ArticleJournal of advanced research2026
Development and characterization of endolysosomal trafficking targeting chimera degraders of α
Article in Journal of advanced research, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.
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Abstract
introductionDespite the booming targeted protein degradation technologies, degrading cell membrane proteins remains an enormous challenge. In particular, only a limited approach is appropriate for the degradation of the G protein-coupled receptor (GPCR) superfamily. It is encouraging that accelerating GPCRs' endocytosis and switching their post-endocytic fate from recycling to lysosomal degradation would represent a promising strategy for developing chemical degraders of GPCRs.
objectivesThis study aimed to elucidate the mechanism underlying post-endocytic sorting of internalized α
methodsThe protein-protein interaction (PPI) of GASP1, Beclin 2, and α
resultsMechanistically, the binding of Beclin 2 to GASP1 is crucial to the endolysosomal sorting and degradation of α
conclusionsProof-of-concept studies of the ETTAC degraders for GPCR successfully elucidate the roles of post-endocytic sorting proteins and applied to directing the lysosomal degradation of α
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