ライフサイエンスコーパス: depsipeptide

1 death) for cultured CLL cells (0.038 microM depsipeptide).

2 ed for sensitivity and molecular response to depsipeptide.

3 and in cells treated with the HDAC inhibitor depsipeptide.

4 tive cleavers of the peptidoglycan precursor depsipeptide.

5 y the higher concentrations of 5-Aza-CdR and depsipeptide.

6 reaction to assemble the 28-membered cyclic depsipeptide.

7 following treatment with the HDAC inhibitor depsipeptide.

8 s before and after exposure to bortezomib or depsipeptide.

9 combinatorial libraries of reversible cyclic depsipeptides.

10 sis of a biaryl ether containing macrocyclic depsipeptide 1 was achieved in 6% overall yield.

11 The effect of treatment with FR901228 (depsipeptide), a histone deacetylase inhibitor in phase

12 Depsipeptide, a histone deacetylase inhibitor, has demon

13 Synthesis of the macrolactone depsipeptide aetheramide A was attempted by three differ

14 we investigated the therapeutic efficacy of depsipeptide alone and in combination with daclizumab (h

15 Depsipeptide, an inhibitor of histone deacetylase, acts

16 Treatment with depsipeptide, an inhibitor of histone deacetylase, was u

17 oesterase that produces a 10-membered cyclic depsipeptide and a nonlinear assembly line, resulting in

18 de ligase while an Phe residue predicts both depsipeptide and dipeptide ligase activity, the F261Y mu

19 demonstration that the LmDdl2 does have both depsipeptide and dipeptide ligase activity.

20 ed stages of clinical development, including depsipeptide and MGCD0103, differ from vorinostat in str

21 data support further clinical evaluation of depsipeptide and other HDACIs in patients with primary a

22 r approach involving synthesis of the cyclic depsipeptide and side chain fragments followed by a late

23 that p21(WAF1) induction by HDAC inhibitors (depsipeptide and trichostatin A) is defective in Ataxia

24 at inhibitors of histone deacetylase (HDAC), depsipeptide and trichostatin A, induce apoptotic cell d

25 nd to demonstrate an interaction between the depsipeptide and tubulin was Hummel-Dreyer equilibrium c

26 n-sensitive cells was replaced by UDP-MurNAc-depsipeptide and UDP-MurNAc-tetrapeptide.

27 e solid-phase synthesis of individual cyclic depsipeptides and combinatorial libraries of these compo

28 tyrocidine NRPS can catalyze cyclization of depsipeptides and other backbone-substituted peptides an

29 he combination of inhibitors of HDACs (i.e., depsipeptide) and DNA methyltransferases (DNMT; i.e., de

30 Telomycin (TEM) is a cyclic depsipeptide antibiotic active against Gram-positive bac

31 Lysobactin, a depsipeptide antibiotic has displayed very strong antiba

32 AP) is the functional cellular target of the depsipeptide antibiotic salinamide A (Sal), and we repor

33 namide A belongs to a rare class of bicyclic depsipeptide antibiotics in which the installation of a

34 est that the binding site(s) for peptide and depsipeptide antimitotic drugs may consist of a series o

35 ide bond exchange and ester bond hydrolysis, depsipeptides are enriched with amino acids over time.

36 ted by screening a model library, the cyclic depsipeptides are linearized and released from the solid

37 The resulting macrocyclic depsipeptides are model compounds for natural products a

38 tone deacetylase inhibitors (HDIs), SAHA and Depsipeptide, are FDA approved for single-agent treatmen

39 , there was little turbidity change with the depsipeptide as opposed to the peptide.

40 Treatment with depsipeptide, as well as other histone deacetylase inhib

41 Six new depsipeptides belonging to two different structural clas

42 d in a specific alpha/alpha-pseudodipeptide, depsipeptide (Boc-Leu-Lac-OEt).

43 kinetics of turnover of a beta-lactam and a depsipeptide by a beta-lactamase.

44 onding residue in the closely related cyclic depsipeptides callipeltins A and B should also be consid

45 olysis and aminolysis of a series of acyclic depsipeptides, catalyzed by the class C beta-lactamase o

46 two biosynthetic precursors into the growing depsipeptide chain that swings between T1 and T2a/T2b wi

47 At the MTD (17 mg/m2), the median depsipeptide clearance was 6.8 L/h/m(2) with an area und

48 ls when pretreated with either bortezomib or depsipeptide compared with untreated tumors.

49 s 6.8 L/h/m(2) with an area under the plasma depsipeptide concentration-time curve from 0 to infinity

50 (LC(50)) at 4 hours, 24 hours, and 4 days at depsipeptide concentrations of 0.038, 0.024, and 0.015 m

51 In a phase I trial of depsipeptide conducted at the National Cancer Institute,

52 eptides, and koshikamides F-H are 17-residue depsipeptides containing a 10-residue macrolactone.

53 ve been reported to comprise a common cyclic depsipeptide core attached to 3-hydroxy,omega-guanidino

54 on for formation of the strained 16-membered depsipeptide core followed by an olefin cross-metathesis

55 These assays revealed that the native cyclic depsipeptide core is an essential structural requirement

56 led, and cyclized to provide the 49-membered depsipeptide core of the aglycon.

57 led, and cyclized to provide the 49-membered depsipeptide core of the aglycon.

58 The antimitotic depsipeptide cryptophycin 1 (CP1) was compared to the an

59 ctural analog of dolastatin 15, and with the depsipeptide cryptophycin 1.

60 r, a case study using the IgG binding cyclic depsipeptide cyclo[(Nalpha-Ac)-S(A)-RWHYFK-Lact-E] is pr

61 y to activate D-lactate (D-Lac) and make the depsipeptide D-Ala-D-Lac as well as D-Ala-D-Ala.

62 Mutants Y216F and S150A have gained depsipeptide (D-Ala-D-Lac, D-Ala-D-hydroxybutyrate) liga

63 istone deacetylase inhibitors, one of which, depsipeptide (DEP), is currently undergoing phase II cli

64 The antineoplastic cyclic depsipeptide didemnin B (DB) inhibits protein synthesis

65 the binding of the antiproliferative cyclic depsipeptide didemnin B to PPT1.

66 the other hand, the V/K transition state for depsipeptide does not seem to involve covalent chemistry

67 The antimitotic depsipeptide dolastatin 15 was radiolabeled with tritium

68 ials, is a peptide analog of the antimitotic depsipeptide dolastatin 15.

69 icrotubule-targeted derivative of the marine depsipeptide dolastatin-15, is currently undergoing clin

70 t induce actin assembly (all are peptides or depsipeptides), dolastatin 11 may interact with actin po

71 The cytotoxic, cyclic depsipeptide (-)-doliculide was originally isolated by I

72 We conclude that depsipeptide effectively inhibits HDAC in vivo in patien

73 HDAC inhibitors (trichostatin A [TSA] and depsipeptide) either alone or in combination with 5-AzaC

74 orporation of the subunit bearing the labile depsipeptide ester and a final stage Asn(1) side chain i

75 orporation of the subunit bearing the labile depsipeptide ester and a final stage Asn(1) side-chain i

76 This highly methylated cyclized depsipeptide exhibited an unprecedented selectivity prof

77 Expression of apoptotic proteins after depsipeptide exposure (0.015 micromol/L) included no cha

78 d by sequential 5-aza 2'-deoxycytidine (DAC)/depsipeptide FK228 (DP) exposure in order to identify tr

79 following 5-aza-2'-deoxycytidine (5-azadC), Depsipeptide FK228 (DP), or sequential 5-azadC/DP exposu

80 The cyclic depsipeptide FK228 is the only natural product histone d

81 Sequential 5-aza-2'deoxycytidine/depsipeptide FK228 treatment markedly induced BORIS expr

82 ith the histone deacetylase (HDAC) inhibitor depsipeptide (FK228) in chronic lymphocytic leukemia (CL

83 novel histone deacetylase inhibitor (HDACI) depsipeptide (FK228) induced P-gp expression and prevent

84 Depsipeptide (FK228) is a novel histone deacetylase inhi

85 omib, and the histone deacetylase inhibitor, depsipeptide (FK228), up-regulate tumor death receptors.

86 hibition of CFU-GM; 57% inhibition BFU-E) of depsipeptide for 4 hours, followed by a 14-day incubatio

87 initial studies, the synthesis incorporated depsipeptide formation, introduction of chromophores, an

88 s with three ligands that mimic peptides and depsipeptides found in vancomycin-sensitive and vancomyc

89 Here we report that the plant-derived depsipeptide FR900359 (FR) is ideally suited to this tas

90 Depsipeptide (FR901228) is a novel agent entering clinic

91 Depsipeptide, FR901228, has demonstrated potent in vitro

92 subsequent incorporation into the kutzneride depsipeptide frameworks.

93 (Cip1) promoter vectors, we demonstrate that depsipeptide functions on Sp1-binding sites to induce p2

94 unreported piperazic acid-containing cyclic depsipeptides, gerumycins A-C.

95 Either depsipeptide, given at 0.5 mg/kg every other day for 2 w

96 Depsipeptide had marked selective cytotoxicity when comp

97 in peptidoglycan intermediates in which the depsipeptide has much lower affinity than the dipeptide

98 These data demonstrate that depsipeptide has significant selective in vitro activity

99 nfortunately, the development of macrocyclic depsipeptides has been hampered in part because of devel

100 Four new depsipeptides have been isolated from the marine cyanoba

101 t small molecule HDACi reported, macrocyclic depsipeptides have the most complex recognition cap-grou

102 ely related bis-thiazoline containing cyclic depsipeptides, have been isolated from extracts of the m

103 phycins, naturally occurring cytotoxic cyclo-depsipeptides, have been modified by total synthesis to

104 These studies confirm the activity of depsipeptide in a T-cell lymphoma model and suggest a ge

105 ide via an ester bond, resulting in a cyclic depsipeptide in contrast to the linear peptide chain of

106 However, cells selected for resistance to depsipeptide in the presence of a Pgp inhibitor had a Pg

107 Treatment with depsipeptide increased expression of the interleukin-2 (

108 the histone deacetylase inhibitor FR901228 (depsipeptide) increased CAR and alpha(v) integrin RNA le

109 Results showed that depsipeptide induced a dose-dependent acetylation of his

110 Depsipeptide induced p21(Cip1) expression was reconstitu

111 Depsipeptide-induced apoptosis is caspase dependent, sel

112 inhibitor z-VAD-fmk significantly inhibited depsipeptide-induced apoptosis, enabling detection of ce

113 We demonstrate that in vitro depsipeptide induces histone H3 and H4 acetylation and h

114 get when cell wall biosynthesis proceeds via depsipeptide intermediates rather than the usual polypep

115 s strongly support the early introduction of depsipeptide into clinical trials for patients with CLL.

116 tients with AML were treated with 13 mg/m(2) depsipeptide intravenously days 1, 8, and 15 of therapy.

117 Depsipeptide is in clinical trials for chronic lymphocyt

118 Depsipeptide is well tolerated in children with recurren

119 Sansalvamide A, a cyclic depsipeptide isolated from a marine fungus of the genus

120 tal synthesis of FR-901375, a novel bicyclic depsipeptide isolated from the fermentation broth of Pse

121 he crocapeptins are described here as cyclic depsipeptides, isolated from cultures of the myxobacteri

122 most similar to those of the sponge-derived depsipeptide jasplakinolide, but dolastatin 11 was about

123 cts have also been reported with a series of depsipeptides known as chondramides.

124 The cytotoxic depsipeptide kulokekahilide-1, which contains two unusua

125 4 showed 30-fold higher activity against the depsipeptide Lac-ester substrate than against the analog

126 to present different structural examples for depsipeptide libraries and demonstrate the process of se

127 xplain the weaker affinity of vancomycin for depsipeptide ligands.

128 he E. coli DdlB leads to gain of D-Ala-D-Lac depsipeptide ligase activity in that enzyme.

129 This depsipeptide ligase activity of VanA is its crucial cata

130 ed substantial defects in both dipeptide and depsipeptide ligase activity, suggesting a role in maint

131 Comparisons are made to the depsipeptide ligase from the vancomycin-resistance casca

132 cin-resistant enterococci, a D-Ala-D-lactate depsipeptide ligase, has the ability to recognize and ac

133 th D-Ala-D-Ala dipeptide and D-Ala-D-lactate depsipeptide ligation.

134 The synthesis of novel cyclic depsipeptide mimics by means of an organocatalytic conju

135 convergent preparation of analogues bearing depsipeptide modifications.

136 Cyclic tetrapeptide and depsipeptide natural products have proven useful as biol

137 dues (fifth amino acid residue in the cyclic depsipeptide of AMD) could bind to DNA as strongly as th

138 ine cyanobacteria-derived lariat-type cyclic depsipeptide of which the macrocyclic core possesses mod

139 pha-hydroxy acids and alpha-amino acids form depsipeptides-oligomers with a combination of ester and

140 mia-bearing mice, compared with those in the depsipeptide or daclizumab alone groups (P < .001).

141 Romidepsin (depsipeptide or FK228) is a histone deacetylase inhibito

142 PURPOSE Romidepsin (depsipeptide or FK228) is a member of a new class of ant

143 leased from the IL-3 promoter by exposure to depsipeptide or stabilized on the promoter by decitabine

144 lines with the histone deacetylase inhibitor depsipeptide or the DNA methyltransferase inhibitor 5-az

145 ith either the histone deacetylase inhibitor depsipeptide or the MEK inhibitor UO126.

146 The successful synthesis of dolastatin 11, a depsipeptide originally isolated from the mollusk Dolabe

147 Cells selected for resistance to depsipeptide overexpressed the multidrug resistance pump

148 with higher concentrations of 5-Aza-CdR and depsipeptide, p16(INK4a) expression was decreased togeth

149 roxybutyrate) ligase activity with dipeptide/depsipeptide partition ratios that mimic the pH behavior

150 ase inhibitors (HDACi) reported, macrocyclic depsipeptides possess the most complex cap groups and ha

151 Cyclic depsipeptides related to sansalvamide A represent a pote

152 6-hydroxy-2-piperidone acid (Ahp)-containing depsipeptides reported with the rare Ahppa unit.

153 The depsipeptide represented by structure 5 was readily gene

154 reactions to afford N-alkylated peptides and depsipeptides, respectively, followed by conversion of t

155 e thioesterase in generating the 16-membered depsipeptide ring of this important natural product syst

156 ncorporating major structural changes in the depsipeptide ring were synthesized.

157 The cyclic depsipeptide sansalvamide A was found to inhibit topoiso

158 us giving access to amido-, glyco-, and lipo-depsipeptide scaffolds featuring natural product-like st

159 Future studies with depsipeptide should examine alternative administration s

160 Depsipeptide significantly reduced the recruitment of Nu

161 the histone deacetylase inhibitors (HDACIs), depsipeptide, sodium butyrate (NaB) and trichostatin A (

162 Using the largazole macrocyclic depsipeptide structure as a starting point for developin

163 oped and reported here will allow the cyclic depsipeptide structure to be tuned for optimum selectivi

164 cyclic peptide corresponding to the proposed depsipeptide structure, to make the ligand stable to the

165 monium-selective ionophore based on a cyclic depsipeptide structure.

166 at affect these targets, such as bortezomib, depsipeptide, suberoylanilide hydroxamic acid, and a hos

167 Four HDAI (depsipeptide, suberoylanilide hydroxamic acid, MS-275, a

168 lactamase-catalyzed hydrolysis of an acyclic depsipeptide substrate bearing a third-generation cephal

169 A depsipeptide substrate is used that contains a europium-

170 The synthesis of the depsipeptide substrate typically takes 2-3 d.

171 netic parameters V/K and V for turnover of a depsipeptide substrate, m-[[(phenylacetyl)glycyl]-oxy]be

172 This protocol describes the use of depsipeptide substrates (containing an ester linkage) wi

173 The depsipeptide substrates contained a constant acyl group,

174 In contrast, switching to depsipeptide substrates effectively renders the reaction

175 Herein we describe the synthesis of depsipeptide substrates that contain an ester linkage be

176 E15Q has negligible depsipeptide synthetase activity but now uniquely activa

177 es of two new, naturally occurring cytotoxic depsipeptides, tamandarins A and B (1 and 2), are presen

178 inimum effective pharmacologic dose study of depsipeptide, targeting an in vivo dose at which acetyla

179 A new sulfated cyclic depsipeptide, termed mutremdamide A, and six new highly

180 Seven new depsipeptides, termed largamides A-G (1-7), and one new

181 smaller versions of dentigerumycin, a cyclic depsipeptide that selectively inhibits a common fungal p

182 Callipeltin A is a novel cyclic depsipeptide that selectively inhibits the cardiac sodiu

183 ecticidal, anti-viral, and phytotoxic cyclic depsipeptides that are also studied for their toxicity t

184 Celebesides are unusual cyclic depsipeptides that comprise a polyketide moiety and five

185 Similarly to the natural depsipeptides, the synthetic oligolactam analogues show

186 inhibited by addition of the HDAC inhibitor depsipeptide to the culture medium for different exposur

187 reduced p21(Cip1) expression in response to depsipeptide treatment.

188 screte collections of oligomeric macrocyclic depsipeptides using an oligomerization/macrocyclization

189 o tubulin (apparent Ki, 3.9 microM); and the depsipeptide was a competitive inhibitor of the binding

190 Depsipeptide was administered as a 4-hour infusion weekl

191 e waters, but the mechanism of action of the depsipeptide was not known.

192 ysis by D-phenylalanine of a cognate pair of depsipeptides was also studied.

193 ituents), cyclic N-methylated peptides and a depsipeptide were produced in good yields using conditio

194 While Beauveria secreted these cyclic depsipeptides when encountering live insect tissues, Met

195 ces sp. Svetamycins A-D, F, and G are cyclic depsipeptides, whereas svetamycin E is a linear analogue

196 ide A (1) is a new, potent antiproliferative depsipeptide which was isolated from a marine Leptolyngb

197 Several naturally occurring peptides and depsipeptides which include the cryptophycins, dolastati

198 Combination of depsipeptide with daclizumab enhanced the antitumor effe

199 y improved therapeutic efficacy by combining depsipeptide with daclizumab supports a clinical trial o

200 ophycins (Crp) are a group of cyanobacterial depsipeptides with activity against drug-resistant tumor

201 d B were the most cytotoxic among these four depsipeptides with an LC(50) of approximately 0.4 muM to

202 The cyclic depsipeptides YM-254890 and FR900359 are the only known

203 erivatives of the naturally occurring cyclic depsipeptide zygosporamide.