GPER partial agonist
G protein-coupled estrogen receptor (GPER) partial agonist
- Fast, non-genomic estrogen signaling
- Distinct from the slow nuclear ERα/ERβ transcriptional actions
Drugs with this mechanism (1)
- Tamoxifen — The classic breast-cancer SERM; a prodrug activated by CYP2D6.
Self-check
- Where is the GPER activated by partial agonists located?
At the membrane. - How does GPER signaling differ from nuclear ERα/ERβ signaling?
It is fast and non-genomic; nuclear signaling is slow and transcriptional.
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