ライフサイエンスコーパス: bexarotene

1 a alone, blocked the induction of IGFBP-6 by bexarotene.

2 d atorvastatin 10 mg orally beginning before bexarotene.

3 sistant patients received both tamoxifen and bexarotene.

4 ntify a novel autophagy-modulating effect of bexarotene.

5 sition significantly affects the response to bexarotene.

6 urons, and APOE3 and APOE4 mice treated with bexarotene.

7 urons, and APOE3 and APOE4 mice treated with bexarotene.

8 r protein kinase B (Akt) was also blunted by bexarotene.

9 at PPARgamma is necessary for the effects of bexarotene.

10 versus physician's choice of methotrexate or bexarotene.

11 to improved cognition and memory elicited by bexarotene.

12 -tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene, 1) as well as seven novel and two reported a

13 l methotrexate 5-50 mg once per week or oral bexarotene 300 mg/m(2) once per day) for up to 48 weeks.

14 nce status 0 to 1, were randomly assigned to bexarotene 400 mg/m(2)/d combined with carboplatin and p

15 Bexarotene 400 mg/m2 orally was to be administered conti

16 ed phase II doses are erlotinib 150 mg/d and bexarotene 400 mg/m2/d orally.

17 luded a platinum and a taxane, received oral bexarotene 400 mg/m2/d plus concomitant levothyroxine an

18 ous T-cell lymphoma with escalating doses of bexarotene (75 mg/day-300 mg/day) and denileukin diftito

19 We investigated the effects of bexarotene (a retinoid X receptor agonist), CD1530 (a re

20 t Nurr1 can be pharmacologically targeted by bexarotene, a ligand for the retinoid X receptor that fo

21 urr1 could be pharmacologically targeted via bexarotene, a ligand of Nurr1's heterodimerization partn

22 Previous studies of the retinoid, bexarotene, a retinoid X receptor-specific ligand, have

23 Bexarotene, a selective agonist for Retinoid X receptors

24 xamined the signaling pathways that transmit bexarotene action in the context of myoblast differentia

25 Bexarotene-activated retinoid X receptors (RXRs) amelior

26 In vitro data from ES cells confirmed that bexarotene-activated RXR affected neuronal development a

27 We conclude that bexarotene-activated RXRs promote genetic programs invol

28 These newly described actions of bexarotene add to the growing amount of compelling data

29 ts in the first two groups were treated with bexarotene alone, whereas the tamoxifen-resistant patien

30 Bexarotene also decreased angiotensin II-mediated inflam

31 Bexarotene also induced mRNA and protein levels for pero

32 Bexarotene also restored mitochondrial respiration defic

33 In primary neurons, bexarotene ameliorated the damaged dendrite complexity a

34 first time the neuroprotective potential of bexarotene, an FDA-approved agent, in a co-morbidity mod

35 hanism of action, reduction of ROS, by which bexarotene and CD1530 inhibit carcinogenesis.

36 nduces apoptosis that is further enhanced by bexarotene and decreases the PPAR-gamma and bcl-xL prote

37 responded rapidly to combination therapy of bexarotene and interferon (IFN)-alpha2b with complete cl

38 h UVA or UVB), topical chemotherapy, topical bexarotene, and radiotherapy including total skin electr

39 )ethynyl]benzoic acid (1), commonly known as bexarotene, and their analysis in acting as retinoid X r

40 Thus, bexarotene appears to be an effective preventive agent a

41 ated and that even low doses (150 mg/day) of bexarotene are capable of in vivo upregulation of CD25 e

42 lgia, and diarrhea were more frequent in the bexarotene arm.

43 e of an agonist to the nuclear receptor RXR, bexarotene, as monotherapy against AD, presents potentia

44 ethynyl]benzoic acid (1), otherwise known as bexarotene, as well as four novel analogues of (E)-3-(3-

45 all groups were randomly assigned to receive bexarotene at either 200 or 500 mg/m(2)/d.

46 ho were enrolled in trials of high-dose oral bexarotene at one institution.

47 that the retinoid X receptor (RXR) retinoid, bexarotene, at biologically relevant concentrations of 1

48 Bexarotene augmented CDDO-induced apoptosis in these cel

49 Previous data demonstrate that bexarotene (Bex), retinoid X receptor (RXR) agonist, red

50 Compared with dimethylsulfoxide, bexarotene blocked angiotensin II-induced SM contractile

51 nts in biological potency and selectivity of bexarotene can be achieved through rational drug design.

52 Bexarotene can be safely added to platinum-based chemoth

53 The data indicate that bexarotene can resensitize gemcitabine-resistant tumor c

54 ) that treatment of APP/PS1DeltaE9 mice with bexarotene decreased Abeta pathology and ameliorated mem

55 IL-2R expression was observed at or above a bexarotene dose of 150 mg/day.

56 In vivo, bexarotene dose-dependently inhibited TNF-alpha-induced

57 Following thromboembolic stroke bexarotene enhanced autophagy in the ischemic brain conc

58 Combining erlotinib with bexarotene enhanced growth suppression in vitro compared

59 In primary neurons, bexarotene enhanced the dendritic complexity characteriz

60 Furthermore, the model of bexarotene-enhanced myogenic differentiation will provid

61 osahexaenoic acid (DHA), in combination with bexarotene, enhances LXR:RXR target gene expression of A

62 of CDDO, either alone or in combination with bexarotene for MF/SS patients.

63 In the intent-to-treat population, bexarotene given as third or subsequent line of therapy

64 In the therapeutic model, bexarotene gradually resensitized Calu3-GemR cells to ge

65 ter in patients treated with higher doses of bexarotene (>300 mg per square meter of body-surface are

66 Bexarotene had a greater effect on calponin reduction, M

67 However, the chemopreventive efficacy of bexarotene has not been determined in mouse lung cancer

68 Bexarotene has shown efficacy in a phase I/II trial of n

69 n in rats in vivo, the results revealed that bexarotene has the capacity to coregulate subsets of Nur

70 onstrated efficacy of the oral RXR retinoid, bexarotene, has altered the treatment paradigm of early-

71 promising and warrant further evaluation of bexarotene in advanced NSCLC.

72 d effects of the retinoid X receptor agonist bexarotene in an aggressive model of AD.

73 Conclusion: The efficacy of bexarotene in patients with refractory metastatic breast

74 may represent a mechanism for resistance to bexarotene in T-cell malignancies.

75 expression profile (RNA-Seq) in response to bexarotene in the cortex of APOE4 mice.

76 findings establish the viability of applying bexarotene in the prevention and treatment of muscle-was

77 We evaluated the efficacy and safety of oral bexarotene in the treatment of patients with metastatic

78 We found bexarotene increased RXR binding to promoter regions in

79 In in vitro studies bexarotene increased the expression of autophagy markers

80 In chromatin binding experiments, bexarotene increased the occupancy of the identified enh

81 This investigation reveled that bexarotene increases the mRNA and protein levels of ABCA

82 kout cells demonstrated blunted responses to bexarotene, indicating that PPARgamma is necessary for t

83 We demonstrated that bexarotene induced apoptosis of the patient's malignant

84 ne marks H3K4me3 and H3K27me3 revealed that, bexarotene induced epigenetic changes, consistent with i

85 blood malignant T cells became resistant to bexarotene-induced apoptosis.

86 have been extended in patients who developed bexarotene-induced hypertriglyceremia and/or skin rash.

87 al was significantly longer in patients with bexarotene-induced hypertriglyceridemia and/or skin rash

88 Moreover, DHA abrogates bexarotene-induced hypertriglyceridemia in vivo.

89 Bexarotene inhibited both tumor multiplicity and tumor v

90 advanced-stage disease (IIB-IV) and include bexarotene, interferon alpha, extracorporeal photopheres

91 Bexarotene is a drug already used clinically to treat ca

92 owing amount of compelling data showing that bexarotene is a potent neuroprotective agent, and identi

93 Purpose: Bexarotene is a retinoid X receptor-selective retinoid t

94 Bexarotene is an RXR-selective retinoid that can induce

95 t the combination of denileukin diftitox and bexarotene is well tolerated and that even low doses (15

96 LGD1069 (Bexarotene) is a potent RXR-selective retinoid with redu

97 ith the retinoid X receptor-selective ligand bexarotene led us to hypothesize that such ligands could

98 The rexinoids LG100268 and bexarotene (LG1069, Targretin) were highly efficacious i

99 ries enriched in both datasets revealed that bexarotene-liganded RXR affected signaling pathways asso

100 ted with increased survival, suggesting that bexarotene may benefit a segment of first-line NSCLC pat

101 This suggests that bexarotene may have clinical utility in cancers where dr

102 For the 146 assessable patients treated with bexarotene, median age was 66 years (range, 34 to 87 yea

103 cell lymphoma who are treated with high-dose bexarotene, most likely because the retinoid X receptor-

104 d the effects of CDDO and its synergism with bexarotene on apoptosis in MF/SS cell lines (MJ, Hut78,

105 ides originate from the liver, the effect of bexarotene on lipogenesis in breast epithelial cells is

106 investigated the effects of the RXR agonist bexarotene on mRNA and protein levels of apoE, ABCA1, an

107 Here we examine if the effect of bexarotene on RXR cistrome and transcriptomes depend on

108 were pretreated with either an RXR agonist (bexarotene or 9-cis retinoic acid) or vehicle (dimethyls

109 endothelial cells with RXR agonists such as bexarotene or 9-cis-retinoid acid.

110 While monotherapy with either bexarotene or DHA resulted in modest effects in vitro an

111 Exposure to 10(-6) to 10(-10) M bexarotene or Panretin for 48 hours was associated with

112 e to 0.05 mU per liter during treatment with bexarotene (P<0.001), and the mean serum free thyroxine

113 Bexarotene patients also received lipid-lowering agents

114 the 4-NQO plus CD1530 (4N+C) and 4-NQO plus bexarotene plus CD1530 (4N+B+C) groups compared with the

115 Moreover, bexarotene pretreatment improved neuron survival in prim

116 We show that bexarotene promotes myoblast differentiation and fusion

117 Cramer et al. reported that bexarotene rapidly reduces beta-amyloid (Abeta) levels a

118 Furthermore, bexarotene reduced the progression of adenoma to adenoca

119 We now report that, although bexarotene reduces soluble Abeta40 levels in one of the

120 Whereas bexarotene regulates fundamental biological processes th

121 tients (14%) discontinued therapy because of bexarotene-related toxicity.

122 The rexinoid, bexarotene, represses cyclin D1 and EGFR expression in v

123 k treatment of 3.5 month old 5XFAD mice with bexarotene resulted in the clearance of intraneuronal am

124 Furthermore, bexarotene reversed the apoE4-driven accumulation of Abe

125 treatment of apoE4 mice with the RXR agonist bexarotene reverses the apoE4-induced cognitive and neur

126 e provide evidence that retinoids, including Bexarotene, selectively induce CTCL lineages to increase

127 XR-alpha expression compared with pretherapy bexarotene-sensitive cells.

128 Interestingly, bexarotene signaling appears to correlate with residue-s

129 firmed by in vivo studies demonstrating that bexarotene significantly improved the compromised dendri

130 Furthermore, bexarotene stimulated the rapid reversal of cognitive, s

131 ate and validate our central conclusion that bexarotene stimulates the clearance of soluble beta-amyl

132 of the PPARgamma agonist rosiglitazone with bexarotene synergistically suppressed the growth of huma

133 rystal structures of these new rexinoids and bexarotene (Targretin) bound to hRXRalpha-LBD, we reveal

134 The oral rexinoid bexarotene (Targretin) is widely used for treatment of c

135 Bexarotene (Targretin), is a synthetic high-affinity RXR

136 The synthetic rexinoid bexarotene (Targretin, LGD1069) inhibits the formation o

137 e whether addition of the synthetic rexinoid bexarotene (Targretin; Eisai Inc, Woodcliff Lake, NJ) to

138 Bexarotene (Targretin; Ligand Pharmaceuticals, Inc, San

139 However, with inclusion of bexarotene, the cells remained chemosensitive.

140 Oral administration of the RXR agonist bexarotene to a mouse model of AD resulted in enhanced c

141 Although the addition of bexarotene to chemotherapy did not improve survival in t

142 We compared bexarotene to five agonists of nuclear receptors (PPARal

143 s study, we have investigated the ability of bexarotene to inhibit lung tumor progression in the muta

144 Here, we evaluate the ability of bexarotene to modulate the acquisition and maintenance o

145 rrence of high-grade hypertriglyceridemia in bexarotene-treated patients strongly correlated with inc

146 ever, a subpopulation (approximately 40%) of bexarotene-treated patients who experienced National Can

147 Bexarotene-treated patients with grade 3/4 hypertriglyce

148 Bexarotene treatment at a dose of 250 mg/kg diet was ass

149 Cramer et al. demonstrates short-term bexarotene treatment clearing preexisting beta-amyloid d

150 mic adverse effects associated with standard bexarotene treatment from the antiproliferative effects

151 Moreover, bexarotene treatment improved remote memory stabilizatio

152 creased number of neuronal progenitors after bexarotene treatment in the dentate gyrus of APOE3 and A

153 roliferation and apoptosis were modulated by bexarotene treatment independently of estrogen signaling

154 llectively, these data provide evidence that bexarotene treatment reduced neuron loss, elevated level

155 induced by Abeta42 in vitro was inhibited by bexarotene treatment.

156 econdary to renal insufficiency unrelated to bexarotene treatment.

157 d cytoplasmic lipid droplets after long-term bexarotene treatment.

158 mic therapies at least one of which included bexarotene unless intolerable.

159 Moreover, bexarotene was able to restore dysfunctional Ret-depende

160 o gemcitabine but were growth inhibited when bexarotene was added to the cytotoxic agent.

161 In the phase I portion, the daily MTD of bexarotene was determined to be 400 mg/m2.

162 Once the maximum-tolerated dose (MTD) of bexarotene was determined, the study entered the phase I

163 In the phase I portion, the daily dose of bexarotene was escalated in cohorts of three patients fr

164 Bexarotene was given by gavage starting at 16 weeks afte

165 Although our data demonstrated that bexarotene was ineffective in neuroprotection in rats in

166 for non-small-cell lung cancer, the rexinoid bexarotene was most effective for patients who developed

167 tients became euthyroid after treatment with bexarotene was stopped.

168 The salutary effects of bexarotene were accompanied by reduced plaque burden, de

169 the remaining patients, adverse reactions to bexarotene were generally mild to moderate.

170 The agonist bexarotene, when used in concentrations achievable in hu

171 In this phase I/II trial, we combined bexarotene with cisplatin and vinorelbine in the treatme

172 In patients with advanced NSCLC, bexarotene with cisplatin and vinorelbine yielded accept

173 It was hypothesized that combining bexarotene with the EGFR inhibitor, erlotinib, would aug

174 It is noteworthy that combining low doses of bexarotene with the PPARgamma agonist rosiglitazone prov