Synthesis and evaluation of "Ama-Flash", a photocaged amatoxin prodrug for light-activated RNA Pol II inhibition and cell death. Issue 75 (27th August 2021) - Matinkhoo, Kaveh
Abstract : It's now a matter of light and death. A non-toxic photoactivatable amatoxin, Ama-Flash is synthesized and evaluated on cells wherein it remains non-toxic until photoactivation. Abstract : Amanitin is used extensively as a research tool to inhibit RNA Pol II thereby implicating its role in mRNA transcription. Recently, amanitin has gained traction as a toxic payload for targeted therapy. Here we report the first-ever photocaged amanitin analog, that is non-toxic and can be pre-loaded into cells. Light provides a means to inhibit RNA Pol II and provoke cell death on-demand.