FOLATE-ANTIBODY CONJUGATES AS LYSOSOME TARGETING DEGRADERS

Abstract: provided herein are bifunctional lysosomal targeting degraders that comprise folate or a folate analog configured to bind to folate receptor as a shuttle molecule for lysosome degradation, and a protein binder configured to bind a membrane or extracellular protein of interest. the bifunctional degraders find use, e.g., for selectively targeted degradation of membrane and extracellular proteins via the endosomal/lysosomal pathway. also provided herein are compositions comprising the bifunctional degraders, as well as methods of using the bifunctional degraders.

Inventor(s): Weiping Tang, Yaxian Zhou, Chunrong Li, Hao Wu

CPC Classification: A61K47/551 (the modifying agent being also a pharmacologically or therapeutically active agent, i.e. the entire conjugate being a codrug, i.e. a dimer, oligomer or polymer of pharmacologically or therapeutically active compounds)

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