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)

• Record Type: Journal Article
• Authors: Matinkhoo, Kaveh; Pryyma, Alla; Wong, Antonio A. W. L.; Perrin, David M.
• Is Part Of: Chemical communications. Volume 57:Issue 75(2021)
• Page Start: 9558
• Page End: 9561
• Publication Date: 2021-08-27
• Subjects: Chemistry -- Periodicals; 540
• DOI: 10.1039/d1cc03279h
• Languages: English
• ISSNs: 1359-7345

Abstract

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.