ライフサイエンスコーパス: rottlerin

1 bitors (i.e., 4 microM GF109203X or 5 microM rottlerin).

2 egative PKCdelta, and the PKCdelta inhibitor rottlerin.

3 inhibitors including the PKCdelta inhibitor rottlerin.

4 o TRAIL either in the absence or presence of rottlerin.

5 orine (up to 0.1 mM) but can be inhibited by rottlerin.

6 appaBalpha degradation were not inhibited by rottlerin.

7 a Ca(2+)-independent PKC isoform inhibitor, rottlerin.

8 to the mammalian channel agonists NS1619 and rottlerin.

9 e have used the PKCdelta-specific inhibitor, rottlerin.

10 jority of beneficial effects associated with rottlerin.

11 e protein kinase Cdelta (PKCdelta) inhibitor rottlerin.

12 y the novel protein kinase C (PKC) inhibitor rottlerin.

13 ffect on the down-regulation of caspase-2 by rottlerin.

14 e protein kinase Cdelta (PKCdelta) inhibitor rottlerin.

15 expression of dominant-negative PKCdelta and rottlerin.

16 on of Src, which was blocked by both BIM and rottlerin.

17 he PKC inhibitors chelerythrine chloride and rottlerin.

18 Hearts were treated with rottlerin 1 mumol/L (CP+R) (n=7) or without rottlerin (C

19 Treatment with rottlerin 1 mumol/L significantly improved CP-induced ca

20 ression of alpha4beta2delta was decreased by rottlerin (10 muM), suggesting a role for PKC-delta.

21 ls, whereas the PKC-delta specific inhibitor rottlerin (3 microM) or knockdown of this isoenzyme with

22 mic administration of the BK channel agonist rottlerin (5 mug/g) during the challenge period reduced

23 Intravenous rottlerin (5 mug/g) reduced AHR within 5 min in the OVA-

24 by the PKC-delta isoform-specific inhibitor rottlerin (50 microm).

25 of conventional and novel PKC isoforms) and rottlerin (a PKCdelta-selective inhibitor) but not Go697

26 AM (an intracellular free calcium chelator), rottlerin (a protein kinase Cdelta inhibitor), and prote

27 Inhibition of PKC-delta by rottlerin (a relatively specific inhibitor of PKC-delta)

28 uced by the selective inhibitor of PKCdelta (rottlerin), a PKCdelta-specific inhibitory peptide (delt

29 (PKC delta-KR) or pretreatment of cells with rottlerin, a chemical PKC delta inhibitor, attenuated TN

30 Rottlerin, a compound reported to be a PKCdelta-selectiv

31 Similarly, rottlerin, a novel class PKC inhibitor, abrogated PA-med

32 Rottlerin, a pharmacologic inhibitor of PKC-delta, suppr

33 hen the expression of p21cip1 was reduced by rottlerin, a PKC delta inhibitor, p27kip1- and BrdU-posi

34 persecretion was significantly attenuated by rottlerin, a PKC delta-selective inhibitor.

35 Rottlerin, a PKC-delta inhibitor, also had no effect, li

36 the protein kinase C (PKC)-delta inhibitor, rottlerin, a PKC-zeta peptide inhibitor, or by overexpre

37 nhibition variably increased apoptosis, with rottlerin, a PKCdelta inhibitor, being most effective an

38 Treatment of cells with rottlerin, a PKCdelta inhibitor, blocked IL-13-induced 1

39 induced dense granule release was blocked by rottlerin, a PKCdelta selective inhibitor.

40 itivity of fMLP-induced O()(2) production to rottlerin, a PKCdelta-selective inhibitor.

41 indolylmaleimide (BIM), a PKC inhibitor, and rottlerin, a PKCdelta-specific inhibitor.

42 harmacologic inhibitors were used, including rottlerin, a protein kinase C delta (PKC delta) inhibito

43 rc caused transformation of these cells, and rottlerin, a protein kinase inhibitor with specificity f

44 Using the inhibitors Go6976 and rottlerin, a role for both conventional and novel PKC is

45 Blocking the PKC delta isoform with either rottlerin, a selective antagonist, or small interference

46 Among the PKC inhibitors used only rottlerin, a selective inhibitor of PKCdelta, markedly i

47 Rottlerin, a selective PKCdelta inhibitor, also inhibite

48 ediated TRAF1 mRNA and promoter stimulation; rottlerin, a selective PKCdelta inhibitor, had no effect

49 e findings is implicated by the finding that rottlerin, a selective PKCtheta inhibitor, blocked FasL

50 hetamine-stimulated dopamine efflux, whereas rottlerin, a specific inhibitor of PKC delta, had no eff

51 Rottlerin, a specific inhibitor of PKC-delta, exerted a

52 27 STAT1 phosphorylation could be blocked by rottlerin, a specific inhibitor of protein kinase C-delt

53 600125, a specific inhibitor of JNK, or with rottlerin, a specific inhibitor of protein kinase Cdelta

54 Rottlerin, a specific PKC-theta inhibitor, diminished p-

55 The PKCdelta inhibitor rottlerin abolished PbTx-2-induced Src activation demons

56 Data suggest that rottlerin affects mitochondrial function independent of

57 e protein kinase Cdelta (PKCdelta) inhibitor rottlerin also blocked the induction of p21(Cip1) protei

58 Rottlerin also caused a significant increase in coronary

59 Rottlerin also inhibited O2 production at similar doses.

60 Rottlerin also inhibited the activation of MAP kinase ki

61 Inhibition of PKCdelta activation by rottlerin also markedly attenuated IL-13-induced Stat3 D

62 Rottlerin also prevented the formation of p-CREB/p300 co

63 Rottlerin also reduced PMA- or human neutrophil elastase

64 Rottlerin, an inhibitor of novel isoforms of PKC, specif

65 Rottlerin, an inhibitor of nPKCdelta, blocked caspase-3

66 Rottlerin, an inhibitor of nPKCdelta, inhibited cAMP-ind

67 Rottlerin, an inhibitor of PKC delta in J774 cells, also

68 Furthermore, rottlerin, an inhibitor of protein kinase Cdelta (PKCdel

69 n the absence or presence of BAPTA/AM, H7 or rottlerin and (2) bile flow.

70 PKC delta, the PKC delta-specific inhibitor rottlerin and a dominant negative PKC delta mutant trans

71 Both rottlerin and a dominant-negative PKCdelta construct inh

72 Interestingly, both rottlerin and EGF induced substantial increases in phosp

73 accumulate in parotid C5 cells treated with rottlerin and etoposide together, suggesting that the ca

74 of freshly isolated parotid acinar cells to rottlerin and FCCP reduced cellular ATP levels and reduc

75 Meanwhile, rottlerin and GF109203X markedly inhibited UVB-induced a

76 diated inhibition of Akt activation, whereas rottlerin and Go6976, inhibitors of PKCdelta and PKCalph

77 n accordance with other results showing that rottlerin and hispidin have the highest efficacy in supp

78 apoptotic factors was demonstrated only when rottlerin and TRAIL were combined, and Bcl-2 overexpress

79 BCR signaling are differentially affected by rottlerin, and by Go6976 or LY294002, respectively.

80 (2) is attenuated by the PKCdelta inhibitor, rottlerin, and by overexpression of the regulatory domai

81 on, an effect that was inhibited by PD98059, rottlerin, and protein kinase Cepsilon (PKCepsilon) inhi

82 Rottlerin at concentrations that block novel and atypica

83 or CGS24592, or inhibition of PKCdelta using Rottlerin at concentrations that inhibit PKCdelta but no

84 Furthermore, rottlerin (at doses that inhibit PKCdelta activity) inhi

85 lta by RNA interference or its inhibition by rottlerin blocked ASMase phosphorylation and membrane ta

86 Rottlerin blocked c-Abl activation, but the c-Abl inhibi

87 Furthermore, rottlerin blocked combined MGO and cisplatin-induced ROS

88 the relatively specific PKC-delta inhibitor rottlerin blocked most of the E(2)-induced Erk activatio

89 Inhibition of PKCdelta activity with rottlerin blocked the increase in SPAK kinase activity.

90 03X, and a selective inhibitor of PKC-delta, Rottlerin, blocked the TPA-induced differentiation of PK

91 phorylation, whereas the nPKCdelta inhibitor rottlerin blocks CREB phosphorylation following BCR cros

92 Finally, we show that rottlerin blocks etoposide-induced apoptosis by inhibiti

93 on and that the PKC delta-specific inhibitor rottlerin blocks thrombin-induced PKD activation, sugges

94 effect was blocked by the PKCdelta inhibitor rottlerin but not by NAC.

95 ara-C was blocked by the PKCdelta inhibitor rottlerin but not by the PKCalpha and -beta inhibitor Go

96 d dense granule secretion was potentiated by rottlerin but was abolished by Go6976, a classical PKC i

97 tion and selective inhibition of PKCdelta by rottlerin, but not by Ca(2+)-chelators.

98 ls with the protein kinase C delta inhibitor rottlerin, but not by classical protein kinase C inhibit

99 hibited by the PKCdelta-selective inhibitor, rottlerin, but not by Go-6976, an inhibitor of conventio

100 Additionally, the protein kinase C inhibitor rottlerin, but not other kinase inhibitors, blocks both

101 or with the protein kinase Cdelta inhibitor rottlerin, but not with broad-based protein kinase C inh

102 sindolylmaleimide I, Ro-32-0432, Go6983, and Rottlerin, by the phorbol 12-myristate 13-acetate-mediat

103 tors (EIPA [5-N-ethyl-N-isoproamiloride] and rottlerin [C(30)H(28)O(8)]) and by cytochalasin D, which

104 Furthermore, down-regulation of caspase-2 by rottlerin can explain its antiapoptotic function during

105 y, inhibitors of MEK (PD98059) and PKCdelta (rottlerin) completely blocked PMA-induced monocytic cell

106 ythrine, or the putative PKCdelta inhibitor, rottlerin, completely inhibited the T-mediated increase

107 Optimal rottlerin concentrations caused a 70-90% inhibition of t

108 rottlerin 1 mumol/L (CP+R) (n=7) or without rottlerin (CP) (n=9), and the BK(Ca++) channel inhibitor

109 Pharmacologic inhibitors Go6976 and rottlerin demonstrate that both conventional and novel p

110 Similarly, calphostin C and rottlerin depressed activation of p44/42 MAPK.

111 Finally, rottlerin did not affect SFLLRN-induced platelet aggrega

112 The inhibition of PKCdelta by rottlerin did not affect the activation of p38 MAPK by a

113 ewise, treatment of cells with the inhibitor rottlerin did not block the stimulatory effect of EtOH o

114 is, whereas the PKCdelta selective inhibitor rottlerin did not.

115 These results demonstrate that rottlerin directly uncouples mitochondrial respiration f

116 A PKCdelta-specific inhibitor, rottlerin, failed to inhibit PMA-induced PLD2 phosphoryl

117 In contrast, rottlerin had no effect on STAT1 phosphorylation induced

118 ivation was attenuated by (i) treatment with rottlerin, (ii) expression of a kinase-inactive PKCdelta

119 Rottlerin increased BK channel activity in human ASM cel

120 binding to aggregates of the small molecule rottlerin increased the deuterium exchange of all 10 rep

121 Rottlerin increased the QO2 of isolated rat liver mitoch

122 We made a novel observation that rottlerin induced down-regulation of caspase-2 but not o

123 In RKO, rottlerin induced the release of cytochrome c, HtrA2/Omi

124 These results suggest that rottlerin induces down-regulation of caspase-2 via PKC d

125 Rottlerin inhibited activation and processing of caspase

126 cleotides or the PKCdelta-specific inhibitor rottlerin inhibited FGF- and NGF-induced, but not EGF-in

127 TRO, RSG, and rottlerin inhibited PDGF-induced expression of p21(Cip1)

128 During treatment with palmitate, rottlerin inhibited phosphorylation of Mcl-1 at Ser(159)

129 minant-negative PKCdelta, PKCdelta-siRNA, or rottlerin inhibits promoter activation.

130 The first total synthesis of rottlerin is described.

131 orm, and the preferential PKCdelta inhibitor rottlerin largely prevented EGF-induced phosphorylation

132 Blockade of this effect via rottlerin may suggest that PKC delta is a downstream sig

133 We tested the hypothesis that rottlerin mitigates deleterious effects associated with

134 However, after 15-min incubation with rottlerin, mitochondrial membrane potential (Delta psi m

135 Neither rottlerin nor FCCP reduced stimuli-dependent PKCdelta ty

136 The effects of rottlerin on mitochondrial QO2 were neither mimicked nor

137 RAIL-induced apoptosis was not influenced by rottlerin or Bcl-2 overexpression in type I (GC(3)/c1) c

138 ent of IMCD3 cells with the TonEBP inhibitor rottlerin or silencing its expression with specific shRN

139 nduced EndoMT and that imatinib mesylate and rottlerin or similar kinase inhibitor molecules may be e

140 on of protein kinase C delta (PKCdelta) with rottlerin or siRNA-mediated knockdown abrogates the oste

141 atment of cells with the PKC-delta inhibitor rottlerin or the expression of a dominant-negative PKC-d

142 aA25E is abrogated by the PKCtheta inhibitor rottlerin or the expression of the kinase-inactive form

143 tment with the PKC delta-selective inhibitor rottlerin or transfection with an antisense PKC delta ol

144 atment with the PKCdelta-selective inhibitor rottlerin or transfection with PKCdelta siRNA attenuated

145 a or pretreatment with a PKCdelta inhibitor (rottlerin) or Src kinase family inhibitor (PP2) partiall

146 Rottlerin, originally identified as a delta-protein kina

147 inhibitors (Go6976, bisindolylmaleimide, and Rottlerin), PKC-alpha, and PKC-delta small interfering (

148 tive protein kinase Cdelta (dn-PKCdelta) and rottlerin (PKCdelta inhibitor) completely suppressed PMA

149 PKCdelta activity with the kinase inhibitor rottlerin, PKCdelta-small interfering RNA, or with PKCde

150 otriene B4, and that process was reversed by rottlerin, presumably through the blockage of PKCdelta-d

151 all interfering RNAs or PKCdelta antibody or rottlerin pretreatment significantly suppressed the phos

152 Specific inhibition of PKCdelta by rottlerin prevented both apoptosis- and activation-induc

153 Specific inhibition of PKCdelta by rottlerin prevented IkappaBalpha degradation and NF-kapp

154 Furthermore, the PKCdelta/PKC inhibitor rottlerin prevented the effects induced by phorbol 12-my

155 of these cells with the PKC-delta inhibitor rottlerin prevented the thrombin-induced phosphorylation

156 Pretreatment of parotid C5 cells with rottlerin prior to the addition of etoposide blocks the

157 omoter deletion constructs demonstrated that rottlerin profoundly reduced COL1A1 transcription and th

158 reviously shown that the PKC delta inhibitor rottlerin protects against cisplatin-induced apoptosis a

159 Eight of these, rottlerin, quercetin, K-252c, bisindolylmaleimide I, bis

160 n the present study, we have investigated if rottlerin regulates caspase-2 activation.

161 the use of an ex vivo lung slice technique, rottlerin relaxed acetylcholine-stimulated murine airway

162 The rottlerin-sensitive element is not PKCdelta, inasmuch as

163 ivated monocytes phosphorylated p47phox in a rottlerin-sensitive manner.

164 These results indicate that the rottlerin-sensitive, Lyn-dependent alternate pathway, an

165 This COL1A1 segment imparted rottlerin sensitivity to a heterologous promoter.

166 itor cycloheximide showed that TRO, RSG, and rottlerin shortened the half-life of p21(Cip1) protein.

167 Previous studies using rottlerin should be evaluated cautiously.

168 r digitorum longus muscles with GF109203X or rottlerin significantly attenuated increases in myocellu

169 Rottlerin significantly improves cardiac performance aft

170 (vi) The specific inhibitor for PKC delta, rottlerin, significantly blocked the inhibition by 5-HT.

171 PKCdelta activity with a specific inhibitor, rottlerin, significantly inhibited caspase-3 activation

172 toma cell proliferation were reduced by BIM, rottlerin, the MEK inhibitor U0126, and PKCdelta and c-S

173 Rottlerin, the PKC delta inhibitor, down-regulated colla

174 ed genes, was potently inhibited by the drug Rottlerin, through a mechanism independent of STAT1 acti

175 ion by calphostin C, bisindolylmaleimide, or rottlerin treatment versus activation by phorbol 12-myri

176 d myocyte contraction, which was restored by rottlerin treatment.

177 Rottlerin was not effective in blocking PKCdelta activit

178 41251, and the PKCdelta-selective inhibitor rottlerin were able to suppress serotonin up-regulation

179 inhibitory effects of imatinib mesylate and rottlerin were mediated by inhibition of phosphorylation

180 Kamalachalcone A and dimeric rottlerin were synthesized in a very practical and econo

181 MG132 reversed caspase-2 down-regulation by rottlerin, whereas calpain inhibitor had no effect.

182 tin C and by the PKCdelta-specific inhibitor rottlerin, whereas Go6976, an inhibitor of conventional

183 region of VCAM-1 was blocked by LY294002 and rottlerin, whereas the inducible binding of GATA-2 to a

184 zation of a lipid soluble toxin, mallotoxin (rottlerin), which potently activates the large conductan

185 ect of PKC activators only slightly, whereas rottlerin, which inhibits PKCdelta preferentially at 5 m

186 stration of hypothalamic PKC-delta inhibitor rottlerin with OAG prevented the ability of OAG to activ

187 These findings suggest that rottlerin, with both anti-inflammatory and ASM relaxatio