Topo I inhibitors for TB

What is it about?

We used a homology model of Mycobacterium tuberculosis topoisomerase I and docked approved drugs. We identified two novel inhibitors in vitro, imipramine and norclomipramine. The binding of these molecules was characterized through extensive experiments. We propose they bind near the metal binding site of the enzyme

Featured Image

Why is it important?

Small molecule inhibitors of Mtb Topo I had not previously been identified. By finding known drugs it has stimulated the search for similar molecules.

Perspectives