Quarfloxin (Quadruplexes in the clinic)

As I've mentioned before, I'm a booster for DNA G-quadruplexes as drug targets. While telomeres might not be the best target, there are lots of potentially oncogenically relevant quadruplexes. Here is the only quadruplex-targeting antineoplastic that's made it into the clinic that I know of.

i-151c91df6b7a91cae0f7eac8b3b15db8-quarfloxin.png

Quarfloxin, predictably, has a large aromatic surface area and a chirally disposed positive charge - perfect for targeting a groove or loop. It has shown great promise in early clinical work (it's currently in phase II) - I am rooting for the class!

Tags

More like this