
Selective Estrogen Receptor Modulators
A New Brand of Multitarget Drugs
By: Antonio Cano (Editor), Joacquim Calaf i Alsina (Editor), Jose Luis Duenas-Diez (Editor)
Hardcover | 13 June 2006
At a Glance
376 Pages
24.13 x 15.88 x 1.91
Hardcover
$169.00
or 4 interest-free payments of $42.25 with
 orÂShips in 5 to 7 business days
Industry Reviews
From the reviews of the first edition:
"Sanchez and colleagues have assembled a timely addition to the clinician's library. Their book is an up-to-date synthesis of the basic mechanisms of action of estrogen and SERMs with a comprehensive analysis of receptor-mediated and non-receptor mediated events in target tissue. The sections on new SERMs and the clinical endocrinology of SERMs are very useful and will remain so for some time. The choice of basic and clinical topics makes for interesting reading. ... Overall, the book is well written and easy to read." (V. Craig Jordan, The New England Journal of Medicine, January, 2007)
| Basic Area | |
| Molecular Mechanisms of Estrogen Action in Target Tissues | p. 3 |
| Introduction | p. 3 |
| General Aspects | p. 4 |
| The Discovery of Hormone Receptors for Steroid Hormones | p. 4 |
| Nuclear Hormone Receptors? | p. 5 |
| Structure of Estrogen Receptors | p. 7 |
| Primary Structure of Estrogen Receptors | p. 7 |
| Activity Domains in the Molecules of Estrogen Receptors | p. 8 |
| Genetic Encoding of Estrogen Receptors | p. 8 |
| Native Receptor | p. 10 |
| Estrogen Transforms the Native Receptor | p. 11 |
| Domain of Nuclear Location | p. 11 |
| Hormone-Receptor Interaction | p. 12 |
| Ligand Binding Domain | p. 12 |
| Structure of Receptor and Hormonal Antagonism | p. 14 |
| Receptor Folding in Separate Domains | p. 16 |
| Dimerization Domains | p. 17 |
| Receptor-Genome Interaction | p. 18 |
| Specific DNA Sequences for the Hormone Response | p. 18 |
| DNA-Binding Domain | p. 19 |
| Recognition of Hormone Response Element | p. 21 |
| Role of Receptor-Hormone Response Element Complex | p. 22 |
| Hormonal Regulation of Gene Transcription | p. 23 |
| Domains of Transcription Activation (Transactivators) | p. 24 |
| Intermediary Transcription Cofactors | p. 25 |
| Interaction of Receptor with Transcription Cofactors | p. 27 |
| Coactivators in Cellular and Gene Promoter Context | p. 27 |
| Concept of SERM from Point of View of Coactivator | p. 29 |
| Structure of Chromatin and Hormone Response | p. 29 |
| Specificity of Gene Transcription Induced by Hormones | p. 31 |
| Multiple Regulation of Gene Expression | p. 31 |
| Nuclear Hormone Receptors and Endocrine Disruptors | p. 32 |
| Regulation of Intensity of Hormone Response | p. 33 |
| Membrane Receptors for Steroid Hormones | p. 33 |
| Regulation of Concentration of Receptors per Cell | p. 34 |
| Receptor Destiny After Activation | p. 35 |
| Cross-Talk Signaling | p. 35 |
| Silencing of Genes for Nuclear Hormone Receptors | p. 37 |
| Summary | p. 39 |
| References | p. 41 |
| Clinical Pharmacology of Selective Estrogen Receptor Modulators (SERMs) | p. 49 |
| Introduction | p. 49 |
| Classification | p. 50 |
| Pharmacological Characteristics of SERMs | p. 52 |
| Triphenylethylenes | p. 52 |
| Benzothiophenes | p. 55 |
| Naphthalenes | p. 57 |
| Indoles | p. 58 |
| Benzopyrans | p. 60 |
| Conclusions | p. 62 |
| References | p. 65 |
| Action of Selective Estrogen Receptor Modulators (SERMs) Through the Classical Mechanism of Estrogen Action | p. 71 |
| Introduction | p. 71 |
| Estrogen Receptor Subtypes | p. 72 |
| Conformation of Ligand-ER Complex | p. 73 |
| Coregulator Protein Cell Content and Coactivators/Corepressors Ratio | p. 73 |
| Transrepression: Regulation of Gene Expression by an ERE-Independent Mechanism | p. 75 |
| References | p. 76 |
| Cellular and Molecular Basis for Acute Nongenomically Mediated Actions of SERMs | p. 79 |
| Introduction | p. 79 |
| Cellular and Molecular Targets for Rapid Actions | p. 79 |
| Interaction with Ion Channels | p. 79 |
| Multidrug Resistance and P-glycoprotein | p. 86 |
| Signalling Transducers | p. 87 |
| Lipids, Membrane Lipids, and Fluidity | p. 92 |
| Specific Antiestrogen-Binding Sites (AEBS) | p. 94 |
| Final Considerations | p. 95 |
| References | p. 96 |
| The Hypothalamus-Pituitary-Ovarian Axis as a Model System for the Study of... SERM Effects: An Overview of Experimental and Clinical Studies | p. 103 |
| Introduction | p. 103 |
| Hypothalamus-Pituitary-Ovarian Axis of Mammals | p. 104 |
| General Aspects | p. 104 |
| Functional Organization | p. 105 |
| Estrogen Feedback Regulation of Hypothalamus-Pituitary Axis | p. 106 |
| Overview of Hypothalamic-Pituitary Function at Time of Gonadotropin Surge | p. 112 |
| Effects of SERMs on Hypothalamus-Pituitary-Ovarian Axis | p. 114 |
| Experimental Studies in the Rat | p. 115 |
| Lessons in SERM Behavior from Effects of Tamoxifen on Rat Pituitary Function | p. 119 |
| Clinical Studies | p. 122 |
| Summary and Conclusions | p. 126 |
| References | p. 127 |
| Pure Antiestrogens | p. 141 |
| Introduction | p. 141 |
| Type I | p. 141 |
| Type II | p. 141 |
| Chemical Structure and Classification | p. 142 |
| Mechanism of Action | p. 143 |
| Effects of Pure Antiestrogens | p. 146 |
| In Vitro Studies | p. 146 |
| Experiments in Animals | p. 147 |
| Clinical Studies | p. 150 |
| Clinical Utility | p. 152 |
| References | p. 153 |
| Clinical Area | |
| Physiological Regulation of Bone Metabolism and Estrogen Agonism | p. 161 |
| Normal Bone Remodeling | p. 162 |
| Executive Cells: Osteoblasts and Osteoclasts | p. 163 |
| Role of Proinflammatory Cytokines in Bone Resorption | p. 166 |
| The RANKL/RANK/OPG System | p. 167 |
| Bone Remodeling After Estrogen Deficiency | p. 171 |
| Effects of Estrogen and Agonist of Estrogen Receptor on Bone Cells | p. 174 |
| Conclusions | p. 177 |
| References | p. 177 |
| The Role of SERMs in the Treatment of Osteoporosis | p. 187 |
| Introduction | p. 187 |
| Experimental Results | p. 188 |
| Tamoxifen | p. 188 |
| Raloxifene | p. 188 |
| Other SERMs | p. 189 |
| Clinical Effects of SERMs | p. 190 |
| Tamoxifen | p. 190 |
| Raloxifene | p. 192 |
| Bone Quality and Its Relevance | p. 195 |
| Future SERMs | p. 199 |
| References | p. 199 |
| Cardiovascular Disease and SERMs | p. 207 |
| The Focal Phenotype of CVD | p. 208 |
| The Crucial Role of the Endothelium | p. 210 |
| Estrogen Agonism and CVD | p. 212 |
| Lipids | p. 212 |
| Vascular Wall | p. 213 |
| SERMs as an Alternative to Estrogens in CVD | p. 214 |
| Actions of SERMs | p. 216 |
| Arterial Disease | p. 216 |
| VTED | p. 226 |
| Conclusion and Outlook for the Future | p. 227 |
| References | p. 228 |
| SERMs and the Breast | p. 239 |
| Introduction | p. 239 |
| Biology of Breast Development and its Endocrine Regulation | p. 240 |
| Framework of Breast Cancer Research | p. 241 |
| Relationship Between Estrogens and Breast Cancer | p. 243 |
| Endogenous Estrogens | p. 243 |
| Exogenous Estrogens | p. 244 |
| Pharmacological Blockade of Estrogen Receptors: The Concept of Chemoprophylaxis | p. 247 |
| Tamoxifen as Adjuvant Therapy in Early ER(+) Breast Cancer | p. 248 |
| Tamoxifen in Primary Prevention of ER(+) Breast Cancer | p. 250 |
| Drawbacks of Tamoxifen as a Preventive Agent | p. 252 |
| Raloxifene and Breast Cancer | p. 255 |
| Clinical Studies | p. 255 |
| Estrogen Receptor Status | p. 258 |
| Estrogen Circulating Levels and Raloxifene Protection | p. 258 |
| Bone Density and Effect of Raloxifene on the Breast | p. 260 |
| Other Conditions Related to Raloxifene Protection | p. 262 |
| Raloxifen as a Breast Cancer Preventive Agent | p. 264 |
| New Perspectives | p. 265 |
| References | p. 266 |
| Endometrial Effects of SERMs | p. 271 |
| Introduction | p. 271 |
| Mechanism of Action in the Endometrium | p. 271 |
| Tamoxifen | p. 272 |
| Raloxifene | p. 274 |
| Tamoxifen and Endometrium: Clinical Consideration | p. 275 |
| Ultrasonographic Findings | p. 275 |
| Hystological Findings | p. 275 |
| Tamoxifen and Risk of Endometrial Cancer | p. 277 |
| Raloxifene | p. 279 |
| Data Obtained from Biopsy | p. 279 |
| Ultrasonographic Data and Symptomatology | p. 280 |
| Others SERMs | p. 283 |
| Arzoxifene | p. 283 |
| Bazedoxifene Acetate | p. 283 |
| Lasofoxifene | p. 284 |
| Ospemifene | p. 284 |
| Conclusions | p. 285 |
| References | p. 285 |
| Benign Gynecological Diseases and SERMs | p. 291 |
| Introduction | p. 291 |
| Uterine Leiomyomas | p. 291 |
| Treatments of Uterine Leiomyomas | p. 292 |
| SERMs and Uterine Leiomyomas | p. 294 |
| Endometriosis | p. 302 |
| Treatments of Endometriosis | p. 303 |
| SERMs and Endometriosis | p. 304 |
| Conclusions | p. 305 |
| References | p. 306 |
| Other Clinical Effects of SERMs | p. 313 |
| Urogenital Tract | p. 314 |
| Vaginal Trophism and Dyspareunia | p. 314 |
| Pelvic Floor Function and Urinary Disorders | p. 315 |
| Central nervous system | p. 318 |
| Hot Flashes and Beta Endorphins | p. 320 |
| Mood, Sleep, Waking Episodes | p. 321 |
| Cognitive Function, Alzheimer's Disease (AD) | p. 321 |
| Libido, Sexual Function | p. 323 |
| Gallbladder and Hepatobiliar System | p. 324 |
| Desmoids and Mesenteric Fibromatosis | p. 325 |
| Endocrine Functions | p. 325 |
| Insulin Sensitivity and Diabetes | p. 325 |
| Thyroid Function | p. 325 |
| Eye, Cataracts | p. 326 |
| Other Effects | p. 328 |
| Arthritis | p. 328 |
| Hemorheological Effects | p. 328 |
| Quality of Life (QoL) | p. 328 |
| References | p. 329 |
| The Role of SERMs in the Management of Postmenopausal Women | p. 333 |
| Introduction | p. 333 |
| Identifying Troubles and Threats | p. 334 |
| Cardiovascular Risk | p. 334 |
| Menopausal Syndrome | p. 335 |
| Osteoporosis | p. 336 |
| Breast Cancer | p. 337 |
| Intervention Tools | p. 338 |
| Lifestyle Optimization | p. 338 |
| Hormone Therapy | p. 338 |
| Cardioprotective Treatments | p. 339 |
| Bone Resorption Inhibitors | p. 339 |
| Breast Cancer Risk | p. 340 |
| Adressing Health Expectancy Improvement | p. 340 |
| Poly Approach and Multitasking | p. 340 |
| Pharmacological Poly Approach | p. 341 |
| Multitasking Drugs | p. 342 |
| Dynamic Decision-Making Diagram | p. 344 |
| References | p. 346 |
| Subject Index | p. 351 |
| Table of Contents provided by Ingram. All Rights Reserved. |
ISBN: 9783540242277
ISBN-10: 3540242279
Published: 13th June 2006
Format: Hardcover
Language: English
Number of Pages: 376
Audience: Professional and Scholarly
Publisher: Springer Nature B.V.
Country of Publication: DE
Dimensions (cm): 24.13 x 15.88 x 1.91
Weight (kg): 0.75
Shipping
| Standard Shipping | Express Shipping | |
|---|---|---|
| Metro postcodes: | $9.99 | $14.95 |
| Regional postcodes: | $9.99 | $14.95 |
| Rural postcodes: | $9.99 | $14.95 |
Orders over $79.00 qualify for free shipping.
How to return your order
At Booktopia, we offer hassle-free returns in accordance with our returns policy. If you wish to return an item, please get in touch with Booktopia Customer Care.
Additional postage charges may be applicable.
Defective items
If there is a problem with any of the items received for your order then the Booktopia Customer Care team is ready to assist you.
For more info please visit our Help Centre.
You Can Find This Book In

The Baby Loss Guide
Practical and compassionate support with a day-by-day resource to navigate the path of grief
Paperback
RRP $24.99
$21.75
OFF
This product is categorised by
- Non-FictionFamily & HealthPopular Medicine & HealthWomen's Health
- Non-FictionMedicineClinical & Internal MedicineEndocrinology
- Non-FictionMedicineOther Branches of MedicinePharmacology
- Non-FictionMedicineClinical & Internal MedicineGynaecology & Obstetrics
- Non-FictionMedicineClinical & Internal MedicineRheumatology
- Non-FictionMedicinePre-Clinical Medicine & Basic SciencesPhysiologyMetabolism























