also potentially an option to genetically modify the bacterial genes to mutate the efflux pumps, which may allow for similar conclusions.
How could brinzolamide be altered to better enter into bacterial cells?
This is a really good question and is a complex one! Generally, medicinal chemists alter the functional groups on a given compound to change properties that may facilitate its entry into the cell. As far as I know there’s no one specific way to do this, but involves a ton of trial and error for each specific compound that a chemist works with.
what kind of structural modifications would have to be made in order for the brinzolamide to enter the cell?
Thanks for the question! Please see my response to Maria’s question above.
what kind of structural modifications would have to be made so that brinzolomide can enter the bacterial cell?
In the conclusion it states that it might be possible that the outer layer might have blocked the entry way into the cell, so if that is the case is there a way to get past that our would a new compound need to be used?
Thanks for this question! I think there are options for both, actually! Sometimes, researchers will make genetic modifications to the bacterial cells to make them hyperpermeable, making them extra sensitive to the effects of any potential antibiotics. We would definitely be interested in seeing how our compound worked in such cells. The other option would be to modify the structure of brinzolamide (e.g., making small changes to its functional groups), which might change its properties such that it would have an easier time entering the bacterial cells.
what structural changes would have to be made so that brinzolamide can enter the bacterial cell?
ps. sorry if this is like the 3rd post, i cant tell if its going through