Enzastaurin is a compound that is under clinical investigation as anti-cancer drug. It has been developed as inhibitor of protein kinase beta, a serine/threonine kinase that is often found highly activated in cancer cells and that contributes to cancer cell aggressiveness. A research team including Martin Michaelis, Professor of Cell Biology in Kent, discovered that enzastaurin also inhibits ABCB1 (also known as P-glycoprotein), an efflux pump that transports many different anti-cancer drugs out of cells and that is known to be involved in multi-drug resistance in cancer cells. This offers future opportunities to develop strategies the circumvent common mechanisms of resistance.
The research was published in the journal Oncotarget and is available for open access here.