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Methyl-piperidino-pyrazole (MPP), an estrogen receptor α (ERα)-selective antagonist we developed, has a basic side chain (BSC) attached to an ERα-selective agonist ligand, methyl-pyrazole-triol (MPT) through an ether linkage. To remove the possibility that metabolic cleavage of the BSC in MPP would regenerate MPT, we have replaced the N-piperidinylethoxy moiety with an N-piperidinylpropyl group, giving...
The estrogen receptor (ER) α is a hormone-inducible transcription factor that has a pivotal physiological role. Intriguingly, a clear and undisputed physiological function of the recently described ERβ remains elusive, with the exception of the ovary where a cooperative role of ERα and ERβ has been demonstrated. We have, therefore, investigated whether endogenous ERs, in particular ERβ, act as ligand-inducible...
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