Estrogen, selective estrogen receptor modulators and now mechanism-specific ligands of the estrogen or androgen receptor? 2003

Sundeep Khosla
Endocrine Research Unit, Division of Endocrinology, Metabolism, and Nutrition, Mayo Clinic and Foundation, 200 First Street SW, 5-194 Joseph, Rochester, MN 55905, USA. khosla.sundeep@mayo.edu

Estrogen, the traditional treatment of both short- and long-term consequences of the menopause, has fallen into disfavor. Thus, selective estrogen receptor modulators (SERMs) have been used as an alternative approach to activate estrogen signaling pathways in a tissue-specific manner. In addition, recent findings indicate that some compounds might activate specific estrogen signaling pathways that are beneficial without affecting other pathways that might lead to the harmful side-effects associated with estrogen. These so-called mechanism-specific ligands of estrogen or androgen receptors hold considerable promise as novel approaches to treat (or at least ameliorate) the consequences of estrogen deficiency.

UI MeSH Term Description Entries
D008024 Ligands A molecule that binds to another molecule, used especially to refer to a small molecule that binds specifically to a larger molecule, e.g., an antigen binding to an antibody, a hormone or neurotransmitter binding to a receptor, or a substrate or allosteric effector binding to an enzyme. Ligands are also molecules that donate or accept a pair of electrons to form a coordinate covalent bond with the central metal atom of a coordination complex. (From Dorland, 27th ed) Ligand
D011944 Receptors, Androgen Proteins, generally found in the CYTOPLASM, that specifically bind ANDROGENS and mediate their cellular actions. The complex of the androgen and receptor migrates to the CELL NUCLEUS where it induces transcription of specific segments of DNA. Androgen Receptors,5 alpha-Dihydrotestosterone Receptor,Androgen Receptor,Dihydrotestosterone Receptors,Receptor, Testosterone,Receptors, Androgens,Receptors, Dihydrotestosterone,Receptors, Stanolone,Stanolone Receptor,Testosterone Receptor,5 alpha Dihydrotestosterone Receptor,Androgens Receptors,Receptor, 5 alpha-Dihydrotestosterone,Receptor, Androgen,Receptor, Stanolone,Stanolone Receptors,alpha-Dihydrotestosterone Receptor, 5
D011960 Receptors, Estrogen Cytoplasmic proteins that bind estrogens and migrate to the nucleus where they regulate DNA transcription. Evaluation of the state of estrogen receptors in breast cancer patients has become clinically important. Estrogen Receptor,Estrogen Receptors,Estrogen Nuclear Receptor,Estrogen Receptor Type I,Estrogen Receptor Type II,Estrogen Receptors Type I,Estrogen Receptors Type II,Receptor, Estrogen Nuclear,Receptors, Estrogen, Type I,Receptors, Estrogen, Type II,Nuclear Receptor, Estrogen,Receptor, Estrogen
D004967 Estrogens Compounds that interact with ESTROGEN RECEPTORS in target tissues to bring about the effects similar to those of ESTRADIOL. Estrogens stimulate the female reproductive organs, and the development of secondary female SEX CHARACTERISTICS. Estrogenic chemicals include natural, synthetic, steroidal, or non-steroidal compounds. Estrogen,Estrogen Effect,Estrogen Effects,Estrogen Receptor Agonists,Estrogenic Agents,Estrogenic Compounds,Estrogenic Effect,Estrogenic Effects,Agents, Estrogenic,Agonists, Estrogen Receptor,Compounds, Estrogenic,Effects, Estrogen,Effects, Estrogenic,Receptor Agonists, Estrogen
D005260 Female Females
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D015914 Estrogen Replacement Therapy The use of hormonal agents with estrogen-like activity in postmenopausal or other estrogen-deficient women to alleviate effects of hormone deficiency, such as vasomotor symptoms, DYSPAREUNIA, and progressive development of OSTEOPOROSIS. This may also include the use of progestational agents in combination therapy. Hormone Replacement Therapy, Post-Menopausal,Postmenopausal Hormone Replacement Therapy,Replacement Therapy, Estrogen,Estrogen Progestin Combination Therapy,Estrogen Progestin Replacement Therapy,Estrogen Replacement,Replacement, Estrogen,Therapy, Estrogen Replacement,Estrogen Replacement Therapies,Estrogen Replacements,Hormone Replacement Therapy, Post Menopausal,Replacement Therapies, Estrogen,Replacements, Estrogen,Therapies, Estrogen Replacement
D016032 Randomized Controlled Trials as Topic Works about clinical trials that involve at least one test treatment and one control treatment, concurrent enrollment and follow-up of the test- and control-treated groups, and in which the treatments to be administered are selected by a random process, such as the use of a random-numbers table. Clinical Trials, Randomized,Controlled Clinical Trials, Randomized,Trials, Randomized Clinical
D017698 Postmenopause The physiological period following the MENOPAUSE, the permanent cessation of the menstrual life. Post-Menopause,Post-menopausal Period,Postmenopausal Period,Period, Post-menopausal,Period, Postmenopausal,Post Menopause,Post menopausal Period,Post-Menopauses
D020845 Selective Estrogen Receptor Modulators A structurally diverse group of compounds distinguished from ESTROGENS by their ability to bind and activate ESTROGEN RECEPTORS but act as either an agonist or antagonist depending on the tissue type and hormonal milieu. They are classified as either first generation because they demonstrate estrogen agonist properties in the ENDOMETRIUM or second generation based on their patterns of tissue specificity. (Horm Res 1997;48:155-63) Estrogen Receptor Modulators, Selective,SERMs,Estrogen Receptor Modulator, Selective,SERM,Selective Estrogen Receptor Modulator

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