molecules of the month

“Compound 10”

XIAP E3-ligase degrader via SM ubiquitylation

novel mechanism of induced degradation

from derivatization of XIAP-binder

Journal of the American Chemical Society

Genentech, San Francisco, US

Chemical structure of compound 10 Genentech XIAP E3-ligase degrader
1 min read

The Genentech XIAP E3-ligase degrader, compound 10, has an interesting mechanism of action, triggering the degradation of its target (XIAP) by ubiquitylation of the small molecule. The molecule behaves as a lysine mimetic, accepting ubiquitin from the targeted E3 complex, promoting XIAP’s own degradation. As E3 ligases are often difficult to drug, this “K-tag” approach adds an interesting new concept to the toolbox, which may be easier to translate into drugs than heterobifunctional degraders which tend to be much larger and less synthetically accessible.

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