estrogen receptor degrader AC699
An orally bioavailable estrogen receptor (ER)-targeted chimeric protein degrader composed of ligands of ER and cereblon (CRBN) E3 ubiquitin ligase, with potential antineoplastic activity. Upon oral administration of ER degrader AC699, the ER-targeting moiety targets and binds to ER, and the CRBN-binding moiety recruits CRBN, a component of the CRL4-CRBN E3 ubiquitin ligase complex. This catalyzes ubiquitination and proteasome-mediated degradation of ER, prevents ER-mediated signaling, and inhibits both the growth and survival of ER-expressing cancer cells. ER is overexpressed in a variety of cancers and plays a key role in cancer cell proliferation.
| Synonym: | ER degrader AC699 ER-targeting chimeric protein degrader AC699 |
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| Code name: | AC 699 AC-699 AC699 |