ライフサイエンスコーパス: ebselen

1 preventable with a peroxynitrite scavenger, ebselen.

2 n be completely prevented by the antioxidant ebselen.

3 al cells in 22-week-old ZDF was prevented by ebselen.

4 nd provided an additive inhibitory effect to ebselen.

5 locked by the glutathione peroxidase mimetic ebselen.

6 diselenides 8 were 3-6-fold more active than ebselen.

7 contributing to the therapeutic potential of ebselen.

8 menable to inhibition by compounds including ebselen.

9 (pro) and four M(pro) inhibitors superior to ebselen.

10 d LRRK2/PRDX3 flies with a peroxidase mimic, Ebselen.

11 of catalase as well as by co-treatment with Ebselen.

12 a previously unrecognized in vivo target of ebselen.

13 talase, and the glutathione peroxidase mimic ebselen.

14 eveloping OLs was prevented by the GPx mimic ebselen.

15 restored by the ONOO(-) scavengers urate and ebselen.

16 Ebselen 1% and 2% significantly reduced the bacterial lo

17 Rats were given ebselen (1-100 mg/kg i.p.) followed by aerosolized LPS e

18 Ebselen (10-100 microM) inhibited the proliferation of S

19 lenge treatment with oral administrations of ebselen (100 mg/kg per day).

20 t phase 1 was unaffected by the antioxidants ebselen (100 mum) and TEMPOL (3 mm).

21 -benzisoselenazol-3(2H)-ones, represented by ebselen (1a), are being studied intensively for a range

22 lene iodonium, 1.4+/-0.3-fold migration; and ebselen, 2.0+/-0.5-fold migration), as did overexpressio

23 Ebselen (20-50 microm), a glutathione peroxidase mimetic

24 re enrolled and randomly assigned to receive ebselen 200 mg (n=22), 400 mg (n=20), or 600 mg (n=21),

25 of Florida (Gainsville, FL, USA) to receive ebselen 200 mg, 400 mg, or 600 mg, or placebo orally twi

26 S-dependent as assessed by pretreatment with ebselen (3.6 +/- 0.2 versus 1.1 +/- 0.2), diphenylene io

27 PBN (100 microm), POBN (100 microm), and ebselen (50 microm) restored complex I activity.

28 Whereas azo-bis-ebselens 7 were poor mimics of the glutathione peroxidas

29 In contrast, ebselen (a glutathione peroxidase mimetic and inhibitor

30 ential therapeutics for suicidality, such as ebselen (a lithium mimetic), piracetam (a nootropic), ch

31 ormation was greatly diminished when GSH and ebselen (a selenoperoxidase mimetic) were present, consi

32 Consistent with this idea, it was found that ebselen, a compound with GSHPx-like activity, was able t

33 cysteine (NAC), a non-specific antioxidant, ebselen, a glutathione mimetic, or combined SOD plus cat

34 A decrease in ROS by ebselen, a glutathione peroxidase mimetic, or by transdu

35 constants for amino acid hydroperoxides with ebselen, a glutathione peroxidase mimic, were also deter

36 nergic neuronal cells and determined whether ebselen, a glutathione peroxidase-mimetic, protected aga

37 Oral treatment of diabetic rodents with ebselen, a GPx mimetic that is approved for human clinic

38 Ebselen, a novel GPx1 mimic, has been shown to reduce bo

39 r (CE) hydroperoxides and were diminished by ebselen, a reducing agent.

40 Trx1 in HeLa cells from oxidation caused by ebselen, a superfast oxidant for Trx1.

41 antioxidants pyrrolidine dithiocarbamate and ebselen abolish transcriptional activation of these gene

42 We demonstrated that ebselen acts through inhibition of protein synthesis and

43 In summary, ebselen affects the phosphoinositide cycle and has CNS e

44 PBN and ebselen also restored glutathione levels in DOX-treated

45 atment with the glutathione peroxidase mimic ebselen also reversed behavioral deficits in this animal

46 One of these compounds (ebselen) also exhibited promising antiviral activity in

47 and resonance Raman spectroscopy showed that ebselen altered the active site heme of rIDO by inducing

48 Ebselen ameliorated fasting hyperglycemia, sustained non

49 Ascorbic acid, melatonin and ebselen (an additional antioxidant) also fully prevented

50 own that 2-phenylbenzisoselenazol-3(2H)-one (ebselen), an organoselenium anti-inflammatory small-mole

51 We further demonstrate that ebselen, an anti-oxidant drug already safely used in hum

52 n (ZL) rats and after chronic treatment with ebselen, an antioxidant and peroxinitrite scavenger.

53 ent of Zucker diabetic fatty (ZDF) rats with ebselen, an oral GPx mimetic, will prevent beta-cell det

54 Ebselen, an organoselenium compound, is known to be clin

55 the second part of our work, we employed 11 ebselen analogues-bis(2-carbamoylaryl)phenyl diselenides

56 Ebselen and a caspase-3 inhibitor provided significant p

57 Both ebselen and boronates may be used as small molecule scav

58 n this study, we screened a collection of 34 ebselen and ebselen diselenide derivatives for SARS-CoV-

59 At therapeutically relevant concentrations, ebselen and ebselen oxide caused decreased 14-3-3 levels

60 ly measured barrier of 8.8 kcal/mol for both ebselen and GPx.

61 ilised SOD1 is arrested by the clinical drug ebselen and its analogues (MR6-8-2 and MR6-26-2) by rede

62 We have examined the binding modes of ebselen and its derivative in M(pro) via high resolution

63 The reaction of ebselen and its derivatives (1-7) with peroxynitrite ani

64 n crystallographic structures of M(pro) with ebselen and MR6-31-2 suggesting hydrolysis of the enzyme

65 structures of Ag85C covalently modified with ebselen and other thiol-reactive compounds, p-chloromerc

66 Stronger M(pro) inhibition than ebselen and potent ability to rescue infected cells were

67 tential and is inhibited by the antioxidants ebselen and TEMPOL, consistent with the concept that it

68 antioxidants pyrrolidinedithiocarbamate and ebselen and the Cu,Zn superoxide dismutase inhibitor die

69 computed value of 7.1 kcal/mol for the drug ebselen and the experimentally measured barrier of 8.8 k

70 n SARS-CoV-2 major protease (Mpro) inhibitor ebselen and the HIV integrase inhibitor raltegravir, rev

71 inhibitable by the peroxynitrite scavengers ebselen and uric acid, was markedly increased in apoE(-/

72 re, antiapoptotic antioxidants (e.g. FeTBAP, ebselen, and alpha-phenyl-tert-butyl nitrone) inhibited

73 The antioxidants tempol, ebselen, and deferoxamine inhibited CO-induced O2*- prod

74 ibited by the antioxidants N-acetylcysteine, ebselen, and exogenously added catalase.

75 e (III) tetrakis (4-benzoic acid) porphyrin, ebselen, and N-acetylcysteine failed to prevent cell dea

76 Concomitant with the reversal of senescence, ebselen, and NOHA each restored NO production to levels

77 which is improved by peroxinitrite scavenger ebselen, and thus considered its cause and not consequen

78 est that the anti-inflammatory properties of ebselen are achieved through an inhibition of lung ICAM-

79 tion for further analysis and development of ebselen as a potential treatment for multidrug-resistant

80 H. pylori enzymes, respectively, indicating ebselen as one of the most potent low-molecular-weight i

81 Ebselen at 5-20 micro M inhibited Con A-induced prolifer

82 s ROS production in both populations; and 3) ebselen at 5-20 micro M inhibits DC-induced proliferatio

83 ing ligand of 14-3-3 isoforms z, e, y, and n Ebselen bonding decreased 14-3-3z binding to its partner

84 nin) or enhancement of peroxide consumption (ebselen) but not inhibition of xanthine oxidase (allopur

85 Pretreatment with ebselen, catalase, and the flavoprotein inhibitor diphen

86 Novel azo-bis-ebselen compounds 7 were prepared by reduction of 7-nitr

87 s with crystallographic analysis of the CypD-ebselen crystal structure (PDB code: 8EJX).

88 Ebselen decreased slow-wave sleep and affected emotional

89 Ebselen decreased the abundance of 3-nitrotyrosine-modif

90 uction of pre-existing lipid peroxides using ebselen delayed HbLDL kinetics and inhibited HO-1 induct

91 Our studies revealed that ebselen derivatives are potent inhibitors of both the pr

92 Ebselen did not induce any behavioral changes and did no

93 , we screened a collection of 34 ebselen and ebselen diselenide derivatives for SARS-CoV-2 PL(pro) an

94 nd, 2-phenyl-1,2-benzisoselenazol-3(2H)-one (ebselen), displayed Ki values equal to 2.11 and 226 nM a

95 Screening of 25 analogs of Ebselen, diversified at the N-aromatic residue, led to t

96 re tone audiometry; a reduction of 50% in an ebselen dose group compared with the placebo group was j

97 Ebselen doubled beta-cell mass, prevented apoptosis, pre

98 We identified ebselen (EB) and its analogs ebselen oxide (EO) and 2-(4

99 Here we identify ebselen (EBS) as a potent inhibitor of the Mycobacterium

100 Ebselen (EBS), 2-phenyl-1,2-benzisoselenazol-3(2H)-one,

101 Substrate binding studies showed that ebselen enhanced nonproductive l-tryptophan binding, whi

102 treatments with the peroxynitrite scavenger, ebselen, eNOS intermediate N(omega)-hydroxy-L-arginine (

103 We assessed the safety and efficacy of ebselen for the prevention of noise-induced hearing loss

104 Combining ATG with ebselen gave a strong synergistic effect, leading to Trx

105 at 4 kHz was 1.32 dB (SE 0.91) in the 400 mg ebselen group compared with 4.07 dB (0.90) in the placeb

106 Two participants in the 200 mg ebselen group were discontinued from the study before th

107 try, or radiological assessments between the ebselen groups and the placebo group.

108 Ebselen had no effect on the monoamine oxidase activity

109 An organoselenium drug called ebselen has been demonstrated to have potent M(pro) inhi

110 Ebselen has been tested in clinical trials for other dis

111 This study provides evidence that ebselen has great potential for topical treatment of MRS

112 Ebselen has recently emerged as a promising drug candida

113 n peroxide three times more efficiently than Ebselen in the presence of glutathione as a stoichiometr

114 h from menadione was blocked by catalase and ebselen, indicating that death was secondary to oxidant

115 We conclude that nitrone spin traps and ebselen inhibit the DOX-induced apoptotic signaling mech

116 Exposure of human macrophages to ebselen inhibited IDO activity in a manner independent o

117 The antioxidant ebselen inhibited SMC activities in vitro and intralesio

118 Ebselen inhibited the activity of recombinant human IDO

119 These findings indicate that ebselen inhibits IDO activity by reacting with the enzym

120 We previously reported that ebselen inhibits inositol monophosphatase (IMPase) and e

121 Here we report that the antioxidant ebselen inhibits inositol monophosphatase and induces li

122 C25 appeared to be the preferential site of ebselen interaction in vitro, whereas modification of C9

123 Infusion of the antioxidant ebselen into WT mice also significantly blocked the incr

124 Here we show that the selenezal drug ebselen is a potent IDO inhibitor.

125 Since ebselen is an oral antioxidant currently used in clinica

126 We conclude by showing that ebselen is capable of inducing transcription of the anti

127 s, we find that polytherapy using CuATSM and ebselen is highly effective and acts in synergy to reduc

128 Ebselen is part of the National Institutes of Health Cli

129 ompound ebsulfur (EbS), a sulfur analogue of ebselen, is a potent inhibitor of T. brucei growth with

130 Our work shows that ebselen, its derivatives, and diselenide analogues const

131 d a selenium-containing antioxidant compound ebselen known to modulate both thioredoxin and glutaredo

132 nt response element (ARE) and postulate that ebselen may act both by the transcriptional upregulation

133 ata suggest that a polytherapy of CuATSM and ebselen may merit more study as an effective method of t

134 "redox cycling"), biochemical pharmacology (ebselen), nutritional biochemistry and micronutrients (s

135 ectroscopy revealed covalent modification by ebselen of all cysteines through a selenylsulfide bond.

136 ly explanation for the beneficial effects of ebselen on beta-cell mass and function.

137 Therefore, the effect of ebselen on endothelial senescence and vasculopathy in a

138 We evaluated the effect of ebselen on human SH-SY5Y dopaminergic neuronal cells and

139 This was not a global effect of ebselen on LPS-induced gene expression, because the rise

140 Studies using the H(+)-ATPase inhibitor ebselen or a yeast genetic strain with reduced H(+)-ATPa

141 s and by co-incubations with the antioxidant ebselen or cytochalasin D.

142 d either the antioxidants, alpha tocopherol, ebselen, or idebenone (a coenzyme Q analogue); or the MP

143 We identified ebselen (EB) and its analogs ebselen oxide (EO) and 2-(4-methylphenyl)-1,2-benzisothi

144 tically relevant concentrations, ebselen and ebselen oxide caused decreased 14-3-3 levels in SH-SY5Y

145 Ebselen potently protects lysosomal membrane integrity,

146 Ebselen pretreatment also prevented lung ICAM-1 mRNA up-

147 Ebselen pretreatment inhibited neutrophil influx and act

148 An antioxidant/peroxynitrite scavenger, ebselen, prevented stress-induced SIRT1 depletion and su

149 of oxidative stress is the mechanism whereby ebselen prevents apoptosis and preserves intranuclear Pd

150 Inhibition of CypD by ebselen protects against sporadic Alzheimer's disease- a

151 labeling and mass spectrometry revealed that ebselen reacted with multiple cysteine residues of IDO.

152 Challenges with Ebselen recapitulated similar rescue of these phenotypic

153 trial with healthy participants, acute oral ebselen reduced brain myo-inositol in the anterior cingu

154 The ONOO- scavenger ebselen reduced DNA fragmentation and caspase-3 activity

155 hondria-targeted hydrogen peroxide scavenger ebselen, reduced Sirt3 S-glutathionylation, diminished S

156 Therefore, ebselen represents a lithium mimetic with the potential

157 Treatment of db/db mice with Ebselen restored the resistance of both BMDCs and endoth

158 s well as reducing lipid hydroperoxides with ebselen, resulted in inhibition of macrophage activation

159 onium, or the glutathione peroxidase mimetic ebselen significantly attenuated migration (PDGF alone,

160 nium or the antioxidants N-acetylcysteine or ebselen significantly inhibited Ang II-induced cAbl phos

161 tion states upon Ag-specific interaction; 2) ebselen significantly inhibits ROS production in both po

162 late, alpha-phenyl-N-tert-butyl nitrone, and ebselen significantly suppressed iNOS transgene inductio

163 Chronic ebselen therapy also ameliorated vasculopathy with lipid

164 challenge; their competence was restored by Ebselen therapy.

165 lthiosemicarbazonato)copper(II) (CuATSM) and ebselen to mimic the metal delivery and disulfide bond p

166 as well as a high affinity substrate of TR1, ebselen, to demonstrate that Tat-dependent transcription

167 CuDIPs and the glutathione reductase mimetic ebselen, TPA-stimulated TNFalpha shedding from PKCepsilo

168 Moreover, ebselen-treated zebrafish displayed decreased brain 14-3

169 Chronic ebselen treatment of ZDF rats restored renal tissue leve

170 Ebselen treatment was well tolerated across all doses an

171 pared to that of the diphenyl diselenide and ebselen, used as references, respectively.

172 non-toxic and biocompatible CypD inhibitor, ebselen, using a conventional PPIase assay to screen a l

173 ticles, was almost completely prevented when ebselen was administered from 8 to 22 weeks and partiall

174 The therapeutic efficacy of ebselen was evaluated in a mouse model of staphylococcal

175 stability of 14-3-3z Among these compounds, ebselen was identified as a covalent, destabilizing liga

176 Recently, ebselen was identified as an effective inhibitor of the

177 Additionally, ebselen was remarkably active and significantly reduced

178 INTERPRETATION: Treatment with ebselen was safe and effective at a dose of 400 mg twice

179 Independently, ebselen was shown to inhibit the N7-methyltransferase ac

180 the corresponding des-bromo compound 3a and ebselen when evaluated in the coupled reductase assay.

181 ith either 5 mM GSH, 2 mM GSH-MEE, or 0.1 mM ebselen, when instilled into the mucosal fluid, resulted

182 This study shows that ebselen, which is a promising drug candidate against can

183 Removal of cysteine-bound ebselen with dithiothreitol reversed the effects of the

184 ersion of protein beta-lactoglobulin A using ebselen within 30 s.

185 postulated that the seleno-organic compound ebselen would attenuate neutrophil recruitment and activ