The world's first wiki where authorship really matters (Nature Genetics, 2008). Due credit and reputation for authors. Imagine a global collaborative knowledge base for original thoughts. Search thousands of articles and collaborate with scientists around the globe.

wikigene or wiki gene protein drug chemical gene disease author authorship tracking collaborative publishing evolutionary knowledge reputation system wiki2.0 global collaboration genes proteins drugs chemicals diseases compound
Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
Chemical Compound Review

CHEMBL10030     [6-hydroxy-2-(4- hydroxyphenyl)benzothiophe...

Synonyms: SureCN4884822, CHEBI:106886, Lilly 117018, KST-1A7098, AC1L2XRN, ...
 
 
Welcome! If you are familiar with the subject of this article, you can contribute to this open access knowledge base by deleting incorrect information, restructuring or completely rewriting any text. Read more.
 

Disease relevance of LY-117018

 

High impact information on LY-117018

  • Interestingly, soluble ER bound by LY 117018 did not produce this decreased mobility complex, suggesting that it was specific to the nuclear form of the ER antagonist complex [2].
  • In a competitive binding assay, LY 117018 competes for [3H]estradiol binding to its cytosol receptor with the same Ki in both MCF-7 and LY2 cells [1].
  • Since this serum site has little affinity for the benzythiophene antiestrogens (LY 117018 and 156758), we have chosen the name of triphenylethylene-antiestrogen binding site (TABS) [3].
  • Intact female Sprague-Dawley rats (195-249 g) and rats that had been ovariectomized (210-285 g) were injected subcutaneously for 14 days with ethinyl estradiol (15 micrograms/kg), the antiestrogen LY 117018 (500 micrograms/kg), both drugs simultaneously, or the vehicle (sesame oil) alone [4].
  • LY 117018 increased PR mRNA expression 8% while ICI 182,780 did not increase PR mRNA expression at all [5].
 

Biological context of LY-117018

 

Anatomical context of LY-117018

  • Comparison of the biological effects of tamoxifen and a new antioestrogen (LY 117018) on the immature rat uterus [8].
  • To investigate the "in vitro" properties of LY 139478 on osteoclast precursors, the human pre-osteoclastic cell line FLG 29.1 was examined for evidence of bioeffects of this compound [7].
  • The chronic administration of LY 117018 in fertile rats significantly decreased beta-EP content in the anterior pituitary, hippocampus and plasma (p < 0.01), while it increased beta-EP hypothalamic content and did not change beta-EP content in the neurointermediate lobe [9].
  • The administration of 17 beta-estradiol or LY 117018 in ovx rats significantly increased beta-EP concentration in the anterior and neurointermediate pituitary lobe, in the hypothalamus and plasma (p < 0.01), though they did not significantly modify hippocampal beta-EP content [9].
 

Associations of LY-117018 with other chemical compounds

  • The uterotrophic and antiuterotrophic activities of tamoxifen and 6-hydroxy-2-(p-hydroxyphenyl)-benzo(b)thien-3-yl p- less than 2-(1-pyrrolidinyl) ethoxyphenyl ketone (LY 117018) in the immature rat uterus have been evaluated [8].
 

Gene context of LY-117018

 

Analytical, diagnostic and therapeutic context of LY-117018

References

  1. Selection and characterization of a breast cancer cell line resistant to the antiestrogen LY 117018. Bronzert, D.A., Greene, G.L., Lippman, M.E. Endocrinology (1985) [Pubmed]
  2. Uterine estrogen receptor-DNA complexes: effects of different ERE sequences, ligands, and receptor forms. Curtis, S.W., Korach, K.S. Mol. Endocrinol. (1991) [Pubmed]
  3. Characterization of a triphenylethylene-antiestrogen-binding site on rat serum low density lipoprotein. Winneker, R.C., Guthrie, S.C., Clark, J.H. Endocrinology (1983) [Pubmed]
  4. Effects of the antiestrogen LY 117018 on the modulation by ethinyl estradiol of the metabolism of [1-14C]oleic acid by perfused livers from normal and ovariectomized rats. Weinstein, I., Heimberg, M. Biochem. Pharmacol. (1988) [Pubmed]
  5. Target specificity of selective estrogen receptor modulators within human endometrial cancer cells. Bramlett, K.S., Burris, T.P. J. Steroid Biochem. Mol. Biol. (2003) [Pubmed]
  6. Effects of LY-117018 HCl on bone remodeling and mineral density in the oophorectomized rat. Curiel, M.D., Calero, J.A., Guerrero, R., Gala, J., Gazapo, R., de la Piedra, C. Am. J. Obstet. Gynecol. (1998) [Pubmed]
  7. Evidence for bioeffects of LY 139478 on the human pre-osteoclastic cell line FLG 29.1. Fiorelli, G., Gori, F., Frediani, U., Morelli, A.M., Falchetti, A., Benvenuti, S., Masi, L., Brandi, M.L. Biochem. Biophys. Res. Commun. (1995) [Pubmed]
  8. Comparison of the biological effects of tamoxifen and a new antioestrogen (LY 117018) on the immature rat uterus. Wakeling, A.E., O'Connor, K.M., Newboult, E. J. Endocrinol. (1983) [Pubmed]
  9. Raloxifene analog LY 117018 effects on central and peripheral beta-endorphin. Genazzani, A.R., Bernardi, F., Stomati, M., Rubino, S., Giardina, L., Luisi, S., Monteleone, P., Genazzani, A.D., Luisi, M., Petraglia, F. Gynecol. Endocrinol. (1999) [Pubmed]
  10. Inhibition of LDL oxidation by a new estradiol receptor modulator compound LY-139478, comparative effect with other steroids. Rattan, A.K., Arad, Y. Atherosclerosis (1998) [Pubmed]
  11. Effects of estradiol and raloxifene analog on brain, adrenal and serum allopregnanolone content in fertile and ovariectomized female rats. Genazzani, A.R., Bernardi, F., Stomati, M., Monteleone, P., Luisi, S., Rubino, S., Farzati, A., Casarosa, E., Luisi, M., Petraglia, F. Neuroendocrinology (2000) [Pubmed]
 
WikiGenes - Universities