Molecular determinants of tissue selectivity in estrogen receptor modulators

Cloning of a novel receptor expressed in rat prostate and ovary.

1996 • 4,782 citations

ERβ: Identification and characterization of a novel human estrogen receptor

1996 • 2,262 citations

Quantum chemistry program exchange

1987 • 1,001 citations

Role of the two activating domains of the oestrogen receptor in the cell-type and promoter-context dependent agonistic activity of the anti-oestrogen 4-hydroxytamoxifen.

1990 • 772 citations

Tamoxifen activation of the estrogen receptor/AP-1 pathway: potential origin for the cell-specific estrogen-like effects of antiestrogens.

1995 • 665 citations

Human estrogen receptor transactivational capacity is determined by both cellular and promoter context and mediated by two functionally distinct intramolecular regions.

1994 • 649 citations

Raloxifene (LY139481 HCI) prevents bone loss and reduces serum cholesterol without causing uterine hypertrophy in ovariectomized rats.

1994 • 614 citations

The estradiol pharmacophore: Ligand structure-estrogen receptor binding affinity relationships and a model for the receptor binding site

1997 • 611 citations

Effects of tamoxifen on uterus and ovaries of postmenopausal women in a randomised breast cancer prevention trial

1994 • 531 citations

Tripartite steroid hormone receptor pharmacology: interaction with multiple effector sites as a basis for the cell- and promoter-specific action of these hormones.

1996 • 505 citations

Analysis of estrogen receptor function in vitro reveals three distinct classes of antiestrogens.

1995 • 502 citations

A MONOHYDROXYLATED METABOLITE OF TAMOXIFEN WITH POTENT ANTIOESTROGENIC ACTIVITY

1977 • 502 citations

Identification of an Estrogen Response Element Activated by Metabolites of 17β-Estradiol and Raloxifene

1996 • 432 citations

A controlled trial of raloxifene (LY139481) HCl: Impact on bone turnover and serum lipid profile in healthy postmenopausal women

1996 • 362 citations

Raloxifene, tamoxifen, nafoxidine, or estrogen effects on reproductive and nonreproductive tissues in ovariectomized rats

1996 • 285 citations

Antiestrogens. 2. Structure-activity studies in a series of 3-aroyl-2-arylbenzo[b]thiophene derivatives leading to [6-hydroxy-2-(4-hydroxyphenyl)benzo[b]thien-3-yl]-[4-[2-(1-piperidinyl)ethoxy]phenyl]methanone hydrochloride (LY 156758), a remarkably effective estrogen antagonist with only minimal intrinsic estrogenicity

1984 • 280 citations

Transcriptional activation by the estrogen receptor requires a conformational change in the ligand binding domain.

1993 • 249 citations

Novel antioestrogens without partial agonist activity

1988 • 215 citations

Discovery and Synthesis of [6-Hydroxy-3-[4-[2-(1-piperidinyl)ethoxy]phenoxy]- 2-(4-hydroxyphenyl)]benzo[b]thiophene: A Novel, Highly Potent, Selective Estrogen Receptor Modulator

1997 • 175 citations

Structure−Activity Relationships of Selective Estrogen Receptor Modulators: Modifications to the 2-Arylbenzothiophene Core of Raloxifene

1997 • 172 citations

Environmental estrogens: Effects on cholesterol lowering and bone in the ovariectomized rat

1996 • 151 citations

Nuclear hormone receptors: ligand-activated regulators of transcription and diverse cell responses

1996 • 143 citations

Antiestrogen basicity-activity relationships: a comparison of the estrogen receptor binding and antiuterotrophic potencies of several analogs of (Z)-1,2-diphenyl-1-[4-[2-(dimethylamino)ethoxy]phenyl]-1-butene (Tamoxifen, Nolvadex) having altered basicity

1982 • 123 citations

Longitudinal and cross-sectional analysis of raloxifene effects on tibiae from ovariectomized aged rats.

1995 • 118 citations

The Intracellular Receptor and Signal Transducers and Activators of Transcription Factor Superfamilies: Novel Targets for Small-Molecule Drug Discovery

1995 • 77 citations

Cellular Mechanisms Which Distinguish between Hormone‐ and Antihormone‐Activated Estrogen Receptor

1995 • 57 citations

Identification of an Estrogen Response Element Activated by Metabolites of 17 beta-Estradiol and Raloxifene

1997 • 56 citations

Regioselectivity in the Alkaline Thiolate Deprotection of Aryl Methyl Ethers

1995 • 54 citations

Potential antifertility agents. 1. Substituted diaryl derivatives of benzo[b]thiophenes, benzo[b]furans, 1H-2-benzothiapyrans, and 2H-1-benzothiapyrans

1971 • 35 citations

The Mechanism of Action of Steroid Hormones: A New Twist to an Old Tale

1993 • 26 citations

Chapter 19. Estrogen Receptor Modulators: Effects in Non-Traditional Target Tissues

1996 • 23 citations

Site-directed estrogen receptor antibodies stabilize 4-hydroxytamoxifen ligand, but not estradiol, and indicate ligand-specific differences in the recognition of estrogen response element DNA in vitro

1996 • 20 citations

Thianaphthen-2-one chemistry. I. Synthesis of 6H-benzothieno[3,2-c][1]benzopyran-6-ones (11-thiacoumestans)

1975 • 20 citations

Benzopyran selective estrogen receptor modulators (SERMs): Pharmacological effects and structural correlation with raloxifene

1996 • 16 citations

Relationship between estrogen structure and conformational changes in estrogen receptor/DNA complexes

1995 • 15 citations

Non-isomerisable antiestrogens related to tamoxifen

1988 • 11 citations

Conversion of the phytoestrogen coumestrol into a selective estrogen receptor modulator (SERM) by attachment of an amine-containing sidechain

1996 • 9 citations