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Chemical Compound Review

CHEMBL279301     4-[(E)-1-[4-(2- dimethylaminoethoxy)phenyl]...

Synonyms: SureCN640496, AKOS015894466, BCP9000165, BCP9000243, FT-0647372, ...
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Disease relevance of nchembio775-comp3


Psychiatry related information on nchembio775-comp3


High impact information on nchembio775-comp3

  • To investigate the functions of the p53 tumor suppressor, we created a new knock-in gene replacement mouse model in which the endogenous Trp53 gene is substituted by one encoding p53ER(TAM), a p53 fusion protein whose function is completely dependent on ectopic provision of 4-hydroxytamoxifen [7].
  • Here we report the crystal structure of the human estrogen receptor alpha (hER alpha) ligand-binding domain (LBD) bound to both the agonist diethylstilbestrol (DES) and a peptide derived from the NR box II region of the coactivator GRIP1 and the crystal structure of the hER alpha LBD bound to the selective antagonist 4-hydroxytamoxifen (OHT) [8].
  • Mutant receptors in which the ligand binding cavity is filled up by bulkier side chains still interact with SRC-1 in vitro and are transcriptionally active in vivo, but are no longer efficiently inactivated by diethylstilbestrol or 4-hydroxytamoxifen [9].
  • BACKGROUND: Human sulfotransferase 1A1 (SULT1A1) catalyzes the sulfation of a variety of phenolic and estrogenic compounds, including 4-hydroxytamoxifen (4-OH TAM), the active metabolite of tamoxifen [10].
  • Crucially, addition of the anti-estrogen 4-hydroxytamoxifen caused a differential recruitment in vivo of ERalpha and ERbeta onto the hTERT promoter and inhibited telomerase activity [11].

Chemical compound and disease context of nchembio775-comp3


Biological context of nchembio775-comp3


Anatomical context of nchembio775-comp3


Associations of nchembio775-comp3 with other chemical compounds


Gene context of nchembio775-comp3


Analytical, diagnostic and therapeutic context of nchembio775-comp3


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