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 dipeptide with the corresponding d-Ala-d-Lac depsipeptide.

7 reaction to assemble the 28-membered cyclic depsipeptide.

8 following treatment with the HDAC inhibitor depsipeptide.

9 s before and after exposure to bortezomib or depsipeptide.

10 ucts closely resembling antimicrobial cyclic depsipeptides.

11 solutions to form nucleobase-functionalized depsipeptides.

12 combinatorial libraries of reversible cyclic depsipeptides.

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

14 onical polymers and macrocyclic peptides and depsipeptides(1-3).

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

16 Depsipeptide, a histone deacetylase inhibitor, has demon

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

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

19 Depsipeptide, an inhibitor of histone deacetylase, acts

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

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

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

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

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

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

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

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

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

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

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

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

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

33 Here we show that cationic proto-peptides (depsipeptides and polyesters), either produced as mixtur

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

35 d at the ability of amino acids, peptides, a depsipeptide, and proteins to partition into a non-polar

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

37 Lysobactin, a depsipeptide antibiotic has displayed very strong antiba

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

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

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

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

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

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

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

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

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

47 hydrophobic hydroxy acids and indicate that depsipeptide assemblies containing alpha hydroxy acid ba

48 Six new depsipeptides belonging to two different structural clas

49 ucture to dock small-molecule drugs into the depsipeptide binding site of Galphaq.

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

51 In turn, RNA increases the lifetime of a depsipeptide by >30-fold.

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

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

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

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

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

57 Cyclic oligomeric depsipeptides (COD) are a structural class within natura

58 pected 18- and 30-membered cyclic oligomeric depsipeptides (CODs).

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

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

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

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

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

64 Depsipeptides, containing both ester and amide linkages,

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

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

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

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

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

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

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

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

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

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

75 e vancomycin family of glycopeptides and the depsipeptide daptomycin.

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

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

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

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

80 The antimitotic depsipeptide dolastatin 15 was radiolabeled with tritium

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

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

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

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

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

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

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

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

89 This highly methylated cyclized depsipeptide exhibited an unprecedented selectivity prof

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

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

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

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

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

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

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

97 Depsipeptide (FK228) is a novel histone deacetylase inhi

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

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

100 However, it is unknown whether depsipeptides form assemblies in an aqueous environment

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

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

103 Here, we report that the cyclic depsipeptide FR900359 (FR) directly interacted with GTPa

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

105 ctive pigment violacein and bioactive cyclic depsipeptide FR900359.

106 Previously discovered bacterial depsipeptides (FR900359 and YM-254890) bind directly to

107 Depsipeptide (FR901228) is a novel agent entering clinic

108 Depsipeptide, FR901228, has demonstrated potent in vitro

109 subsequent incorporation into the kutzneride depsipeptide frameworks.

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

111 inhibitors with better bioavailability than depsipeptide Galphaq inhibitors.

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

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

114 Depsipeptide had marked selective cytotoxicity when comp

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

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

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

118 Four new depsipeptides have been isolated from the marine cyanoba

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

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

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

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

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

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

125 selectivity results in predominantly linear depsipeptides in which the amino acids are alpha-amine-l

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

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

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

129 Depsipeptide induced p21(Cip1) expression was reconstitu

130 Depsipeptide-induced apoptosis is caspase dependent, sel

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

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

133 ty of polymyxin B and Leu(10)-teixobactin, a depsipeptide inhibitor of cell wall biosynthesis.

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

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

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

137 Depsipeptide is in clinical trials for chronic lymphocyt

138 Depsipeptide is well tolerated in children with recurren

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

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

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

142 designed from the F-actin-stabilizing marine depsipeptide jasplakinolide by functionalizing them with

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

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

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

146 4 showed 30-fold higher activity against the depsipeptide Lac-ester substrate than against the analog

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

148 xplain the weaker affinity of vancomycin for depsipeptide ligands.

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

150 This depsipeptide ligase activity of VanA is its crucial cata

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

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

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

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

155 l-based synthesis of non-natural peptide and depsipeptide macrocycles is an outstanding challenge.

156 encoded synthesis of 12 diverse non-natural depsipeptide macrocycles, which contain two non-canonica

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

158 convergent preparation of analogues bearing depsipeptide modifications.

159 ed, uncovering a paradox in which the MCO of depsipeptide monomers can produce "impossible" ring size

160 Although the cyclooligomeric depsipeptide natural product (-)-verticilide had no effe

161 y of analogues of the cyanobacterium-derived depsipeptide natural product gallinamide A were designed

162 Teixobactin, a macrocyclic depsipeptide natural product, isolated from uncultured b

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

164 and ecumicin are structurally related cyclic depsipeptide natural products that possess activity agai

165 e report a new class of nucleic acid analog, depsipeptide nucleic acid (DepsiPNA), which displays sev

166 The monomers of depsipeptide nucleic acids can form under plausibly preb

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

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

169 To test this hypothesis, we generated depsipeptides, oligomers composed of ester bonds and pep

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

171 dual modulatory potential of cyclooligomeric depsipeptides on ryanodine receptor 2, with ent-verticil

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

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

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

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

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

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

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

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

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

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

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

183 Cyclic depsipeptides related to sansalvamide A represent a pote

184 6-hydroxy-2-piperidone acid (Ahp)-containing depsipeptides reported with the rare Ahppa unit.

185 Cyclic oligomeric depsipeptides represent a distinct structural class of n

186 The depsipeptide represented by structure 5 was readily gene

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

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

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

190 The cyclic depsipeptide sansalvamide A was found to inhibit topoiso

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

192 Future studies with depsipeptide should examine alternative administration s

193 Depsipeptide significantly reduced the recruitment of Nu

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

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

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

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

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

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

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

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

202 A depsipeptide substrate is used that contains a europium-

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

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

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

206 The depsipeptide substrates contained a constant acyl group,

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

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

209 We demonstrate that depsipeptides ("switch peptides") can undergo enzyme-tri

210 E15Q has negligible depsipeptide synthetase activity but now uniquely activa

211 ur results demonstrate assembly formation in depsipeptide systems containing hydrophobic hydroxy acid

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

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

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

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

216 Novo29 is an eight-residue depsipeptide that contains the noncanonical amino acid h

217 ilide (ent-1), a 24-membered cyclooligomeric depsipeptide that is the enantiomeric form of a natural

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

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

220 Here we describe KZR-8445, a cyclic depsipeptide that targets the Sec61 translocon and selec

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

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

223 In this paper, we investigate cationic depsipeptides that form under mild dry-down reactions.

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

225 NRPSs involved in biosynthesis of anticancer depsipeptides thiocoraline and echinomycin, and by mutan

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

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

228 readily than beta backbones, we synthesized depsipeptides using a matrix of eight alpha- and beta-hy

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

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

231 Depsipeptide was administered as a 4-hour infusion weekl

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

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

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

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

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

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

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

239 elucidation revealed cinnapeptin as a cyclic depsipeptide with an unusual 2-methyl-cinnamoyl group.

240 Combination of depsipeptide with daclizumab enhanced the antitumor effe

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

242 Kahalalide F is a cyclic depsipeptide with notable anticancer properties, initial

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

244 To test the hypothesis that depsipeptides with alpha backbones will form assemblies

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

246 This is the first report of cyclic depsipeptides with antifungal activity isolated from fro

247 y acid-containing linear peptides and cyclic depsipeptides with high efficiency.

248 Microviridins are cyanobacterial tricyclic depsipeptides with unique ring architectures and functio

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

250 erivatives of the naturally occurring cyclic depsipeptide zygosporamide.