Compound class:
Synthetic organic
Comment: PHTPP-1304 is a novel protein degrader [1-2]. It binds to the estrogen receptor β via the ERβ antagonist PHTPP domain, and simultaneously to the autophagy receptor p62, to target the ERβ . This class of degrader is called an AUTOphagy-TArgeting Chimera, or AUTOTAC. AUTOTACs can be designed to target proteins of interest to autophagic membranes where they undergo lysosomal degradation, in a proteasome-independent manner.
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Bioactivity Comments |
PHTPP-1304 has a half-degrading concentration (DC50) for ERβ of ~2 nM in HEK293T cells. Binding affinity for ERβ is expected to be similar to that for the parent antagonist PHTPP. |