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

Chetan K. Chana, Pierre Maisonneuve, Ganna Posternak, Nicolas G.A. Grinberg, Juline Poirson, Samara Mishelle Ona, Derek F. Ceccarelli, P. Mäder, Daniel J. St‐Cyr, Victor P.T. Pau,

Journal of Medicinal Chemistry · 2022 · 54 citations · 44 references

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Abstract

of 558 nM in cells with strong selectivity for GID4. X-ray co-structure determination revealed the basis for GID4-small molecule interactions. These results position GID4-CTLH as an E3 for TPD and provide candidate scaffolds for high-affinity moieties that bind GID4.

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