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Volumn 15, Issue 24, 2005, Pages 5562-5566

Estrogen receptor β selective ligands: Discovery and SAR of novel heterocyclic ligands

Author keywords

ER beta selective ligands; Estrogen receptor

Indexed keywords

ANILINE DERIVATIVE; BENZENE DERIVATIVE; BENZIMIDAZOLE DERIVATIVE; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; GENISTEIN; HETEROCYCLIC COMPOUND; IMIDAZOLE DERIVATIVE; INDOLE DERIVATIVE; ISOXAZOLE DERIVATIVE; L 384M; LIGAND; M 421I; SELECTIVE ESTROGEN RECEPTOR MODULATOR; UNCLASSIFIED DRUG;

EID: 27644480409     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2005.08.010     Document Type: Article
Times cited : (31)

References (35)
  • 15
    • 27644457751 scopus 로고    scopus 로고
    • Unpublished data.
    • Wessel, M. Unpublished data.
    • Wessel, M.1
  • 28
    • 0004093293 scopus 로고
    • B. Green R.E. Leake Roe IRL Press Oxford
    • 3H]estradiol. After 16 h at 4°C, dextran-coated charcoal (20 μL) was added. After 15 min at room temperature, the charcoal was removed by centrifugation and the radioactive ligand present in the supernatant was measured by scintillation counting. All reagents were obtained from Sigma (St. Louis, MO).
    • (1990) Steroid Hormone Receptors a Practical Approach , pp. 67-92
    • Leake, R.E.1    Habib, F.2
  • 29
    • 27644462598 scopus 로고    scopus 로고
    • 2,3-Diphenyl Indole CAS # 3469-20-3. MP BioMedicals 15 Morgan, Irvine, CA 92618-2005.
    • 2,3-Diphenyl Indole CAS # 3469-20-3. MP BioMedicals 15 Morgan, Irvine, CA 92618-2005.
  • 31
    • 27644466222 scopus 로고    scopus 로고
    • note
    • We used the Sybyl program (Tripos Associates, St. Louis, MO.) for docking structures 7c manually into the active sites of ER-α and ER-β crystal structures (pdb codes 1L2I,1QKM, respectively). The compounds were manually overlapped with the co-crystallized ligands and then allowed to relax in the active site of the protein using the Sybyl force field, Gasteiger-Huckel charges on the ligands, and Kollman All Atom charges on the protein. The phenolic substituents of each structure were held in place to mimic the phenolic substituents of the co-crystallized ligands. The resulting conformations were then used to analyze contact points between the protein and the ligand for the purpose of explaining potential selectivity differences in the active sites of ER-α and ER-β based on our predicated binding modes.
  • 35
    • 0031791153 scopus 로고    scopus 로고
    • Whole cell assays. Estrogenic activity in human breast cancer MCF7 cells and primary rat granulosa cells was assessed by transient transfection of an estrogen responsive ERE3-TK-lux luciferase reporter vector essentially as we have described previously in other cell backgrounds (Petersen et al.). The MCF7 cell activity was considered to be mediated through ER-α and the granulosa activity was considered to be mediated through ER-β. MCF7 cells were obtained from ATTC (Manassas, VA) and transfected with Lipofectamine Plus (Gibco/BRL, Rockville, MD), as described by the manufacturers. Luciferase activity was measured 24 h after the addition of compounds. D.N. Petersen, G.T. Tkalcevic, P.H. Koza-Taylor, T.G. Turi, and T.A. Brown Endocrinology 139 1998 1082
    • (1998) Endocrinology , vol.139 , pp. 1082
    • Petersen, D.N.1    Tkalcevic, G.T.2    Koza-Taylor, P.H.3    Turi, T.G.4    Brown, T.A.5


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.