Clues about estrogen and antiestrogen action from X-ray crystallography

GL Greene, VC Jordan - Estrogen Action, Selective Estrogen …, 2013 - World Scientific
During the 1980s the structure–function relationship of nonsteroidal estrogens and
antiestrogens using an a prolactin gene target in primary cultures of rat pituitary cells created …

Structure-activity relationships

E Von Angerer - Estrogens and Antiestrogens I: Physiology and …, 1999 - Springer
Estrogens and anti estrogens are understood to exert their hormonal action after binding to
the estrogen receptor (ER), a member of the nuclear receptor superfamily. Until recently, the …

Understanding the Molecular Mechanism of Action of Estrogen Receptor Modulators

MJ Meegan, DG Lloyd - Frontiers in Medicinal Chemistry-Online, 2005 - ingentaconnect.com
Estrogen receptor modulators are recognised as playing a central role in the regulation of
many endocrine functions. In recent years, the discovery of many new members of this class …

Molecular mechanisms of estrogen action: selective ligands and receptor pharmacology

BS Katzenellenbogen, I Choi… - The Journal of steroid …, 2000 - Elsevier
Estrogens exert profound effects on the physiology of diverse target cells and these effects
appear to be mediated by two estrogen receptor (ER) subtypes, ERα and ERβ. We have …

Mechanisms of estrogen action

S Nilsson, S Makela, E Treuter… - Physiological …, 2001 - journals.physiology.org
Our appreciation of the physiological functions of estrogens and the mechanisms through
which estrogens bring about these functions has changed during the past decade. Just as …

Probing conformational changes in the estrogen receptor: evidence for a partially unfolded intermediate facilitating ligand binding and release

AC Gee, JA Katzenellenbogen - Molecular Endocrinology, 2001 - academic.oup.com
Because the ligand bound to the ligand-binding domain (LBD) of nuclear hormone receptors
is completely enveloped by protein, it is thought that the process of ligand binding or …

A structural biologist's view of the oestrogen receptor

ACW Pike, AM Brzozowski, RE Hubbard - The Journal of steroid …, 2000 - Elsevier
Here we review the results that have emerged from our structural studies on the oestrogen
receptor ligand-binding domain (ER-LBD). The effects of agonists and antagonists on the …

Crystallographic comparison of the estrogen and progesterone receptor's ligand binding domains

DM Tanenbaum, Y Wang… - Proceedings of the …, 1998 - National Acad Sciences
The 2.8-Å crystal structure of the complex formed by estradiol and the human estrogen
receptor-α ligand binding domain (hERαLBD) is described and compared with the recently …

Different residues of the human estrogen receptor are involved in the recognition of structurally diverse estrogens and antiestrogens

K Ekena, KE Weis, JA Katzenellenbogen… - Journal of Biological …, 1997 - ASBMB
We have previously examined, by alanine scanning mutagenesis, amino acids 515-535 of
the estrogen receptor (ER) ligand binding domain to determine which of these residues are …

Estrogen receptor interaction with co-activators and co-repressors☆

CM Klinge - Steroids, 2000 - Elsevier
Estrogens exert a wide variety of effects on growth, development, and differentiation,
including important regulatory functions within the reproductive systems of both females and …