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1 (cRbm20(DeltaRRM)-DMSO and cRbm20(DeltaRRM)-raloxifene).
2 t expressed N2BAsc (TAC/DOCAcRbm20(DeltaRRM)-raloxifene).
3 y to their target (biotin, desthiobiotin and raloxifene).
4 d with the experimental structure of ERalpha-raloxifene.
5 efits from chemoprevention with tamoxifen or raloxifene.
6 moxifen was associated with more events than raloxifene.
7 of metabolism of the known CYP3A4 substrate raloxifene.
8 diated oxygenation versus dehydrogenation of raloxifene.
9 per year and causes cataracts compared with raloxifene.
10 drugs modulating estrogen signaling such as Raloxifene.
11 0.82; 95% CI, 0.68-0.99) in the women taking raloxifene.
12 ated by 17beta-estradiol (E2), tamoxifen, or raloxifene.
13 0002); no increase has been seen so far with raloxifene.
14 in the prevention trials; p<0.0001) and with raloxifene.
15 ffect on the potency or efficacy of the SERM raloxifene.
16 k of breast cancer who may benefit most from raloxifene.
17 phene (BT) scaffold common to arzoxifene and raloxifene.
18 at is not required for inhibition of PLD1 by raloxifene.
19 f raloxifene, and 94 (3.7%) with 120 mg/d of raloxifene.
20 n both cell lines after exposure to 10(-6) M raloxifene.
21 duction and is enhanced by acetazolamide and raloxifene.
22 ptor alpha and responded to retreatment with raloxifene.
23 relative benefits and harms of tamoxifen and raloxifene.
24 e estrogen receptor modulators tamoxifen and raloxifene.
25 k-reducing medications, such as tamoxifen or raloxifene.
26 ncer and cataracts compared with placebo and raloxifene.
29 ge was significantly lower in those assigned raloxifene (50 events) compared with placebo (84 events;
31 101; mean age, 67 years) were randomized to raloxifene 60 mg/d or placebo for a median of 5.6 years.
36 Patients were randomly assigned to receive raloxifene, 60 mg/d (n = 2557), or 120 mg/d (n = 2572),
37 gen agonist (ethynyl estradiol) and the SERM raloxifene, 7-(R) was found to be a potent SERM that beh
38 ration mouse model (Abca4 (-/-) Rdh8 (-/-)), raloxifene (a benzothiophene-type scaffold SERM) prevent
42 e Use for The Heart (RUTH) trial showed that raloxifene, a selective estrogen receptor modulator, had
46 by the effective synthesis of a precursor of raloxifene, a selective estrogen receptor modulator.
49 In endometrial cells, tamoxifen, but not raloxifene, acts like estrogen by stimulating the recrui
50 or (ER) modulators tamoxifen and LY117018 (a raloxifene analogue) partially reversed SPF45-mediated d
52 n of estradiol (E(2)) and two antiestrogens, raloxifene and 4-hydroxytamoxifen, in estrogen receptor
53 found convincing evidence that tamoxifen and raloxifene and adequate evidence that aromatase inhibito
56 of virtual hits on drug databases identified raloxifene and bazedoxifene as potential inhibitors of I
58 ind, randomized, placebo-controlled trial of raloxifene and CVD outcomes in 10 101 postmenopausal wom
59 ntly associated with serious adverse events; raloxifene and estrogen increase thromboembolic events;
61 important difference in the effects of TAM, raloxifene and ICI 182,780 on immunosurveillance in brea
62 The minor structural differences between raloxifene and one of its derivatives (Y 134) had a majo
64 controlled, multiyear Study of Tamoxifen and Raloxifene and Raloxifene Use in the Heart clinical tria
65 ancer cells are not completely eradicated by raloxifene and rapidly expand if raloxifene treatment is
73 lective estrogen receptor modulators (SERM), raloxifene and tamoxifen, can perturb DC development and
75 .7%) with placebo, 82 (3.2%) with 60 mg/d of raloxifene, and 94 (3.7%) with 120 mg/d of raloxifene.
76 found that the benefits of taking tamoxifen, raloxifene, and aromatase inhibitors to reduce risk for
78 medications (bisphosphonates, teriparatide, raloxifene, and denosumab) compared with placebo, usual
79 d by antiestrogen ligands such as tamoxifen, raloxifene, and droloxifen, which was confirmed in chrom
80 women, bisphosphonates, parathyroid hormone, raloxifene, and estrogen reduce primary vertebral fractu
82 /p160 interactions, whereas 4(OH)-tamoxifen, raloxifene, and ICI-182,780 inhibit these interactions.
83 fine the complex tissue responses to 4HT and raloxifene, and suggests that these ligands can have a b
86 egulated in ERalpha cells in response to E2, raloxifene, and tamoxifen were distinct from those regul
88 ulators (SERMs) 4-hydroxytamoxifen (4HT) and raloxifene are able to elevate SRC-1 and SRC-3 protein l
91 n studies such as the Study of Tamoxifen and Raloxifene are available to women at increased risk of d
95 oestrogen-receptor modulators--tamoxifen and raloxifene--are so far the only medical options approved
97 rogen receptor modulators (SERMs; tamoxifen, raloxifene, arzoxifene, and lasofoxifene) with placebo,
98 revention agents were identified: tamoxifen, raloxifene, arzoxifene, lasofoxifene, exemestane, and an
99 itor exemestane in addition to tamoxifen and raloxifene as a breast cancer prevention medication, alt
100 by Spurgeon et al which evaluates oral SERM raloxifene as a potential therapeutic agent for HPV-asso
102 Early findings on the use of tamoxifen or raloxifene as prophylaxis against breast cancer have bee
104 ery P450 tested except CYP2E1 was capable of raloxifene bioactivation, based on glutathione adduct fo
105 as seen in the STAR (Study of Tamoxifen and Raloxifene) breast cancer prevention trial and in other
106 d threshold of 1.66% for use of tamoxifen or raloxifene but >or= 1.66% when using the updated model.
112 the Cognition in the Study of Tamoxifen and Raloxifene (Co-STAR) trial, beginning 18 months after ST
114 h outcomes to calculate the net benefit from raloxifene compared with placebo and tamoxifen compared
115 in the PANSS general symptom scores for the raloxifene compared with the placebo (beta = -3.72; 95%
118 ion in adult mice was triggered by injecting raloxifene (cRbm20(DeltaRRM)-raloxifene), with dimethyl
119 or multiple risk factors for CHD to 60 mg of raloxifene daily or placebo and followed them for a medi
120 trial, low strength of evidence); high-dose raloxifene decreased risk for MCI but not for dementia (
123 is model using various ER ligands, including Raloxifene, Diethylstilbestrol, E2, and 4-hydroxytamoxif
124 putative ester, formed by the conjugation of raloxifene diquinone methide with a carboxylic acid moie
127 (ICI), as well as a selective ER modulator, raloxifene, efficiently clear cancer and its precursor l
128 to sham control rats (p < 0.05), whereas E2, raloxifene, EM652, and alendronate regulated 613, 765, 6
129 e risk for thromboembolic events (tamoxifen, raloxifene), endometrial cancer (tamoxifen), or stroke (
130 or dihydrotestosterone, but differently from raloxifene, estren alters the activity of Elk-1, CCAAT e
132 ent data from the MORE (Multiple Outcomes of Raloxifene Evaluation) trial have evaluated health-relat
134 estradiol levels greater than 10 pmol/L with raloxifene for 4 years would have avoided 47% of breast
136 ld not prescribe anastrozole, exemestane, or raloxifene for breast cancer risk reduction to premenopa
137 sized to play an important role in orienting raloxifene for dehydrogenation through a combination of
138 opausal estrogen plus progestogen therapy or raloxifene for the treatment of osteoporosis in women.
139 enistein), but not antagonists (tamoxifen or raloxifene), for 48 h inhibits GR-mediated MMTV-LUC tran
140 tine use of medications,such as tamoxifen or raloxifene, for risk reduction of primary breast cancer
141 gs diclofenac (DCF), troglitazone (TGZ), and raloxifene, for which we observed known metabolic oxidat
143 n the tamoxifen group (57 cases) than in the raloxifene group (80 cases) (incidence, 1.51 vs 2.11 per
145 tradiol levels greater than 10 pmol/L in the raloxifene group had a rate of breast cancer that was 76
146 symptom assessment analyses, the 9769 in the raloxifene group reported greater mean symptom severity
147 adder control problems, whereas women in the raloxifene group reported more musculoskeletal problems,
148 BMD at the femoral neck; however, within the raloxifene group, lower baseline CrCl was associated wit
149 ifferences existed between the tamoxifen and raloxifene groups in patient-reported outcomes for physi
154 for the reduction of breast cancer risk, and raloxifene has demonstrated a reduced risk of breast can
156 erential impact in vivo In summary, the SERM raloxifene has structural and functional neuroprotective
160 eatment strategies, such as the antiestrogen raloxifene, have shown promising results; however, furth
163 ound to ERalpha in an orientation similar to raloxifene; however, a number of residues adopted differ
164 ratio [HR], 1.01 [95% CI, 0.85 to 1.21]) or raloxifene (HR, 1.18 [CI, 0.96 to 1.46]) and alendronate
168 effectiveness of SERMs such as tamoxifen and raloxifene in breast cancer depends on their antiestroge
169 he comparative abilities of tamoxifen versus raloxifene in breast cancer prevention are currently bei
170 ers and SERM nonusers, suggesting a role for raloxifene in endometrial cancer prevention and individu
171 are minimally regulated by estradiol (E2) or raloxifene in ERalpha-positive MCF-7 human breast cancer
176 ed to tamoxifen and 168 in those assigned to raloxifene (incidence, 4.30 per 1000 vs 4.41 per 1000; r
179 that the mixed estrogen agonist/antagonist, raloxifene, induces apoptosis in androgen-independent hu
181 titin (N2BAsc), which, within 3 weeks after raloxifene injection, made up approximately 45% of total
187 nown whether treatment for osteoporosis with raloxifene is safe or effective in those with chronic ki
189 erent for each pharmaceutical agent and that raloxifene maintained more genes at sham levels than any
191 lecular mechanism of apoptosis suggests that raloxifene may be a therapeutic agent for human bladder
196 icate that a prolonged treatment period with raloxifene might be required to prevent recurrence of ne
198 y assigned to receive 60 mg/d or 120 mg/d of raloxifene (n = 4843) or matching placebo (n = 2447) for
201 We provide detailed results of the effect of raloxifene on coronary outcomes over time and for 24 sub
202 udy, we compare the effects of tamoxifen and raloxifene on PLD in the ER-positive mammary epithelial
203 ausal women with osteoporosis, the effect of raloxifene on rate of change of bone mineral density (BM
206 cells was completely inhibited by 500 nmol/L raloxifene or 500 nmol/L 4-hydroxytamoxifen, these conce
207 of PI-9, and makes tamoxifen (TAM), but not raloxifene or ICI 182,780, a potent inducer of PI-9.
212 dent and was nearly absent when ICI 182,780, raloxifene, or 4-hydroxytamoxifen were bound to the ERs.
213 e that risk-reducing medications (tamoxifen, raloxifene, or aromatase inhibitors) provide at least a
214 isk-reducing medications, such as tamoxifen, raloxifene, or aromatase inhibitors, in women who are no
215 isk-reducing medications, such as tamoxifen, raloxifene, or aromatase inhibitors, to women who are at
216 ERalpha and increased the reactivity of the raloxifene- or ICI 182,780-bound ERalpha, with probes th
218 tazolamide (oral or intra-arterial) and oral raloxifene (P=0.0248, P<0.0001, and P=0.0006, respective
220 dence suggesting the antagonistic effects of raloxifene persisted in the reproductive tract after tre
221 en with osteoporosis, and both tamoxifen and raloxifene prevent breast cancer in high-risk women.
222 d, estrogen, parathyroid hormone (1-34), and raloxifene prevent vertebral fractures more than placebo
223 Moreover, continuous treatment of mice with raloxifene prevented the emergence of recurrent disease
225 y the SERMs trans-hydroxytamoxifen (TOT) and raloxifene (Ral) or ICI 182,780 (ICI) and by estradiol (
226 owever, among those with a fracture history, raloxifene recipients experienced more nonvertebral frac
231 ures (both moderate SOE), whereas 4 years of raloxifene reduced vertebral but not nonvertebral fractu
233 d in part on the improved safety profile for raloxifene relative to the standard treatment of tamoxif
235 formation activity and that ovariectomy plus raloxifene resembles sham more closely than ovariectomiz
236 d to formation of estrogen receptor-positive raloxifene-responsive mammary carcinomas with features o
237 r risk whether or not they were treated with raloxifene (risk difference, -0.1%; 95% CI, -0.8% to 0.6
238 tio, 0.70 [95% CI, 0.59 to 0.82]; 4 trials), raloxifene (risk ratio, 0.44 [CI, 0.27 to 0.71]; 2 trial
239 atio, 1.93 [CI, 1.41 to 2.64]; 4 trials) and raloxifene (risk ratio, 1.60 [CI, 1.15 to 2.23]; 2 trial
240 [95% CI, 0.59-0.84]; 4 trials [n = 28 421]), raloxifene (RR, 0.44 [95% CI, 0.24-0.80]; 2 trials [n =
241 k [RR], 0.69 [95% CI, 0.59-0.84]; 4 trials), raloxifene (RR, 0.44 [95% CI, 0.24-0.80]; 2 trials), and
243 ew results from STAR (Study of Tamoxifen and Raloxifene) showed that tamoxifen reduced breast cancer
244 xypurinol or aldehyde oxidase (AO) inhibitor raloxifene significantly decreased NO generation from ni
245 en Receptor Modulators (SERMs) tamoxifen and raloxifene, so called for their ability to function as E
247 t provided data on the harms of tamoxifen or raloxifene, studies of the costs of chemoprevention, and
249 wn without cardiomyopathy is achievable with raloxifene, suggesting toxicity is not simply from Cre.
250 olved in the positioning and/or catalysis of raloxifene supporting dehydrogenation were identified wi
251 are endometrial cancer risks associated with raloxifene, tamoxifen, and nonusers of a selective estro
252 The SERMs investigated in this study include raloxifene, tamoxifen, and the tamoxifen metabolites 4-h
254 sk for invasive breast cancer was higher for raloxifene than tamoxifen in 1 trial after long-term fol
255 ethinyl estradiol, the benzothiophene SERM, raloxifene, the benzopyran SERM, (S)-3-(4-hydroxyphenyl)
256 ated the recurrence of cervical cancer after raloxifene therapy in our preclinical model of human pap
257 y confirm CYP3A4-mediated dehydrogenation of raloxifene to a reactive diquinone methide but also sugg
258 hanism of CYP3A4-mediated dehydrogenation of raloxifene to a reactive diquinone methide, while exclud
260 ent studies have demonstrated the ability of raloxifene to form reactive intermediates and act as a m
262 ective ability of the SERM tamoxifen but not raloxifene to regulate miR-451 and 14-3-3zeta may assist
266 cancer in mice re-exposed to estrogen after raloxifene treatment, despite evidence suggesting the an
267 ast and Bowel Project Study of Tamoxifen and Raloxifene trial, a prospective, double-blind, randomize
272 tiyear Study of Tamoxifen and Raloxifene and Raloxifene Use in the Heart clinical trials have recentl
276 actors, the odds of endometrial cancer among raloxifene users was 50% that of nonusers (odds ratio [O
278 studies of medication initiators: a study of raloxifene versus alendronate in 1-year nonvertebral fra
280 positive symptom scores (beta for change in raloxifene vs placebo, -1.92; 95% CI, -3.83 to 0.00; P =
281 esigned to evaluate the relative efficacy of raloxifene vs tamoxifen in reducing the incidence of inv
283 ifen and Raloxifene (STAR) demonstrated that raloxifene was as effective as tamoxifen in reducing the
284 al stroke according to group assignment, but raloxifene was associated with an increased risk of fata
287 in cellular morphology after treatment with raloxifene was no longer observed when cells were pretre
288 onary events, the overall lack of benefit of raloxifene was similar across the prespecified subgroups
293 AF2ER activation levels with ICI, OHT, and raloxifene were parallel with the degree of AF2ER-LBD ho
296 esults from the NSABP Study of Tamoxifen and Raloxifene, which compares the risk-reducing efficacy as
299 tion, pairing the estrogen response modifier raloxifene with the c-Met/VEGFR2 kinase inhibitor caboza
300 ed by injecting raloxifene (cRbm20(DeltaRRM)-raloxifene), with dimethyl sulfoxide (DMSO)-injected mic