Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4

Expansion of the E3 ligase toolbox has the potential to dramatically advance the field of targeted protein degradation.  WuXi AppTec scientists recently contributed to a research article in the Journal of Medicinal Chemistry describing the discovery of novel small molecule binders of GID4, a substrate receptor in the human CTLH E3 ligase complex.  Researchers used both fragment-based NMR and DNA-encoded library (DEL) screening to identify high affinity binders to GID4, while also demonstrating the ability of GID4 to induce the degradation of a protein substrate when brought into close proximity.

https://pubmed.ncbi.nlm.nih.gov/36117290/

Discovery and Structural Characterization of Small Molecule Binders of the Human CTLH E3 Ligase Subunit GID4

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