Selective estrogen receptor modulators: a new brand of multitarget drugs
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| Format: | Book |
|---|---|
| Language: | English |
| Published: |
Berlin [u.a.]
Springer
2006
|
| Subjects: | |
| Online Access: | Inhaltsverzeichnis |
| Physical Description: | XVII, 357 S. Ill., graph. Darst. |
| ISBN: | 3540242279 9783540242277 |
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| 020 | |a 9783540242277 |c Gb. : ca. EUR 106.95 (freier Pr.), ca. sfr 169.00 (freier Pr.) |9 978-3-540-24227-7 | ||
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| 245 | 1 | 0 | |a Selective estrogen receptor modulators |b a new brand of multitarget drugs |c Antonio Cano Sanchez ... (ed.) |
| 264 | 1 | |a Berlin [u.a.] |b Springer |c 2006 | |
| 300 | |a XVII, 357 S. |b Ill., graph. Darst. | ||
| 336 | |b txt |2 rdacontent | ||
| 337 | |b n |2 rdamedia | ||
| 338 | |b nc |2 rdacarrier | ||
| 650 | 4 | |a Estrogen Antagonists | |
| 650 | 4 | |a Estrogen |x Antagonists | |
| 650 | 4 | |a Menopause |x Hormone therapy | |
| 650 | 4 | |a Receptors, Estrogen | |
| 650 | 4 | |a Selective Estrogen Receptor Modulators |x pharmacology | |
| 650 | 4 | |a Selective Estrogen Receptor Modulators |x therapeutic use | |
| 650 | 4 | |a Selective estrogen receptor modulators | |
| 650 | 0 | 7 | |a Selektiver Östrogen-Rezeptor-Modulator |0 (DE-588)4689537-1 |2 gnd |9 rswk-swf |
| 655 | 7 | |0 (DE-588)4143413-4 |a Aufsatzsammlung |2 gnd-content | |
| 689 | 0 | 0 | |a Selektiver Östrogen-Rezeptor-Modulator |0 (DE-588)4689537-1 |D s |
| 689 | 0 | |5 DE-604 | |
| 700 | 1 | |a Cano Sanchez, Antonio |e Sonstige |4 oth | |
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Record in the Search Index
| _version_ | 1804135466749919232 |
|---|---|
| adam_text | ANTONIO
CANO
SANCHEZ
JOAQUIM
CALAF
I
ALSINA
JOSE-LUIS
DUERIAS-DFEZ
(EDITORS)
YY
E
ECTLVE
ECE
TOR
STRO
EN
O
U
ATORS
A
NEW
BRAND
OF
MULTITARGET
DRUGS
WITH
74
FIGURES,
INCLUDING
40
IN
COLOR
::::
SPRINGER
CONTENTS
PART
I
BASIC
AREA
1
MOLECULAR
MECHANISMS
OF
ESTROGEN
ACTION
IN
TARGET
TISSUES
B.
NICOLAS
DIAZ
CHICO,
DOMINGO
NAVARRO
BOSCH,
JUAN
C.
DIAZ
CHICO,
EDUARDO
ESCRICH
ESCRICHE
.
3
1.1
INTRODUCTION......
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3
1.2
GENERAL
ASPECTS
4
1.2.1
THE
DISCOVERY
OF
HORMONE
RECEPTORS
FOR
STEROID
HORMONES
4
1.2.2
NUCLEAR
HORMONE
RECEPTORS?
5
1.3
STRUCTURE
OF
ESTROGEN
RECEPTORS
7
1.3.1
PRIMARY
STRUCTURE
OF
ESTROGEN
RECEPTORS
..
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7
1.3.2
ACTIVITY
DOMAINS
IN
THE
MOLECULES
OF
ESTROGEN
RECEPTORS.
.
.
8
1.3.3
GENETIC
ENCODING
OF
ESTROGEN
RECEPTORS.
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8
1.3.4
NATIVE
RECEPTOR
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10
1.3.5
ESTROGEN
TRANSFORMS
THE
NATIVE
RECEPTOR.
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11
1.3.6
DOMAIN
OF
NUCLEAR
LOCATION
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11
1.4
HORMONE-RECEPTOR
INTERACTION.
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12
1.4.1
LIGAND
BINDING
DOMAIN
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12
1.4.2
STRUCTURE
OF
RECEPTOR
AND
HORMONAL
ANTAGONISM
14
1.4.3
RECEPTOR
FOLDING
IN
SEPARATE
DOMAINS
...
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16
1.4.4
DIMERIZATION
DOMAINS
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17
1.5
RECEPTOR-GENOME
INTERACTION.
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18
1.5.1
SPECIFIC
DNA
SEQUENCES
FOR
THE
HORMONE
RESPONSE.
.
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..
18
1.5.2
DNA
BINDING
DOMAIN
19
1.5.3
RECOGNITION
OF
HORMONE
RESPONSE
ELEMENT
21
1.5.4
ROLE
OF
RECEPTOR-HORMONE
RESPONSE
ELEMENT
COMPLEX..
..
22
1.6
HORMONAL
REGULATION
OF
GENE
TRANSCRIPTION
23
1.6.1
DOMAINS
OF
TRANSCRIPTION
ACTIVATION
(TRANSACTIVATORS)
.
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..
24
1.6.2
INTERMEDIARY
TRANSCRIPTION
COFACTORS
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25
1.6.3
INTERACTION
OF
RECEPTOR
WITH
TRANSCRIPTION
COFACTORS.
.
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..
27
1.6.4
COACTIVATORS
IN
CELLULAR
AND
GENE
PROMOTER
CONTEXT.
.
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..
27
1.6.5
CONCEPT
OF
SERM
FROM
POINT
OF
VIEW
OF
COACTIVATOR
29
VIII
CONTENTS
1.6.6
STRUCTURE
OF
CHROMATIN
AND
HORMONE
RESPONSE.
.
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..
29
1.6.7
SPECIFICITY
OF
GENE
TRANSCRIPTION
INDUCED
BY
HORMONES.
.
..
31
1.6.8
MULTIPLE
REGULATION
OF
GENE
EXPRESSION
.
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31
1.6.9
NUCLEAR
HORMONE
RECEPTORS
AND
ENDOCRINE
DISRUPTORS
32
1.7
REGULATION
OF
INTENSITY
OF
HORMONE
RESPONSE
33
1.7.1
MEMBRANE
RECEPTORS
FOR
STEROID
HORMONES.
.
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..
33
1.7.2
REGULATION
OF
CONCENTRATION
OF
RECEPTORS
PER
CELL
.
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..
34
1.
7.3
RECEPTOR
DESTINY
AFTER
ACTIVATION
35
1.8
CROSS-TALK
SIGNALING
35
1.9
SILENCING
OF
GENES
FOR
NUCLEAR
HORMONE
RECEPTORS.
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37
1.10
SUMMARY...................................................
39
REFERENCES
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41
2
CLINICAL
PHARMACOLOGY
OF
SELECTIVEESTROGEN
RECEPTORMODULATORS
(SERMS)
FERNANDO
MARIN,
M
A
CARMEN
BARBANCHO
49
2.1
INTRODUCTION.
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49
2.2
CLASSIFICATION................................................
50
2.3
PHARMACOLOGICAL
CHARACTERISTICS
OF
SERMS
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52
2.3.1
TRIPHENYLETHYLENES.
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52
2.3.2
BENZOTHIOPHENES..
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55
2.3.3
NAPHTHALENES.
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57
2.3.4
INDOLES
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58
2.3.5
BENZOPYRANS
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60
2.4
CONCLUSIONS.................................................
62
REFERENCES
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65
3
ACTION
OF
SELECTIVE
ESTROGEN
RECEPTOR
MODULATORS
(SERMS)
THROUGH
THE
CLASSICAL
MECHANISM
OF
ESTROGEN
ACTION
FERNANDO
MARIN,
M
CARMEN
BARBANCHO
71
3.1
INTRODUCTION.
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71
3.2
ESTROGEN
RECEPTOR
SUBTYPES.
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72
3.3
CONFORMATION
OF
LIGAND-ER
COMPLEX.
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73
3.4
COREGULATOR
PROTEIN
CELL
CONTENT
AND
COACTIVATORS/COREPRESSORS
RATIO
.
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73
3.5
TRANSREPRESSION:
REGULATION
OF
GENE
EXPRESSION
BY
AN
ERE-INDEPENDENT
MECHANISM.
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75
REFERENCES.
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76
CONTENTS
IX
4
CELLULAR
AND
MOLECULAR
BASIS
FOR
ACUTE
NONGENOMICALLY
MEDIATED
ACTIONS
OF
SERMS
MARIO
DIAZ,
JORGE
MARRERO-ALONSO,
BENITO
GARCIA
MARRERO,
RAQUEL
MARIN,
TOMAS
GOMEZ,
RAFAEL
ALONSO.
..
....
.....
.....
....
79
4.1
INTRODUCTION....
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79
4.2
CELLULAR
AND
MOLECULAR
TARGETS
FOR
RAPID
ACTIONS
79
4.2.1
INTERACTION
WITH
ION
CHANNELS.
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79
4.2.2
MULTIDRUG
RESISTANCE
AND
P-GLYCOPROTEIN
.
0
0
YYYY
0
YY
YY
YY
YY
YY
YY
YY
YY
YY
YYYY
86
4.2.3
SIGNALLING
TRANSDUCERS
.
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87
4.2.4
LIPIDS,
MEMBRANE
LIPIDS,
AND
FLUIDITY
92
4.2.5
SPECIFIC
ANTIESTROGEN-BINDING
SITES
(AEBS)
.
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..
94
4.3
FINAL
CONSIDERATIONS
0
0
YYYY
0
0
YYYYYYYY
0
YYYY
0
95
REFERENCES
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96
5
THE
HYPOTHALAMUS-PITUITARY-OVARIAN
AXIS
AS
A
MODEL
SYSTEM
FOR
THE
STUDY
OF
...
SERM
EFFECTS:
AN
OVERVIEW
OF
EXPERIMENTAL
AND
CLINICAL
STUDIES
R.
ALONSO,
F.
MARIN,
M.
GONZALEZ,
P.
GUELMES,
C.
BELLIDO,
G.
HERNANDEZ,
R.
MARIN,
MO
DIAZ,
J.EO
SDNCHEZ-CRIADO
....
.....
.
..
103
5.1
INTRODUCTION
103
5.2
HYPOTHALAMUS-PITUITARY-OVARIAN
AXIS
OF
MAMMALS
.
.
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..
104
5.2.1
GENERAL
ASPECTS
0
YYYY
0
0
YY
YY
YY
YYYY
104
.
5.2.2
FUNCTIONAL
ORGANIZATION
0
0
0
YYYY
0
YYYYYYYYYY
0
105
5.2.3
ESTROGEN
FEEDBACK
REGULATION
OF
HYPOTHALAMUS
PITUITARY
AXIS
0
YYYY
0
0
0
106
5.2.4
OVERVIEW
OF
HYPOTHALAMIC
PITUITARY
FUNCTION
AT
TIME
OF
GONADOTROPIN
SURGE.
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..
112
5.3
EFFECTS
OF
SERMS
ON
HYPOTHALAMUS
PITUITARY-OVARIAN
AXIS
0
0
YYYY
0
O.
114
5.3.1
EXPERIMENTAL
STUDIES
IN
THE
RAT
115
5.3.2
LESSONS
IN
SERM
BEHAVIOR
FROM
EFFECTS
OF
TAMOXIFEN
ON
RAT
PITUITARY
FUNCTION.
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119
5.3.3
CLINICAL
STUDIES
0
YYYYYY
0
YYYY
0
YYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYY
122
5.4
SUMMARY
AND
CONCLUSIONS.
0
YY
0
0
YYYY
0
0
0
0
YYYY
0
YYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYY
126
REFERENCES
127
6
PURE
ANTIESTROGENS
CARLOS
HERMENEGILDO
0
0
YYYY
0
0
YYYY
0
0
0
0
YY
0
0
0
YYYY
0
0
YYYY
141
6.1
INTRODUCTION.........
.
.
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.
..
141
6.1.1
TYPE
I
141
6.1.2
TYPE
II
141
6.2
CHEMICAL
STRUCTURE
AND
CLASSIFICATION
.
.
.
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.
..
142
9
CARDIOVASCULAR
DISEASE
AND
SERMS
ANTONIO
CANO
207
PART
II
CLINICAL
AREA
CONTENTS
X
7
PHYSIOLOGICAL
REGULATION
OF
BONE
METABOLISM
AND
ESTROGEN
AGONISM
MIGUEL
ANGELGARCIA-PEREZ
161
7.1
NORMAL
BONE
REMODELING
162
7.2
EXECUTIVE
CELLS:
OSTEOBLASTS
AND
OSTEOCLASTS
163
7.3
ROLE
OF
PROINFLAMMATORY
CYTOKINES
IN
BONE
RESORPTION.
.
.
.
.
.
.
.
.
..
166
7.4
THE
RANKLIRANK/OPG
SYSTEM
167
7.5
BONE
REMODELING
AFTER
ESTROGEN
DEFICIENCY
171
7.6
EFFECTS
OF
ESTROGEN
AND
AGONIST
OF
ESTROGEN
RECEPTOR
ON
BONE
CELLS
174
7.7
CONCLUSIONS.................................................
177
REFERENCES
.
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..
177
6.3
MECHANISM
OF
ACTION.
.
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..
.
..
..
143
6.4
EFFECTS
OF
PURE
ANTIESTROGENS
.
.
.
.
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..
.
.
..
..
146
6.4.1
IN
VITRO
STUDIES
146
6.4.2
EXPERIMENTS
IN
ANIMALS.
.
.
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..
.
.
..
147
6.4.3
CLINICAL
STUDIES
150
6.5
CLINICAL
UTILITY
152
REFERENCES
153
8
THE
ROLE
OF
SERMS
IN
THE
TREATMENT
OF
OSTEOPOROSIS
ADOLFO
DIEZ-PEREZ,
JOSE
LUIS
DUEHAS-DIEZ
187
9.1
THE
FOCAL
PHENOTYPE
OF
CVD
.
.
.
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.
..
.
..
.
..
.
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.
..
208
9.1.1
THE
CRUCIAL
ROLE
OF
THE
ENDOTHELIUM
210
9.2
ESTROGEN
AGONISM
AND
CVD
212
8.1
INTRODUCTION
187
8.2
EXPERIMENTAL
RESULTS.
.
.
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..
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..
188
8.2.1
TAMOXIFEN
188
8.2.2
RALOXIFENE...
.
.
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..
188
8.3
OTHER
SERMS
.
.
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.
..
189
8.4
CLINICAL
EFFECTS
OF
SERMS
190
8.4.1
TAMOXIFEN.
.
.
.
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..
190
8.4.2
RALOXIFENE...
.
.
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.
..
192
8.5
BONE
QUALITY
AND
ITS
RELEVANCE
195
8.6
FUTURE
SERMS
....
.
.
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..
199
REFERENCES
.
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..
199
-
CONTENTS
XI
9.2.1
LIPIDS
212
9.2.2
VASCULAR
WALL
213
9.3
SERMS
AS
AN
ALTERNATIVE
TO
ESTROGENS
IN
CVD
214
9.4
ACTIONS
OF
SERMS
216
904.1
ARTERIAL
DISEASE
.
.
.
.
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.
216
9.4.2
VTED.
.
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.
226
9.5
CONCLUSION
AND
OUTLOOK
FOR
THE
FUTURE
227
REFERENCES
.
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.
228
10
SERMS
AND
THE
BREAST
[OAQUIM
CALAFIALSINA,
ANTONIO
CANO
SANCHEZ.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
..
239
10.1
INTRODUCTION
239
10.2
BIOLOGY
OF
BREAST
DEVELOPMENT
AND
ITS
ENDOCRINE
REGULATION
240
10.3
FRAMEWORK
OF
BREAST
CANCER
RESEARCH
241
LOA
RELATIONSHIP
BETWEEN
ESTROGENS
AND
BREAST
CANCER
243
1004.1
ENDOGENOUS
ESTROGENS
.
.
.
.
.
.
.
.
.
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.
.
.
.
.
243
1004.2
EXOGENOUS
ESTROGENS
244
10.5
PHARMACOLOGICAL
BLOCKADE
OF
ESTROGEN
RECEPTORS:
THE
CONCEPT
OF
CHEMOPROPHYLAXIS
247
10.5.1
TAMOXIFEN
AS
ADJUVANT
THERAPY
IN
EARLY
ER(+)
BREAST
CANCER.
.
.
.
.
.
.
.
.
.
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.
..
248
10.5.2
TAMOXIFEN
IN
PRIMARY
PREVENTION
OF
ER(
+)
BREAST
CANCER
250
10.5.3
DRAWBACKS
OF
TAMOXIFEN
AS
A
PREVENTIVE
AGENT
252
10.6
RALOXIFENE
AND
BREAST
CANCER
255
10.6.1
CLINICAL
STUDIES
255
10.6.2
ESTROGEN
RECEPTOR
STATUS
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
258
10.6.3
ESTROGEN
CIRCULATING
LEVELS
AND
RALOXIFENE
PROTECTION
258
10.604
BONE
DENSITY
AND
EFFECT
OF
RALOXIFENE
ON
THE
BREAST
260
10.6.5
OTHER
CONDITIONS
RELATED
TO
RALOXIFENE
PROTECTION
262
10.6.6
RALOXIFEN
AS
A
BREAST
CANCER
PREVENTIVE
AGENT
264
10.
7
NEW
PERSPECTIVES
265
REFERENCES
.
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..
266
11
ENDOMETRIAL
EFFECTS
OF
SERMS
SANTIAGO
PALACIOS
271
11.1
INTRODUCTION
271
11.2
MECHANISM
OF
ACTION
IN
THE
ENDOMETRIUM
271
11.2.1
TAMOXIFEN
272
11.2.2
RALOXIFENE
274
11.3
TAMOXIFEN
AND
ENDOMETRIUM:
CLINICAL
CONSIDERATION
275
11.3.1
ULTRASONOGRAPHIC
FINDINGS
275
-~-~--~~.
XII
CONTENTS
11.3.2
HYSTOLOGICAL
FINDINGS
275
11.3.3
TAMOXIFEN
AND
RISK
OF
ENDOMETRIAL
CANCER
277
11.4
RALOXIFENE
279
11.4.1
DATA
OBTAINED
FROM
BIOPSY
279
11.4.2
ULTRASONOGRAPHIC
DATA
AND
SYMPTOMATOLOGY
280
11.5
OTHERS
SERMS
.
.
.
.
.
.
.
.
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.
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.
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.
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.
.
.
.
..
283
11.5.1
ARZOXIFENE
283
11.5.2
BAZEDOXIFENE
ACETATE
283
11.5.3
LASOFOXIFENE
284
11.5.4
OSPEMIFENE
284
11.6
CONCLUSIONS
285
REFERENCES
.
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.
.
285
12
BENIGN
GYNECOLOGICAL
DISEASES
AND
SERMS
STEFANO
PALOMBA,
FULVIO
ZULLO
.
.
.
.
.
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.
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.
.
..
291
12.1
INTRODUCTION
291
12.2
UTERINE
LEIOMYOMAS
291
12.2.1
TREATMENTS
OF
UTERINE
LEIOMYOMAS
292
12.2.2
SERMS
AND
UTERINE
LEIOMYOMAS
294
12.3
ENDOMETRIOSIS
302
12.3.1
TREATMENTS
OF
ENDOMETRIOSIS.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
..
303
12.3.2
SERMS
AND
ENDOMETRIOSIS
304
12.4
CONCLUSIONS
305
REFERENCES
.
.
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.
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.
..
306
13
OTHER
CLINICAL
EFFECTS
OF
SERMS
P.
ACIEN,
F.
QUEREDA,
M.L.
ACIEN
.....
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
..
313
13.1
UROGENITAL
TRACT
314
13.1.1
VAGINAL
TROPHISM
AND
DYSPAREUNIA
314
13.1.2
PELVIC
FLOOR
FUNCTION
AND
URINARY
DISORDERS
315
13.2
CENTRAL
NERVOUS
SYSTEM
318
13.2.1
HOT
FLASHES
AND
BETA
ENDORPHINS
320
13.2.2
MOOD,
SLEEP,
WAKING
EPISODES
321
13.2.3
COGNITIVE
FUNCTION,
ALZHEIMER SDISEASE
(AD)
321
13.2.4
LIBIDO,
SEXUAL
FUNCTION
323
13.3
GALLBLADDER
AND
HEPATOBILIAR
SYSTEM
324
13.4
DESMOIDS
AND
MESENTERIC
FIBROMATOSIS
325
13.5
ENDOCRINE
FUNCTIONS
325
13.5.1
INSULIN
SENSITIVITY
AND
DIABETES
325
13.5.2
THYROID
FUNCTION
325
13.6
EYE,
CATARACTS
326
YY
CONTENTS
XIII
13.7
OTHER
EFFECTS
328
13.7.1
ARTHRITIS
328
13.7.2
HEMORHEOLOGICAL
EFFECTS
328
13.7.3
QUALITY
OFLIFE
(QOL)
328
REFERENCES
329
14
THE
ROLE
OF
SERMS
IN
THE
MANAGEMENT
OF
POSTMENOPAUSAL
WOMEN
]OAQUIM
CALAFIALSINA
.
.
.
.
.
.
.
.
.
.
.
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.
.
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.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
..
333
14.1
INTRODUCTION
333
14.2
IDENTIFYING
TROUBLES
AND
THREATS
334
14.2.1
CARDIOVASCULAR
RISK
334
14.2.2
MENOPAUSAL
SYNDROME
335
14.2.3
OSTEOPOROSIS
336
14.2.4
BREAST
CANCER
337
14.3
INTERVENTION
TOOLS
338
14.3.1
LIFESTYLE
OPTIMIZATION
338
14.3.2
HORMONE
THERAPY
338
14.3.3
CARDIOPROTECTIVE
TREATMENTS
339
14.3.4
BONE
RESORPTION
INHIBITORS
339
14.3.5
BREAST
CANCER
RISK
340
14.4
ADRESSING
HEALTH
EXPECTANCY
IMPROVEMENT
..
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
..
340
14.4.1
POLY
APPROACH
AND
MULTITASKING
340
14.4.2
PHARMACOLOGICAL
POLY
APPROACH
341
14.4.3
MULTITASKING
DRUGS
342
14.5
DYNAMIC
DECISION-MAKING
DIAGRAM
344
REFERENCES
.
.
.
.
.
.
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.
.
.
..
346
SUBJECT
INDEX
351
|
| adam_txt |
ANTONIO
CANO
SANCHEZ
JOAQUIM
CALAF
I
ALSINA
JOSE-LUIS
DUERIAS-DFEZ
(EDITORS)
YY
E
ECTLVE
ECE
TOR
STRO
EN
O
U
ATORS
A
NEW
BRAND
OF
MULTITARGET
DRUGS
WITH
74
FIGURES,
INCLUDING
40
IN
COLOR
::::
SPRINGER
CONTENTS
PART
I
BASIC
AREA
1
MOLECULAR
MECHANISMS
OF
ESTROGEN
ACTION
IN
TARGET
TISSUES
B.
NICOLAS
DIAZ
CHICO,
DOMINGO
NAVARRO
BOSCH,
JUAN
C.
DIAZ
CHICO,
EDUARDO
ESCRICH
ESCRICHE
.
3
1.1
INTRODUCTION.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
3
1.2
GENERAL
ASPECTS
4
1.2.1
THE
DISCOVERY
OF
HORMONE
RECEPTORS
FOR
STEROID
HORMONES
4
1.2.2
NUCLEAR
HORMONE
RECEPTORS?
5
1.3
STRUCTURE
OF
ESTROGEN
RECEPTORS
7
1.3.1
PRIMARY
STRUCTURE
OF
ESTROGEN
RECEPTORS
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
7
1.3.2
ACTIVITY
DOMAINS
IN
THE
MOLECULES
OF
ESTROGEN
RECEPTORS.
.
.
8
1.3.3
GENETIC
ENCODING
OF
ESTROGEN
RECEPTORS.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
8
1.3.4
NATIVE
RECEPTOR
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
10
1.3.5
ESTROGEN
TRANSFORMS
THE
NATIVE
RECEPTOR.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
11
1.3.6
DOMAIN
OF
NUCLEAR
LOCATION
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
11
1.4
HORMONE-RECEPTOR
INTERACTION.
.
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12
1.4.1
LIGAND
BINDING
DOMAIN
.
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12
1.4.2
STRUCTURE
OF
RECEPTOR
AND
HORMONAL
ANTAGONISM
14
1.4.3
RECEPTOR
FOLDING
IN
SEPARATE
DOMAINS
.
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16
1.4.4
DIMERIZATION
DOMAINS
.
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17
1.5
RECEPTOR-GENOME
INTERACTION.
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18
1.5.1
SPECIFIC
DNA
SEQUENCES
FOR
THE
HORMONE
RESPONSE.
.
.
.
.
.
.
18
1.5.2
DNA
BINDING
DOMAIN
19
1.5.3
RECOGNITION
OF
HORMONE
RESPONSE
ELEMENT
21
1.5.4
ROLE
OF
RECEPTOR-HORMONE
RESPONSE
ELEMENT
COMPLEX.
.
22
1.6
HORMONAL
REGULATION
OF
GENE
TRANSCRIPTION
23
1.6.1
DOMAINS
OF
TRANSCRIPTION
ACTIVATION
(TRANSACTIVATORS)
.
.
.
.
24
1.6.2
INTERMEDIARY
TRANSCRIPTION
COFACTORS
.
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25
1.6.3
INTERACTION
OF
RECEPTOR
WITH
TRANSCRIPTION
COFACTORS.
.
.
.
.
.
27
1.6.4
COACTIVATORS
IN
CELLULAR
AND
GENE
PROMOTER
CONTEXT.
.
.
.
.
.
27
1.6.5
CONCEPT
OF
SERM
FROM
POINT
OF
VIEW
OF
COACTIVATOR
29
VIII
CONTENTS
1.6.6
STRUCTURE
OF
CHROMATIN
AND
HORMONE
RESPONSE.
.
.
.
.
.
.
.
.
.
29
1.6.7
SPECIFICITY
OF
GENE
TRANSCRIPTION
INDUCED
BY
HORMONES.
.
.
31
1.6.8
MULTIPLE
REGULATION
OF
GENE
EXPRESSION
.
.
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.
31
1.6.9
NUCLEAR
HORMONE
RECEPTORS
AND
ENDOCRINE
DISRUPTORS
32
1.7
REGULATION
OF
INTENSITY
OF
HORMONE
RESPONSE
33
1.7.1
MEMBRANE
RECEPTORS
FOR
STEROID
HORMONES.
.
.
.
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.
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.
33
1.7.2
REGULATION
OF
CONCENTRATION
OF
RECEPTORS
PER
CELL
.
.
.
.
.
.
.
.
34
1.
7.3
RECEPTOR
DESTINY
AFTER
ACTIVATION
35
1.8
CROSS-TALK
SIGNALING
35
1.9
SILENCING
OF
GENES
FOR
NUCLEAR
HORMONE
RECEPTORS.
.
.
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.
37
1.10
SUMMARY.
39
REFERENCES
.
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41
2
CLINICAL
PHARMACOLOGY
OF
SELECTIVEESTROGEN
RECEPTORMODULATORS
(SERMS)
FERNANDO
MARIN,
M
A
CARMEN
BARBANCHO
49
2.1
INTRODUCTION.
.
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49
2.2
CLASSIFICATION.
50
2.3
PHARMACOLOGICAL
CHARACTERISTICS
OF
SERMS
.
.
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52
2.3.1
TRIPHENYLETHYLENES.
.
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52
2.3.2
BENZOTHIOPHENES.
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55
2.3.3
NAPHTHALENES.
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57
2.3.4
INDOLES
.
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58
2.3.5
BENZOPYRANS
.
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60
2.4
CONCLUSIONS.
62
REFERENCES
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65
3
ACTION
OF
SELECTIVE
ESTROGEN
RECEPTOR
MODULATORS
(SERMS)
THROUGH
THE
CLASSICAL
MECHANISM
OF
ESTROGEN
ACTION
FERNANDO
MARIN,
M"
CARMEN
BARBANCHO
71
3.1
INTRODUCTION.
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71
3.2
ESTROGEN
RECEPTOR
SUBTYPES.
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72
3.3
CONFORMATION
OF
LIGAND-ER
COMPLEX.
.
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.
73
3.4
COREGULATOR
PROTEIN
CELL
CONTENT
AND
COACTIVATORS/COREPRESSORS
RATIO
.
.
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.
73
3.5
TRANSREPRESSION:
REGULATION
OF
GENE
EXPRESSION
BY
AN
ERE-INDEPENDENT
MECHANISM.
.
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75
REFERENCES.
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76
CONTENTS
IX
4
CELLULAR
AND
MOLECULAR
BASIS
FOR
ACUTE
NONGENOMICALLY
MEDIATED
ACTIONS
OF
SERMS
MARIO
DIAZ,
JORGE
MARRERO-ALONSO,
BENITO
GARCIA
MARRERO,
RAQUEL
MARIN,
TOMAS
GOMEZ,
RAFAEL
ALONSO.
.
.
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.
79
4.1
INTRODUCTION.
.
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79
4.2
CELLULAR
AND
MOLECULAR
TARGETS
FOR
RAPID
ACTIONS
79
4.2.1
INTERACTION
WITH
ION
CHANNELS.
.
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.
79
4.2.2
MULTIDRUG
RESISTANCE
AND
P-GLYCOPROTEIN
.
0
0
YYYY
0
YY
YY
YY
YY
YY
YY
YY
YY
YY
YYYY
86
4.2.3
SIGNALLING
TRANSDUCERS
.
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87
4.2.4
LIPIDS,
MEMBRANE
LIPIDS,
AND
FLUIDITY
92
4.2.5
SPECIFIC
ANTIESTROGEN-BINDING
SITES
(AEBS)
.
.
.
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.
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.
.
94
4.3
FINAL
CONSIDERATIONS
0
0
YYYY
0
0
YYYYYYYY
0
YYYY
0
95
REFERENCES
.
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96
5
THE
HYPOTHALAMUS-PITUITARY-OVARIAN
AXIS
AS
A
MODEL
SYSTEM
FOR
THE
STUDY
OF
.
SERM
EFFECTS:
AN
OVERVIEW
OF
EXPERIMENTAL
AND
CLINICAL
STUDIES
R.
ALONSO,
F.
MARIN,
M.
GONZALEZ,
P.
GUELMES,
C.
BELLIDO,
G.
HERNANDEZ,
R.
MARIN,
MO
DIAZ,
J.EO
SDNCHEZ-CRIADO
.
.
.
.
103
5.1
INTRODUCTION
103
5.2
HYPOTHALAMUS-PITUITARY-OVARIAN
AXIS
OF
MAMMALS
.
.
.
.
.
.
.
.
.
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.
.
104
5.2.1
GENERAL
ASPECTS
0
YYYY
0
0
YY
YY
YY
YYYY
104
.
5.2.2
FUNCTIONAL
ORGANIZATION
0
0
0
YYYY
0
YYYYYYYYYY
0
105
5.2.3
ESTROGEN
FEEDBACK
REGULATION
OF
HYPOTHALAMUS
PITUITARY
AXIS
0
YYYY
0
0
0
106
5.2.4
OVERVIEW
OF
HYPOTHALAMIC
PITUITARY
FUNCTION
AT
TIME
OF
GONADOTROPIN
SURGE.
.
.
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.
112
5.3
EFFECTS
OF
SERMS
ON
HYPOTHALAMUS
PITUITARY-OVARIAN
AXIS
0
0
YYYY
0
O.
114
5.3.1
EXPERIMENTAL
STUDIES
IN
THE
RAT
115
5.3.2
LESSONS
IN
SERM
BEHAVIOR
FROM
EFFECTS
OF
TAMOXIFEN
ON
RAT
PITUITARY
FUNCTION.
.
.
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119
5.3.3
CLINICAL
STUDIES
0
YYYYYY
0
YYYY
0
YYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYY
122
5.4
SUMMARY
AND
CONCLUSIONS.
0
YY
0
0
YYYY
0
0
0
0
YYYY
0
YYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYYY
126
REFERENCES
127
6
PURE
ANTIESTROGENS
CARLOS
HERMENEGILDO
0
0
YYYY
0
0
YYYY
0
0
0
0
YY
0
0
0
YYYY
0
0
YYYY
141
6.1
INTRODUCTION.
.
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.
141
6.1.1
TYPE
I
141
6.1.2
TYPE
II
141
6.2
CHEMICAL
STRUCTURE
AND
CLASSIFICATION
.
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142
9
CARDIOVASCULAR
DISEASE
AND
SERMS
ANTONIO
CANO
207
PART
II
CLINICAL
AREA
CONTENTS
X
7
PHYSIOLOGICAL
REGULATION
OF
BONE
METABOLISM
AND
ESTROGEN
AGONISM
MIGUEL
ANGELGARCIA-PEREZ
161
7.1
NORMAL
BONE
REMODELING
"
162
7.2
EXECUTIVE
CELLS:
OSTEOBLASTS
AND
OSTEOCLASTS
163
7.3
ROLE
OF
PROINFLAMMATORY
CYTOKINES
IN
BONE
RESORPTION.
.
.
.
.
.
.
.
.
.
166
7.4
THE
RANKLIRANK/OPG
SYSTEM
167
7.5
BONE
REMODELING
AFTER
ESTROGEN
DEFICIENCY
171
7.6
EFFECTS
OF
ESTROGEN
AND
AGONIST
OF
ESTROGEN
RECEPTOR
ON
BONE
CELLS
174
7.7
CONCLUSIONS.
177
REFERENCES
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177
6.3
MECHANISM
OF
ACTION.
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143
6.4
EFFECTS
OF
PURE
ANTIESTROGENS
.
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146
6.4.1
IN
VITRO
STUDIES
146
6.4.2
EXPERIMENTS
IN
ANIMALS.
.
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147
6.4.3
CLINICAL
STUDIES
150
6.5
CLINICAL
UTILITY
152
REFERENCES
153
8
THE
ROLE
OF
SERMS
IN
THE
TREATMENT
OF
OSTEOPOROSIS
ADOLFO
DIEZ-PEREZ,
JOSE
LUIS
DUEHAS-DIEZ
187
9.1
THE
FOCAL
PHENOTYPE
OF
CVD
.
.
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208
9.1.1
THE
CRUCIAL
ROLE
OF
THE
ENDOTHELIUM
210
9.2
ESTROGEN
AGONISM
AND
CVD
212
8.1
INTRODUCTION
187
8.2
EXPERIMENTAL
RESULTS.
.
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188
8.2.1
TAMOXIFEN
"
188
8.2.2
RALOXIFENE.
.
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188
8.3
OTHER
SERMS
.
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189
8.4
CLINICAL
EFFECTS
OF
SERMS
190
8.4.1
TAMOXIFEN.
.
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190
8.4.2
RALOXIFENE.
.
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192
8.5
BONE
QUALITY
AND
ITS
RELEVANCE
195
8.6
FUTURE
SERMS
.
.
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199
REFERENCES
.
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199
-
CONTENTS
XI
9.2.1
LIPIDS
212
9.2.2
VASCULAR
WALL
213
9.3
SERMS
AS
AN
ALTERNATIVE
TO
ESTROGENS
IN
CVD
214
9.4
ACTIONS
OF
SERMS
216
904.1
ARTERIAL
DISEASE
.
.
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216
9.4.2
VTED.
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226
9.5
CONCLUSION
AND
OUTLOOK
FOR
THE
FUTURE
227
REFERENCES
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.
228
10
SERMS
AND
THE
BREAST
[OAQUIM
CALAFIALSINA,
ANTONIO
CANO
SANCHEZ.
.
.
.
.
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.
.
239
10.1
INTRODUCTION
239
10.2
BIOLOGY
OF
BREAST
DEVELOPMENT
AND
ITS
ENDOCRINE
REGULATION
240
10.3
FRAMEWORK
OF
BREAST
CANCER
RESEARCH
241
LOA
RELATIONSHIP
BETWEEN
ESTROGENS
AND
BREAST
CANCER
243
1004.1
ENDOGENOUS
ESTROGENS
.
.
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.
243
1004.2
EXOGENOUS
ESTROGENS
244
10.5
PHARMACOLOGICAL
BLOCKADE
OF
ESTROGEN
RECEPTORS:
THE
CONCEPT
OF
CHEMOPROPHYLAXIS
247
10.5.1
TAMOXIFEN
AS
ADJUVANT
THERAPY
IN
EARLY
ER(+)
BREAST
CANCER.
.
.
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.
248
10.5.2
TAMOXIFEN
IN
PRIMARY
PREVENTION
OF
ER(
+)
BREAST
CANCER
250
10.5.3
DRAWBACKS
OF
TAMOXIFEN
AS
A
PREVENTIVE
AGENT
252
10.6
RALOXIFENE
AND
BREAST
CANCER
255
10.6.1
CLINICAL
STUDIES
255
10.6.2
ESTROGEN
RECEPTOR
STATUS
.
.
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.
258
10.6.3
ESTROGEN
CIRCULATING
LEVELS
AND
RALOXIFENE
PROTECTION
258
10.604
BONE
DENSITY
AND
EFFECT
OF
RALOXIFENE
ON
THE
BREAST
260
10.6.5
OTHER
CONDITIONS
RELATED
TO
RALOXIFENE
PROTECTION
262
10.6.6
RALOXIFEN
AS
A
BREAST
CANCER
PREVENTIVE
AGENT
264
10.
7
NEW
PERSPECTIVES
265
REFERENCES
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.
266
11
ENDOMETRIAL
EFFECTS
OF
SERMS
SANTIAGO
PALACIOS
271
11.1
INTRODUCTION
271
11.2
MECHANISM
OF
ACTION
IN
THE
ENDOMETRIUM
271
11.2.1
TAMOXIFEN
272
11.2.2
RALOXIFENE
274
11.3
TAMOXIFEN
AND
ENDOMETRIUM:
CLINICAL
CONSIDERATION
275
11.3.1
ULTRASONOGRAPHIC
FINDINGS
275
-~-~--~~.
XII
CONTENTS
11.3.2
HYSTOLOGICAL
FINDINGS
275
11.3.3
TAMOXIFEN
AND
RISK
OF
ENDOMETRIAL
CANCER
277
11.4
RALOXIFENE
279
11.4.1
DATA
OBTAINED
FROM
BIOPSY
279
11.4.2
ULTRASONOGRAPHIC
DATA
AND
SYMPTOMATOLOGY
280
11.5
OTHERS
SERMS
.
.
.
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.
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.
283
11.5.1
ARZOXIFENE
283
11.5.2
BAZEDOXIFENE
ACETATE
283
11.5.3
LASOFOXIFENE
284
11.5.4
OSPEMIFENE
284
11.6
CONCLUSIONS
285
REFERENCES
.
.
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.
285
12
BENIGN
GYNECOLOGICAL
DISEASES
AND
SERMS
STEFANO
PALOMBA,
FULVIO
ZULLO
.
.
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.
.
291
12.1
INTRODUCTION
291
12.2
UTERINE
LEIOMYOMAS
291
12.2.1
TREATMENTS
OF
UTERINE
LEIOMYOMAS
292
12.2.2
SERMS
AND
UTERINE
LEIOMYOMAS
294
12.3
ENDOMETRIOSIS
302
12.3.1
TREATMENTS
OF
ENDOMETRIOSIS.
.
.
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.
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.
.
303
12.3.2
SERMS
AND
ENDOMETRIOSIS
304
12.4
CONCLUSIONS
305
REFERENCES
.
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.
.
306
13
OTHER
CLINICAL
EFFECTS
OF
SERMS
P.
ACIEN,
F.
QUEREDA,
M.L.
ACIEN
.
.
.
.
.
.
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.
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.
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.
.
.
.
.
313
13.1
UROGENITAL
TRACT
314
13.1.1
VAGINAL
TROPHISM
AND
DYSPAREUNIA
314
13.1.2
PELVIC
FLOOR
FUNCTION
AND
URINARY
DISORDERS
315
13.2
CENTRAL
NERVOUS
SYSTEM
318
13.2.1
HOT
FLASHES
AND
BETA
ENDORPHINS
320
13.2.2
MOOD,
SLEEP,
WAKING
EPISODES
321
13.2.3
COGNITIVE
FUNCTION,
ALZHEIMER'SDISEASE
(AD)
321
13.2.4
LIBIDO,
SEXUAL
FUNCTION
323
13.3
GALLBLADDER
AND
HEPATOBILIAR
SYSTEM
324
13.4
DESMOIDS
AND
MESENTERIC
FIBROMATOSIS
325
13.5
ENDOCRINE
FUNCTIONS
325
13.5.1
INSULIN
SENSITIVITY
AND
DIABETES
325
13.5.2
THYROID
FUNCTION
325
13.6
EYE,
CATARACTS
326
YY
CONTENTS
XIII
13.7
OTHER
EFFECTS
328
13.7.1
ARTHRITIS
328
13.7.2
HEMORHEOLOGICAL
EFFECTS
328
13.7.3
QUALITY
OFLIFE
(QOL)
328
REFERENCES
329
14
THE
ROLE
OF
SERMS
IN
THE
MANAGEMENT
OF
POSTMENOPAUSAL
WOMEN
]OAQUIM
CALAFIALSINA
.
.
.
.
.
.
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.
.
.
.
.
.
.
.
.
.
.
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.
.
.
.
.
.
.
.
333
14.1
INTRODUCTION
333
14.2
IDENTIFYING
TROUBLES
AND
THREATS
334
14.2.1
CARDIOVASCULAR
RISK
334
14.2.2
MENOPAUSAL
SYNDROME
335
14.2.3
OSTEOPOROSIS
336
14.2.4
BREAST
CANCER
337
14.3
INTERVENTION
TOOLS
338
14.3.1
LIFESTYLE
OPTIMIZATION
338
14.3.2
HORMONE
THERAPY
338
14.3.3
CARDIOPROTECTIVE
TREATMENTS
339
14.3.4
BONE
RESORPTION
INHIBITORS
339
14.3.5
BREAST
CANCER
RISK
340
14.4
ADRESSING
HEALTH
EXPECTANCY
IMPROVEMENT
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
.
340
14.4.1
POLY
APPROACH
AND
MULTITASKING
340
14.4.2
PHARMACOLOGICAL
POLY
APPROACH
341
14.4.3
MULTITASKING
DRUGS
342
14.5
DYNAMIC
DECISION-MAKING
DIAGRAM
344
REFERENCES
.
.
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.
346
SUBJECT
INDEX
351 |
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| dewey-sort | 3618.1 575061 |
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| illustrated | Illustrated |
| index_date | 2024-07-02T15:04:54Z |
| indexdate | 2024-07-09T20:40:57Z |
| institution | BVB |
| isbn | 3540242279 9783540242277 |
| language | English |
| oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-014871896 |
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| physical | XVII, 357 S. Ill., graph. Darst. |
| publishDate | 2006 |
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| publisher | Springer |
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| spelling | Selective estrogen receptor modulators a new brand of multitarget drugs Antonio Cano Sanchez ... (ed.) Berlin [u.a.] Springer 2006 XVII, 357 S. Ill., graph. Darst. txt rdacontent n rdamedia nc rdacarrier Estrogen Antagonists Menopause Hormone therapy Receptors, Estrogen Selective Estrogen Receptor Modulators pharmacology Selective Estrogen Receptor Modulators therapeutic use Selective estrogen receptor modulators Selektiver Östrogen-Rezeptor-Modulator (DE-588)4689537-1 gnd rswk-swf (DE-588)4143413-4 Aufsatzsammlung gnd-content Selektiver Östrogen-Rezeptor-Modulator (DE-588)4689537-1 s DE-604 Cano Sanchez, Antonio Sonstige oth DNB Datenaustausch application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=014871896&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis |
| spellingShingle | Selective estrogen receptor modulators a new brand of multitarget drugs Estrogen Antagonists Menopause Hormone therapy Receptors, Estrogen Selective Estrogen Receptor Modulators pharmacology Selective Estrogen Receptor Modulators therapeutic use Selective estrogen receptor modulators Selektiver Östrogen-Rezeptor-Modulator (DE-588)4689537-1 gnd |
| subject_GND | (DE-588)4689537-1 (DE-588)4143413-4 |
| title | Selective estrogen receptor modulators a new brand of multitarget drugs |
| title_auth | Selective estrogen receptor modulators a new brand of multitarget drugs |
| title_exact_search | Selective estrogen receptor modulators a new brand of multitarget drugs |
| title_exact_search_txtP | Selective estrogen receptor modulators a new brand of multitarget drugs |
| title_full | Selective estrogen receptor modulators a new brand of multitarget drugs Antonio Cano Sanchez ... (ed.) |
| title_fullStr | Selective estrogen receptor modulators a new brand of multitarget drugs Antonio Cano Sanchez ... (ed.) |
| title_full_unstemmed | Selective estrogen receptor modulators a new brand of multitarget drugs Antonio Cano Sanchez ... (ed.) |
| title_short | Selective estrogen receptor modulators |
| title_sort | selective estrogen receptor modulators a new brand of multitarget drugs |
| title_sub | a new brand of multitarget drugs |
| topic | Estrogen Antagonists Menopause Hormone therapy Receptors, Estrogen Selective Estrogen Receptor Modulators pharmacology Selective Estrogen Receptor Modulators therapeutic use Selective estrogen receptor modulators Selektiver Östrogen-Rezeptor-Modulator (DE-588)4689537-1 gnd |
| topic_facet | Estrogen Antagonists Menopause Hormone therapy Receptors, Estrogen Selective Estrogen Receptor Modulators pharmacology Selective Estrogen Receptor Modulators therapeutic use Selective estrogen receptor modulators Selektiver Östrogen-Rezeptor-Modulator Aufsatzsammlung |
| url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=014871896&sequence=000001&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA |
| work_keys_str_mv | AT canosanchezantonio selectiveestrogenreceptormodulatorsanewbrandofmultitargetdrugs |