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Sep. 18, 2021

Zotatifin: A First-In-Class eIF4A RNA Helicase Inhibitor

eFT226 (zotatifin)

first-in-class eIF4A RNA helicase inhibitor in clinical dev. for solid tumors (Ph. I, IV QW) from optimization of a natural product J. Med. Chem., May 29, 2020 eFFECTOR Therapeutics, San Diego, CA

drughunter.com
Drug Hunter Team

eFT226 (zotatifin) is a beautiful natural product-derived molecule that inhibits the RNA helicase eIF4A by forming a ternary complex between it, eIF4A, and polypurine RNA. Interestingly, the stability of the ternary complex depends on the RNA sequence bound to eIF4A, with greatest activity for AGAGAG-based complexes. The molecule demonstrates [...]

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