PMID-sentid Pub_year Sent_text compound_name comp_offset prot_official_name organism prot_offset 19354233-3 2009 Initial cycloamidation led to complete epimerization at the C-11 stereocenter due to unique steric constraints in the 12-membered depsipeptide ring. Depsipeptides 130-142 RNA polymerase III subunit K Homo sapiens 60-64 18948574-6 2009 Either depsipeptide, given at 0.5 mg/kg every other day for 2 weeks, or daclizumab, given at 100 microg weekly for 4 weeks, inhibited tumor growth as monitored by serum levels of soluble IL-2R-alpha (sIL-2R-alpha) and soluble beta2-microglobulin (beta2mu) (P < .001), and prolonged survival of the leukemia-bearing mice (P < .001) compared with the control group. Depsipeptides 7-19 interleukin 2 receptor, alpha chain Mus musculus 187-198 19308286-0 2009 Acetylation of FoxO1 activates Bim expression to induce apoptosis in response to histone deacetylase inhibitor depsipeptide treatment. Depsipeptides 111-123 forkhead box O1 Homo sapiens 15-20 19308286-0 2009 Acetylation of FoxO1 activates Bim expression to induce apoptosis in response to histone deacetylase inhibitor depsipeptide treatment. Depsipeptides 111-123 BCL2 like 11 Homo sapiens 31-34 19308286-0 2009 Acetylation of FoxO1 activates Bim expression to induce apoptosis in response to histone deacetylase inhibitor depsipeptide treatment. Depsipeptides 111-123 histone deacetylase 9 Homo sapiens 81-100 19308286-3 2009 In this study, depsipeptide, a novel HDAC inhibitor, was shown to be able to induce significant apoptotic cell death in human lung cancer cells. Depsipeptides 15-27 histone deacetylase 9 Homo sapiens 37-41 19308286-4 2009 Further study showed that Bim, a BH3-only proapoptotic protein, was significantly upregulated by depsipeptide in cancer cells, and Bim"s function in depsipeptide-induced apoptosis was confirmed by knockdown of Bim with RNAi. Depsipeptides 97-109 BCL2 like 11 Homo sapiens 26-29 19308286-5 2009 In addition, we found that depsipeptide-induced expression of Bim was directly dependent on acetylation of forkhead box class O1 (FoxO1) that is catalyzed by cyclic adenosine monophosphate-responsive element-binding protein-binding protein, and indirectly induced by a decreased four-and-a-half LIM-domain protein 2. Depsipeptides 27-39 BCL2 like 11 Homo sapiens 62-65 19308286-5 2009 In addition, we found that depsipeptide-induced expression of Bim was directly dependent on acetylation of forkhead box class O1 (FoxO1) that is catalyzed by cyclic adenosine monophosphate-responsive element-binding protein-binding protein, and indirectly induced by a decreased four-and-a-half LIM-domain protein 2. Depsipeptides 27-39 forkhead box O1 Homo sapiens 130-135 19308286-6 2009 Moreover, our results demonstrated that FoxO1 acetylation is required for the depsipeptide-induced activation of Bim and apoptosis, using transfection with a plasmid containing FoxO1 mutated at lysine sites and a luciferase reporter assay. Depsipeptides 78-90 forkhead box O1 Homo sapiens 40-45 19308286-6 2009 Moreover, our results demonstrated that FoxO1 acetylation is required for the depsipeptide-induced activation of Bim and apoptosis, using transfection with a plasmid containing FoxO1 mutated at lysine sites and a luciferase reporter assay. Depsipeptides 78-90 BCL2 like 11 Homo sapiens 113-116 19308286-6 2009 Moreover, our results demonstrated that FoxO1 acetylation is required for the depsipeptide-induced activation of Bim and apoptosis, using transfection with a plasmid containing FoxO1 mutated at lysine sites and a luciferase reporter assay. Depsipeptides 78-90 forkhead box O1 Homo sapiens 177-182 18677478-6 2009 Induction of NY-ESO-1 expression on tumor targets using the demethylating agent 5-aza-2"-deoxycytidine (alone or in combination with the histone deacetylase inhibitor depsipeptide) resulted in enhanced interferon-gamma secretion by the TCR-transduced PBL on culture with treated targets. Depsipeptides 167-179 cancer/testis antigen 1A Homo sapiens 13-21 18677478-6 2009 Induction of NY-ESO-1 expression on tumor targets using the demethylating agent 5-aza-2"-deoxycytidine (alone or in combination with the histone deacetylase inhibitor depsipeptide) resulted in enhanced interferon-gamma secretion by the TCR-transduced PBL on culture with treated targets. Depsipeptides 167-179 interferon gamma Homo sapiens 202-218 18677478-6 2009 Induction of NY-ESO-1 expression on tumor targets using the demethylating agent 5-aza-2"-deoxycytidine (alone or in combination with the histone deacetylase inhibitor depsipeptide) resulted in enhanced interferon-gamma secretion by the TCR-transduced PBL on culture with treated targets. Depsipeptides 167-179 T cell receptor beta variable 20/OR9-2 (non-functional) Homo sapiens 236-239 18948574-7 2009 Combination of depsipeptide with daclizumab enhanced the antitumor effect, as shown by both sIL-2R-alpha and beta2mu levels and survival of the leukemia-bearing mice, compared with those in the depsipeptide or daclizumab alone groups (P < .001). Depsipeptides 15-27 beta-2 microglobulin Mus musculus 109-116 19175352-3 2009 A83586C antitumor cyclodepsipeptides also inhibit E2F-mediated transcription by downregulating E2F1 expression and inducing dephosphorylation of the oncogenic hyperphosphorylated retinoblastoma protein (pRb). Depsipeptides 18-36 E2F transcription factor 1 Homo sapiens 95-99 19175352-3 2009 A83586C antitumor cyclodepsipeptides also inhibit E2F-mediated transcription by downregulating E2F1 expression and inducing dephosphorylation of the oncogenic hyperphosphorylated retinoblastoma protein (pRb). Depsipeptides 18-36 RB transcriptional corepressor 1 Homo sapiens 203-206 19200053-0 2009 The changing face of HDAC inhibitor depsipeptide. Depsipeptides 36-48 histone deacetylase 9 Homo sapiens 21-25 19200053-2 2009 A novel and potent HDAC inhibitor, depsipeptide, also known as FK228 or FR901228, is highly efficient in inhibiting the activity of HDACs even at nanomolar concentrations. Depsipeptides 35-47 histone deacetylase 9 Homo sapiens 19-23 19014694-5 2008 We observed that the HDAC inhibitors, MS-275, trichostatin-A, phenylbutyrate, LAQ824 and depsipeptide, enhanced the antineoplastic action of 5AZA-CdR on EWS cells. Depsipeptides 89-101 histone deacetylase 9 Homo sapiens 21-25 18821579-2 2009 Here, we show that the histone deacetylase (HDAC) inhibitor FK228 (depsipeptide) has an antitumor effect on MRT cells both in vitro and in vivo. Depsipeptides 67-79 histone deacetylase 9 Homo sapiens 23-42 18821579-2 2009 Here, we show that the histone deacetylase (HDAC) inhibitor FK228 (depsipeptide) has an antitumor effect on MRT cells both in vitro and in vivo. Depsipeptides 67-79 histone deacetylase 9 Homo sapiens 44-48 17200366-10 2007 Moreover, long-term treatment with a low dose of depsipeptide resulted in the induction of differentiation into hypertrophic phenotype, as shown by the increment of the alpha1 chain of type X collagen (COL10A1) expression in chondrosarcoma cells. Depsipeptides 49-61 collagen, type X, alpha 1 Mus musculus 202-209 18605682-1 2008 The conformational study on N-acetyl- N"-methylamide of l-lactic acid (Ac-Lac-NHMe, the Lac dipeptide) is carried out using ab initio HF and density functional methods with the self-consistent reaction field method to explore its backbone conformational preferences and cis-trans isomerization for the depsipeptide with an ester bond in the gas phase and in solution. Depsipeptides 302-314 lactase Homo sapiens 74-77 18605682-1 2008 The conformational study on N-acetyl- N"-methylamide of l-lactic acid (Ac-Lac-NHMe, the Lac dipeptide) is carried out using ab initio HF and density functional methods with the self-consistent reaction field method to explore its backbone conformational preferences and cis-trans isomerization for the depsipeptide with an ester bond in the gas phase and in solution. Depsipeptides 302-314 lactase Homo sapiens 88-91 18332107-2 2008 Here, we report that an HDAC inhibitor, depsipeptide, exhibited significant demethylating activity on the promoters of several genes, including p16, SALL3, and GATA4 in human lung cancer cell lines H719 and H23, colon cancer cell line HT-29, and pancreatic cancer cell line PANC1. Depsipeptides 40-52 cyclin dependent kinase inhibitor 2A Homo sapiens 144-147 18332107-2 2008 Here, we report that an HDAC inhibitor, depsipeptide, exhibited significant demethylating activity on the promoters of several genes, including p16, SALL3, and GATA4 in human lung cancer cell lines H719 and H23, colon cancer cell line HT-29, and pancreatic cancer cell line PANC1. Depsipeptides 40-52 spalt like transcription factor 3 Homo sapiens 149-154 18332107-2 2008 Here, we report that an HDAC inhibitor, depsipeptide, exhibited significant demethylating activity on the promoters of several genes, including p16, SALL3, and GATA4 in human lung cancer cell lines H719 and H23, colon cancer cell line HT-29, and pancreatic cancer cell line PANC1. Depsipeptides 40-52 GATA binding protein 4 Homo sapiens 160-165 18332107-3 2008 Although expression of DNA methyltransferase 1 (DNMT1) was not affected by depsipeptide, a decrease in binding of DNMT1 to the promoter of these genes played a dominant role in depsipeptide-induced demethylation and reactivation. Depsipeptides 177-189 DNA methyltransferase 1 Homo sapiens 23-46 18332107-3 2008 Although expression of DNA methyltransferase 1 (DNMT1) was not affected by depsipeptide, a decrease in binding of DNMT1 to the promoter of these genes played a dominant role in depsipeptide-induced demethylation and reactivation. Depsipeptides 177-189 DNA methyltransferase 1 Homo sapiens 114-119 18332107-4 2008 Depsipeptide also suppressed expression of histone methyltransferases G9A and SUV39H1, which in turn resulted in a decrease of di- and trimethylated H3K9 around these genes" promoter. Depsipeptides 0-12 SUV39H1 histone lysine methyltransferase Homo sapiens 78-85 18332107-5 2008 Furthermore, both loading of heterochromatin-associated protein 1 (HP1alpha and HP1beta) to methylated H3K9 and binding of DNMT1 to these genes" promoter were significantly reduced in depsipeptide-treated cells. Depsipeptides 184-196 chromobox 5 Homo sapiens 67-75 18332107-5 2008 Furthermore, both loading of heterochromatin-associated protein 1 (HP1alpha and HP1beta) to methylated H3K9 and binding of DNMT1 to these genes" promoter were significantly reduced in depsipeptide-treated cells. Depsipeptides 184-196 chromobox 1 Homo sapiens 80-87 18332107-5 2008 Furthermore, both loading of heterochromatin-associated protein 1 (HP1alpha and HP1beta) to methylated H3K9 and binding of DNMT1 to these genes" promoter were significantly reduced in depsipeptide-treated cells. Depsipeptides 184-196 DNA methyltransferase 1 Homo sapiens 123-128 18067154-0 2008 Conformational change from antiparallel beta-sheet to alpha-helix in a series of depsipeptide, -(Leu-Leu-Lac)(n)-: syntheses, spectroscopic studies, and crystal structures of Boc-Leu-Lac-OEt and Boc-(Leu-Leu-Lac)(n)-OEt (n = 1, 2). Depsipeptides 81-93 lactase Homo sapiens 105-108 18067154-0 2008 Conformational change from antiparallel beta-sheet to alpha-helix in a series of depsipeptide, -(Leu-Leu-Lac)(n)-: syntheses, spectroscopic studies, and crystal structures of Boc-Leu-Lac-OEt and Boc-(Leu-Leu-Lac)(n)-OEt (n = 1, 2). Depsipeptides 81-93 lactase Homo sapiens 183-186 18067154-0 2008 Conformational change from antiparallel beta-sheet to alpha-helix in a series of depsipeptide, -(Leu-Leu-Lac)(n)-: syntheses, spectroscopic studies, and crystal structures of Boc-Leu-Lac-OEt and Boc-(Leu-Leu-Lac)(n)-OEt (n = 1, 2). Depsipeptides 81-93 lactase Homo sapiens 183-186 18234154-6 2008 Additionally, 1 microM completely reversed Pgp-mediated resistance to vinblastine, paclitaxel and depsipeptide in SW620 Ad20 cells. Depsipeptides 98-110 ATP binding cassette subfamily B member 1 Homo sapiens 43-46 17623797-0 2007 Histone deacetylase 1 gene expression and sensitization of multidrug-resistant neuroblastoma cell lines to cytotoxic agents by depsipeptide. Depsipeptides 127-139 histone deacetylase 1 Homo sapiens 0-21 17610380-0 2007 Depsipeptide (FK228) preferentially induces apoptosis in BCR/ABL-expressing cell lines and cells from patients with chronic myelogenous leukemia in blast crisis. Depsipeptides 0-12 BCR activator of RhoGEF and GTPase Homo sapiens 57-60 17610380-2 2007 In this study, we report mechanisms of action of histone deacetylase (HDAC) inhibitor, depsipeptide (FK228) in BCR/ABL-expressing cell lines and its effectiveness in imatinib-resistant cells from patients with blast crisis of CML. Depsipeptides 87-99 ABL proto-oncogene 1, non-receptor tyrosine kinase Homo sapiens 111-118 17186014-7 2007 Increased transgene expression following infection with an adenovirus expressing tumor necrosis factor-related apoptosis inducing ligand (TRAIL) was observed only in LNCaP cells treated with depsipeptide or MS-275. Depsipeptides 191-203 TNF superfamily member 10 Homo sapiens 81-136 17186014-7 2007 Increased transgene expression following infection with an adenovirus expressing tumor necrosis factor-related apoptosis inducing ligand (TRAIL) was observed only in LNCaP cells treated with depsipeptide or MS-275. Depsipeptides 191-203 TNF superfamily member 10 Homo sapiens 138-143 17240363-4 2007 We hypothesized that depsipeptide would modulate MMP-2 and MMP-9 production in lung adenocarcinoma cells line (A549). Depsipeptides 21-33 matrix metallopeptidase 2 Homo sapiens 49-54 17240363-4 2007 We hypothesized that depsipeptide would modulate MMP-2 and MMP-9 production in lung adenocarcinoma cells line (A549). Depsipeptides 21-33 matrix metallopeptidase 9 Homo sapiens 59-64 17240363-7 2007 RESULTS: The results showed that depsipeptide treatment decreased the expressions of MMP-2 and MMP-9 in dose-dependent manner. Depsipeptides 33-45 matrix metallopeptidase 2 Homo sapiens 85-90 17240363-7 2007 RESULTS: The results showed that depsipeptide treatment decreased the expressions of MMP-2 and MMP-9 in dose-dependent manner. Depsipeptides 33-45 matrix metallopeptidase 9 Homo sapiens 95-100 17240363-8 2007 The level of mRNA and proteins expressions were significantly decreased in depsipeptide treated A549 cells in a dose-dependent manner and the level of pro-MMP-9 was found to be high in the 100nm depsipeptide-treated cell lysate of A549 cells, suggesting inhibitory role of depsipeptide on pro-MMP-9 activation. Depsipeptides 75-87 matrix metallopeptidase 9 Homo sapiens 155-160 17240363-8 2007 The level of mRNA and proteins expressions were significantly decreased in depsipeptide treated A549 cells in a dose-dependent manner and the level of pro-MMP-9 was found to be high in the 100nm depsipeptide-treated cell lysate of A549 cells, suggesting inhibitory role of depsipeptide on pro-MMP-9 activation. Depsipeptides 75-87 matrix metallopeptidase 9 Homo sapiens 293-298 17240363-8 2007 The level of mRNA and proteins expressions were significantly decreased in depsipeptide treated A549 cells in a dose-dependent manner and the level of pro-MMP-9 was found to be high in the 100nm depsipeptide-treated cell lysate of A549 cells, suggesting inhibitory role of depsipeptide on pro-MMP-9 activation. Depsipeptides 195-207 matrix metallopeptidase 9 Homo sapiens 155-160 17240363-8 2007 The level of mRNA and proteins expressions were significantly decreased in depsipeptide treated A549 cells in a dose-dependent manner and the level of pro-MMP-9 was found to be high in the 100nm depsipeptide-treated cell lysate of A549 cells, suggesting inhibitory role of depsipeptide on pro-MMP-9 activation. Depsipeptides 195-207 matrix metallopeptidase 9 Homo sapiens 293-298 17240363-8 2007 The level of mRNA and proteins expressions were significantly decreased in depsipeptide treated A549 cells in a dose-dependent manner and the level of pro-MMP-9 was found to be high in the 100nm depsipeptide-treated cell lysate of A549 cells, suggesting inhibitory role of depsipeptide on pro-MMP-9 activation. Depsipeptides 195-207 matrix metallopeptidase 9 Homo sapiens 155-160 17240363-8 2007 The level of mRNA and proteins expressions were significantly decreased in depsipeptide treated A549 cells in a dose-dependent manner and the level of pro-MMP-9 was found to be high in the 100nm depsipeptide-treated cell lysate of A549 cells, suggesting inhibitory role of depsipeptide on pro-MMP-9 activation. Depsipeptides 195-207 matrix metallopeptidase 9 Homo sapiens 293-298 17240363-9 2007 Further immunocytochemistry studies showed the weak expression of MMP-2 and MMP-9 in depsipeptide treated cells. Depsipeptides 85-97 matrix metallopeptidase 2 Homo sapiens 66-71 17240363-9 2007 Further immunocytochemistry studies showed the weak expression of MMP-2 and MMP-9 in depsipeptide treated cells. Depsipeptides 85-97 matrix metallopeptidase 9 Homo sapiens 76-81 17240363-10 2007 CONCLUSION: We speculate that inhibition of metastasis-specific MMPs in cancer cells may be one of the targets for anticancer function of depsipeptide, and thus provides the molecular basis for the development of depsipeptide as a novel chemopreventive agent for metastatic lung cancer. Depsipeptides 138-150 matrix metallopeptidase 2 Homo sapiens 64-68 17240363-10 2007 CONCLUSION: We speculate that inhibition of metastasis-specific MMPs in cancer cells may be one of the targets for anticancer function of depsipeptide, and thus provides the molecular basis for the development of depsipeptide as a novel chemopreventive agent for metastatic lung cancer. Depsipeptides 213-225 matrix metallopeptidase 2 Homo sapiens 64-68 18639283-9 2008 Depsipeptide induced apoptosis in Caki-1, ACHN and 786O, and induced G2 cell cycle arrest in 769P. Depsipeptides 0-12 La ribonucleoprotein 6, translational regulator Homo sapiens 42-46 18185535-5 2008 First, by a quantitative assay of caspase-3/7 activity, a sublethal dose of depsipeptide was determined (ED50: 5 nM), in which p21(Waf1/Cip1) and Fas were sufficiently evoked concomitantly with histone H3 acetylation. Depsipeptides 76-88 caspase 3 Mus musculus 34-43 18185535-5 2008 First, by a quantitative assay of caspase-3/7 activity, a sublethal dose of depsipeptide was determined (ED50: 5 nM), in which p21(Waf1/Cip1) and Fas were sufficiently evoked concomitantly with histone H3 acetylation. Depsipeptides 76-88 cyclin-dependent kinase inhibitor 1A (P21) Mus musculus 127-130 18185535-5 2008 First, by a quantitative assay of caspase-3/7 activity, a sublethal dose of depsipeptide was determined (ED50: 5 nM), in which p21(Waf1/Cip1) and Fas were sufficiently evoked concomitantly with histone H3 acetylation. Depsipeptides 76-88 cyclin-dependent kinase inhibitor 1A (P21) Mus musculus 131-135 18185535-5 2008 First, by a quantitative assay of caspase-3/7 activity, a sublethal dose of depsipeptide was determined (ED50: 5 nM), in which p21(Waf1/Cip1) and Fas were sufficiently evoked concomitantly with histone H3 acetylation. Depsipeptides 76-88 cyclin-dependent kinase inhibitor 1A (P21) Mus musculus 136-140 17644301-0 2008 Romidepsin (depsipeptide) induced cell cycle arrest, apoptosis and histone hyperacetylation in lung carcinoma cells (A549) are associated with increase in p21 and hypophosphorylated retinoblastoma proteins expression. Depsipeptides 12-24 H3 histone pseudogene 16 Homo sapiens 155-158 18225533-0 2007 A sequential treatment of depsipeptide followed by 5-azacytidine enhances Gadd45beta expression in hepatocellular carcinoma cells. Depsipeptides 26-38 growth arrest and DNA damage inducible beta Homo sapiens 74-84 18225533-7 2007 A sequential treatment of depsipeptide+5-azacytidine (but not 5-azacytidine+depsipeptide) exhibited a synergistic effect on Gadd45beta gene reactivation in the HepG2 cells. Depsipeptides 26-38 growth arrest and DNA damage inducible beta Homo sapiens 124-134 17286952-3 2007 Histone deacetylase (HDAC) activity was inhibited by addition of the HDAC inhibitor depsipeptide to the culture medium for different exposure times. Depsipeptides 84-96 histone deacetylase 9 Homo sapiens 0-19 17286952-3 2007 Histone deacetylase (HDAC) activity was inhibited by addition of the HDAC inhibitor depsipeptide to the culture medium for different exposure times. Depsipeptides 84-96 histone deacetylase 9 Homo sapiens 21-25 17286952-3 2007 Histone deacetylase (HDAC) activity was inhibited by addition of the HDAC inhibitor depsipeptide to the culture medium for different exposure times. Depsipeptides 84-96 histone deacetylase 9 Homo sapiens 69-73 17286952-6 2007 Detailed information was obtained for both the change of histone H4 acetylation specific to the N terminus and the global transformation of H4 from one acetylation state to another following treatment with the HDAC inhibitor depsipeptide. Depsipeptides 225-237 histone deacetylase 9 Homo sapiens 210-214 17308048-2 2007 Previously, we showed that treatment with low doses of the histone deacetylase inhibitor FK228 (FR901228, depsipeptide) increased coxsackie adenovirus receptor (CAR) levels, histone H3 acetylation, and adenovirus infection efficiencies as measured by viral transgene expression in cancer cell lines but not in cultured normal cells. Depsipeptides 106-118 coxsackie virus and adenovirus receptor Mus musculus 161-164 16799637-3 2007 Here, we show that RUNX1-ETO undergoes degradation in response to treatment with histone deacetylase inhibitors, one of which, depsipeptide (DEP), is currently undergoing phase II clinical testing in a variety of malignancies. Depsipeptides 127-139 RUNX family transcription factor 1 Homo sapiens 19-24 16799637-3 2007 Here, we show that RUNX1-ETO undergoes degradation in response to treatment with histone deacetylase inhibitors, one of which, depsipeptide (DEP), is currently undergoing phase II clinical testing in a variety of malignancies. Depsipeptides 127-139 RUNX1 partner transcriptional co-repressor 1 Homo sapiens 25-28 17064661-0 2006 5-Aza-2"-deoxycytidine and depsipeptide synergistically induce expression of BIK (BCL2-interacting killer). Depsipeptides 27-39 BCL2 interacting killer Homo sapiens 77-80 17109024-3 2007 Notably, the pleiotropic HDAC inhibitors, suberoylanilide hydroxamic acid (SAHA) and depsipeptide, have shown efficacy in a wide range of cancers, in particular for cutaneous T-cell lymphoma (CTCL), and are progressing in phase II clinical studies. Depsipeptides 85-97 TSPY like 2 Homo sapiens 192-196 17064661-0 2006 5-Aza-2"-deoxycytidine and depsipeptide synergistically induce expression of BIK (BCL2-interacting killer). Depsipeptides 27-39 BCL2 interacting killer Homo sapiens 82-105 17064661-6 2006 Histone acetylation of the BIK promoter region increased with depsipeptide treatment but was not further affected by 5-aza-2"-deoxycytidine. Depsipeptides 62-74 BCL2 interacting killer Homo sapiens 27-30 17064661-7 2006 In summary, synergistic upregulation of pro-apoptotic BIK-previously shown to suppress tumor growth-appears to play a critical role in anticancer effects of 5-aza-2"-deoxycytidine plus depsipeptide. Depsipeptides 185-197 BCL2 interacting killer Homo sapiens 54-57 16995669-1 2006 Fungal beauveriolide III (BeauIII, 1b), a cyclodepsipeptide inhibiting acyl-CoA:cholesterol acyltransferase (ACAT) and showing antiatherogenic activity in mouse models, consists of L-Phe, L-Ala, D-allo-Ile, and 3-hydroxy-4-methyloctanoic acid (HMA) moieties, but the stereochemistry of the HMA part has not until now been fully defined. Depsipeptides 42-59 sterol O-acyltransferase 2 Mus musculus 109-113 16533780-0 2006 Increased MDR1 expression in normal and malignant peripheral blood mononuclear cells obtained from patients receiving depsipeptide (FR901228, FK228, NSC630176). Depsipeptides 118-130 ATP binding cassette subfamily B member 1 Homo sapiens 10-14 16951199-3 2006 Epigenetic modifiers such as histone deacetylase inhibitor FK228 (depsipeptide) have been shown to increase CAR expression as well as the uptake of adenovirus in bladder cancer in vivo and in vitro, indicating that altered transcriptional regulation of CAR is the key mechanism responsible for the decreased CAR levels in this cancer. Depsipeptides 66-78 CXADR Ig-like cell adhesion molecule Homo sapiens 108-111 16951199-3 2006 Epigenetic modifiers such as histone deacetylase inhibitor FK228 (depsipeptide) have been shown to increase CAR expression as well as the uptake of adenovirus in bladder cancer in vivo and in vitro, indicating that altered transcriptional regulation of CAR is the key mechanism responsible for the decreased CAR levels in this cancer. Depsipeptides 66-78 CXADR Ig-like cell adhesion molecule Homo sapiens 253-256 16951199-3 2006 Epigenetic modifiers such as histone deacetylase inhibitor FK228 (depsipeptide) have been shown to increase CAR expression as well as the uptake of adenovirus in bladder cancer in vivo and in vitro, indicating that altered transcriptional regulation of CAR is the key mechanism responsible for the decreased CAR levels in this cancer. Depsipeptides 66-78 CXADR Ig-like cell adhesion molecule Homo sapiens 253-256 16537920-0 2006 Acetylation of p53 at lysine 373/382 by the histone deacetylase inhibitor depsipeptide induces expression of p21(Waf1/Cip1). Depsipeptides 74-86 tumor protein p53 Homo sapiens 15-18 16537920-0 2006 Acetylation of p53 at lysine 373/382 by the histone deacetylase inhibitor depsipeptide induces expression of p21(Waf1/Cip1). Depsipeptides 74-86 cyclin dependent kinase inhibitor 1A Homo sapiens 109-112 16537920-0 2006 Acetylation of p53 at lysine 373/382 by the histone deacetylase inhibitor depsipeptide induces expression of p21(Waf1/Cip1). Depsipeptides 74-86 cyclin dependent kinase inhibitor 1A Homo sapiens 113-117 16537920-0 2006 Acetylation of p53 at lysine 373/382 by the histone deacetylase inhibitor depsipeptide induces expression of p21(Waf1/Cip1). Depsipeptides 74-86 cyclin dependent kinase inhibitor 1A Homo sapiens 118-122 16537920-2 2006 Here we found that an inhibitor of HDAC, depsipeptide (FR901228), but not trichostatin A (TSA), induces p21(Waf1/Cip1) expression through both p53 and Sp1/Sp3 pathways in A549 cells (which retain wild-type p53). Depsipeptides 41-53 cyclin dependent kinase inhibitor 1A Homo sapiens 104-107 16537920-2 2006 Here we found that an inhibitor of HDAC, depsipeptide (FR901228), but not trichostatin A (TSA), induces p21(Waf1/Cip1) expression through both p53 and Sp1/Sp3 pathways in A549 cells (which retain wild-type p53). Depsipeptides 41-53 cyclin dependent kinase inhibitor 1A Homo sapiens 108-112 16537920-2 2006 Here we found that an inhibitor of HDAC, depsipeptide (FR901228), but not trichostatin A (TSA), induces p21(Waf1/Cip1) expression through both p53 and Sp1/Sp3 pathways in A549 cells (which retain wild-type p53). Depsipeptides 41-53 cyclin dependent kinase inhibitor 1A Homo sapiens 113-117 16537920-2 2006 Here we found that an inhibitor of HDAC, depsipeptide (FR901228), but not trichostatin A (TSA), induces p21(Waf1/Cip1) expression through both p53 and Sp1/Sp3 pathways in A549 cells (which retain wild-type p53). Depsipeptides 41-53 tumor protein p53 Homo sapiens 143-146 16537920-2 2006 Here we found that an inhibitor of HDAC, depsipeptide (FR901228), but not trichostatin A (TSA), induces p21(Waf1/Cip1) expression through both p53 and Sp1/Sp3 pathways in A549 cells (which retain wild-type p53). Depsipeptides 41-53 Sp3 transcription factor Homo sapiens 155-158 16537920-2 2006 Here we found that an inhibitor of HDAC, depsipeptide (FR901228), but not trichostatin A (TSA), induces p21(Waf1/Cip1) expression through both p53 and Sp1/Sp3 pathways in A549 cells (which retain wild-type p53). Depsipeptides 41-53 tumor protein p53 Homo sapiens 206-209 16537920-8 2006 Furthermore, activity associated with the binding of the acetylated p53 at K373/K382 to the p21 promoter as well as p21(Waf1/Cip1) expression is significantly increased after depsipeptide treatment, as tested by chromatin immunoprecipitations and Western blotting, respectively. Depsipeptides 175-187 tumor protein p53 Homo sapiens 68-71 16537920-8 2006 Furthermore, activity associated with the binding of the acetylated p53 at K373/K382 to the p21 promoter as well as p21(Waf1/Cip1) expression is significantly increased after depsipeptide treatment, as tested by chromatin immunoprecipitations and Western blotting, respectively. Depsipeptides 175-187 cyclin dependent kinase inhibitor 1A Homo sapiens 92-95 16537920-8 2006 Furthermore, activity associated with the binding of the acetylated p53 at K373/K382 to the p21 promoter as well as p21(Waf1/Cip1) expression is significantly increased after depsipeptide treatment, as tested by chromatin immunoprecipitations and Western blotting, respectively. Depsipeptides 175-187 cyclin dependent kinase inhibitor 1A Homo sapiens 116-119 16537920-8 2006 Furthermore, activity associated with the binding of the acetylated p53 at K373/K382 to the p21 promoter as well as p21(Waf1/Cip1) expression is significantly increased after depsipeptide treatment, as tested by chromatin immunoprecipitations and Western blotting, respectively. Depsipeptides 175-187 cyclin dependent kinase inhibitor 1A Homo sapiens 120-124 16537920-8 2006 Furthermore, activity associated with the binding of the acetylated p53 at K373/K382 to the p21 promoter as well as p21(Waf1/Cip1) expression is significantly increased after depsipeptide treatment, as tested by chromatin immunoprecipitations and Western blotting, respectively. Depsipeptides 175-187 cyclin dependent kinase inhibitor 1A Homo sapiens 125-129 16537920-9 2006 In addition, p53 acetylation at K373/K382 is confirmed to be required for recruitment of p300 to the p21 promoter, and the depsipeptide-induced p53 acetylation at K373/K382 is unlikely to be dependent on p53 phosphorylation at Ser15, Ser20, and Ser392 sites. Depsipeptides 123-135 tumor protein p53 Homo sapiens 13-16 16537920-9 2006 In addition, p53 acetylation at K373/K382 is confirmed to be required for recruitment of p300 to the p21 promoter, and the depsipeptide-induced p53 acetylation at K373/K382 is unlikely to be dependent on p53 phosphorylation at Ser15, Ser20, and Ser392 sites. Depsipeptides 123-135 E1A binding protein p300 Homo sapiens 89-93 16537920-9 2006 In addition, p53 acetylation at K373/K382 is confirmed to be required for recruitment of p300 to the p21 promoter, and the depsipeptide-induced p53 acetylation at K373/K382 is unlikely to be dependent on p53 phosphorylation at Ser15, Ser20, and Ser392 sites. Depsipeptides 123-135 cyclin dependent kinase inhibitor 1A Homo sapiens 101-104 16537920-9 2006 In addition, p53 acetylation at K373/K382 is confirmed to be required for recruitment of p300 to the p21 promoter, and the depsipeptide-induced p53 acetylation at K373/K382 is unlikely to be dependent on p53 phosphorylation at Ser15, Ser20, and Ser392 sites. Depsipeptides 123-135 tumor protein p53 Homo sapiens 144-147 16537920-9 2006 In addition, p53 acetylation at K373/K382 is confirmed to be required for recruitment of p300 to the p21 promoter, and the depsipeptide-induced p53 acetylation at K373/K382 is unlikely to be dependent on p53 phosphorylation at Ser15, Ser20, and Ser392 sites. Depsipeptides 123-135 tumor protein p53 Homo sapiens 144-147 16537920-10 2006 Our data suggest that p53 acetylation at K373/K382 plays an important role in depsipeptide-induced p21(Waf1/Cip1) expression. Depsipeptides 78-90 tumor protein p53 Homo sapiens 22-25 16537920-10 2006 Our data suggest that p53 acetylation at K373/K382 plays an important role in depsipeptide-induced p21(Waf1/Cip1) expression. Depsipeptides 78-90 cyclin dependent kinase inhibitor 1A Homo sapiens 99-102 16537920-10 2006 Our data suggest that p53 acetylation at K373/K382 plays an important role in depsipeptide-induced p21(Waf1/Cip1) expression. Depsipeptides 78-90 cyclin dependent kinase inhibitor 1A Homo sapiens 103-107 16537920-10 2006 Our data suggest that p53 acetylation at K373/K382 plays an important role in depsipeptide-induced p21(Waf1/Cip1) expression. Depsipeptides 78-90 cyclin dependent kinase inhibitor 1A Homo sapiens 108-112 16891247-0 2006 In vitro metabolism of the epoxide substructure of cryptophycins by cytosolic glutathione S-transferase: species differences and stereoselectivity. Depsipeptides 51-64 glutathione S-transferase kappa 1 Homo sapiens 78-103 16849582-0 2006 Bortezomib and depsipeptide sensitize tumors to tumor necrosis factor-related apoptosis-inducing ligand: a novel method to potentiate natural killer cell tumor cytotoxicity. Depsipeptides 15-27 TNF superfamily member 10 Homo sapiens 48-103 16260035-4 2006 P-gp expression returned to the parental cell level when resistant cells were cultured in depsipeptide-free medium, while resistant cells cultured in the medium containing 16 nM depsipeptide still showed hyper-acetylation of histones. Depsipeptides 90-102 ATP binding cassette subfamily B member 1 Homo sapiens 0-4 16260035-8 2006 Among the 28 genes that were upregulated, 15 genes also showed an increased expression in parental cells treated with 4 nM depsipeptide for 48 h, while the other 13 genes including P-gp were different. Depsipeptides 123-135 ATP binding cassette subfamily B member 1 Homo sapiens 181-185 16260035-10 2006 These findings suggest that continuous exposure to depsipeptide reversibly induces P-gp, which contributes to the onset of resistance, but the altered gene expression profile of resistant cells may also play a role. Depsipeptides 51-63 ATP binding cassette subfamily B member 1 Homo sapiens 83-87 16533780-7 2006 We next examined MDR1 levels in normal and malignant PBMCs obtained from 15 patients enrolled in clinical trials with depsipeptide and detected up to a 6-fold increase in normal PBMCs and up to an 8-fold increase in circulating tumor cells after depsipeptide administration. Depsipeptides 118-130 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 16533780-7 2006 We next examined MDR1 levels in normal and malignant PBMCs obtained from 15 patients enrolled in clinical trials with depsipeptide and detected up to a 6-fold increase in normal PBMCs and up to an 8-fold increase in circulating tumor cells after depsipeptide administration. Depsipeptides 246-258 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 16533780-9 2006 These studies suggest that depsipeptide induces its own mechanism of resistance and thus provide a basis for clinical trials evaluating depsipeptide in combination with a Pgp inhibitor. Depsipeptides 27-39 ATP binding cassette subfamily B member 1 Homo sapiens 171-174 16533780-2 2006 Because depsipeptide (FR901228, FK228, NSC630176) is a substrate for Pgp, up-regulation of the gene that encodes it, MDR1, would mean that depsipeptide induces its own mechanism of resistance. Depsipeptides 8-20 ATP binding cassette subfamily B member 1 Homo sapiens 69-72 16533780-2 2006 Because depsipeptide (FR901228, FK228, NSC630176) is a substrate for Pgp, up-regulation of the gene that encodes it, MDR1, would mean that depsipeptide induces its own mechanism of resistance. Depsipeptides 8-20 ATP binding cassette subfamily B member 1 Homo sapiens 117-121 15735751-0 2005 Sequential 5-Aza 2"-deoxycytidine/depsipeptide FK228 treatment induces tissue factor pathway inhibitor 2 (TFPI-2) expression in cancer cells. Depsipeptides 34-46 tissue factor pathway inhibitor 2 Homo sapiens 71-104 16676400-7 2006 To study the mechanism of NNMT gene repression by depsipeptide, effects of depsipeptide on NNMT promoter activity were determined by luciferase reporter gene assay. Depsipeptides 50-62 nicotinamide N-methyltransferase Homo sapiens 26-30 16676400-7 2006 To study the mechanism of NNMT gene repression by depsipeptide, effects of depsipeptide on NNMT promoter activity were determined by luciferase reporter gene assay. Depsipeptides 75-87 nicotinamide N-methyltransferase Homo sapiens 91-95 16271139-7 2005 Inducible expression and function of the leukemia inhibitory factor receptor was assessed by treatment with the histone deacetylase inhibitor depsipeptide. Depsipeptides 142-154 LIF receptor subunit alpha Homo sapiens 41-76 15515013-0 2005 Involvement of the tumor necrosis factor (TNF)/TNF receptor system in leukemic cell apoptosis induced by histone deacetylase inhibitor depsipeptide (FK228). Depsipeptides 135-147 tumor necrosis factor Homo sapiens 19-40 15515013-0 2005 Involvement of the tumor necrosis factor (TNF)/TNF receptor system in leukemic cell apoptosis induced by histone deacetylase inhibitor depsipeptide (FK228). Depsipeptides 135-147 tumor necrosis factor Homo sapiens 42-45 15515013-0 2005 Involvement of the tumor necrosis factor (TNF)/TNF receptor system in leukemic cell apoptosis induced by histone deacetylase inhibitor depsipeptide (FK228). Depsipeptides 135-147 tumor necrosis factor Homo sapiens 47-50 15515013-0 2005 Involvement of the tumor necrosis factor (TNF)/TNF receptor system in leukemic cell apoptosis induced by histone deacetylase inhibitor depsipeptide (FK228). Depsipeptides 135-147 histone deacetylase 9 Homo sapiens 105-124 15515013-2 2005 In this study, we conducted a detailed analysis of anti-leukemic effects of an HDAC inhibitor (HDI), depsipeptide (FK228), using myeloid leukemia cell lines HL-60 and K562. Depsipeptides 101-113 histone deacetylase 9 Homo sapiens 79-83 15515013-3 2005 DNA chip analysis revealed upregulation of TNF-alpha mRNA and a number of molecules involved in TNF-signaling such as TRAF-6, caspases-10, and -7 in depsipeptide-treated HL-60 cells, which prompted us to examine the involvement of the TNF/TNF receptor system in the anti-leukemic effects of the drug. Depsipeptides 149-161 tumor necrosis factor Homo sapiens 43-52 15515013-3 2005 DNA chip analysis revealed upregulation of TNF-alpha mRNA and a number of molecules involved in TNF-signaling such as TRAF-6, caspases-10, and -7 in depsipeptide-treated HL-60 cells, which prompted us to examine the involvement of the TNF/TNF receptor system in the anti-leukemic effects of the drug. Depsipeptides 149-161 tumor necrosis factor Homo sapiens 43-46 15515013-3 2005 DNA chip analysis revealed upregulation of TNF-alpha mRNA and a number of molecules involved in TNF-signaling such as TRAF-6, caspases-10, and -7 in depsipeptide-treated HL-60 cells, which prompted us to examine the involvement of the TNF/TNF receptor system in the anti-leukemic effects of the drug. Depsipeptides 149-161 TNF receptor associated factor 6 Homo sapiens 118-124 15515013-3 2005 DNA chip analysis revealed upregulation of TNF-alpha mRNA and a number of molecules involved in TNF-signaling such as TRAF-6, caspases-10, and -7 in depsipeptide-treated HL-60 cells, which prompted us to examine the involvement of the TNF/TNF receptor system in the anti-leukemic effects of the drug. Depsipeptides 149-161 caspase 10 Homo sapiens 126-145 15515013-3 2005 DNA chip analysis revealed upregulation of TNF-alpha mRNA and a number of molecules involved in TNF-signaling such as TRAF-6, caspases-10, and -7 in depsipeptide-treated HL-60 cells, which prompted us to examine the involvement of the TNF/TNF receptor system in the anti-leukemic effects of the drug. Depsipeptides 149-161 tumor necrosis factor Homo sapiens 96-99 15515013-3 2005 DNA chip analysis revealed upregulation of TNF-alpha mRNA and a number of molecules involved in TNF-signaling such as TRAF-6, caspases-10, and -7 in depsipeptide-treated HL-60 cells, which prompted us to examine the involvement of the TNF/TNF receptor system in the anti-leukemic effects of the drug. Depsipeptides 149-161 tumor necrosis factor Homo sapiens 96-99 15515013-4 2005 Upregulation of TNF-alpha was induced by depsipeptide in HL-60 and K562 cells, which expressed type I TNF receptors (TNF-RI). Depsipeptides 41-53 tumor necrosis factor Homo sapiens 16-25 15515013-4 2005 Upregulation of TNF-alpha was induced by depsipeptide in HL-60 and K562 cells, which expressed type I TNF receptors (TNF-RI). Depsipeptides 41-53 tumor necrosis factor Homo sapiens 16-19 15515013-4 2005 Upregulation of TNF-alpha was induced by depsipeptide in HL-60 and K562 cells, which expressed type I TNF receptors (TNF-RI). Depsipeptides 41-53 TNF receptor superfamily member 1A Homo sapiens 117-123 15515013-5 2005 Depsipeptide activated caspases-8 and -10, which in turn cleave caspases-3 and -7, leading to apoptotic cell death in both cell lines. Depsipeptides 0-12 caspase 8 Homo sapiens 23-41 15515013-5 2005 Depsipeptide activated caspases-8 and -10, which in turn cleave caspases-3 and -7, leading to apoptotic cell death in both cell lines. Depsipeptides 0-12 caspase 3 Homo sapiens 64-81 15515013-7 2005 Finally, we demonstrated that the enhanced production of TNF-alpha by depsipeptide was due to transcriptional activation of the TNF-alpha gene through hyperacetylation of histones H3 and H4 in its promoter region (-208 to +35). Depsipeptides 70-82 tumor necrosis factor Homo sapiens 57-66 15515013-7 2005 Finally, we demonstrated that the enhanced production of TNF-alpha by depsipeptide was due to transcriptional activation of the TNF-alpha gene through hyperacetylation of histones H3 and H4 in its promoter region (-208 to +35). Depsipeptides 70-82 tumor necrosis factor Homo sapiens 128-137 15515013-8 2005 These results suggest that autocrine production of TNF-alpha plays a role in the cytotoxicity of depsipeptide against a subset of leukemias. Depsipeptides 97-109 tumor necrosis factor Homo sapiens 51-60 15771957-0 2005 Depsipeptide (FR901228) enhances the cytotoxic activity of TRAIL by redistributing TRAIL receptor to membrane lipid rafts. Depsipeptides 0-12 TNF superfamily member 10 Homo sapiens 59-64 15771957-0 2005 Depsipeptide (FR901228) enhances the cytotoxic activity of TRAIL by redistributing TRAIL receptor to membrane lipid rafts. Depsipeptides 0-12 TNF superfamily member 10 Homo sapiens 83-88 15771957-5 2005 Thus, studies were initiated to evaluate the ability of depsipeptide to enhance the cytotoxic activity of Ad5-TRAIL against human prostate tumor cells. Depsipeptides 56-68 Alzheimer disease, familial, type 5 Homo sapiens 106-109 15771957-5 2005 Thus, studies were initiated to evaluate the ability of depsipeptide to enhance the cytotoxic activity of Ad5-TRAIL against human prostate tumor cells. Depsipeptides 56-68 TNF superfamily member 10 Homo sapiens 110-115 15771957-7 2005 Additionally, tumor cell killing by Ad5-TRAIL was higher following depsipeptide pretreatment. Depsipeptides 67-79 Alzheimer disease, familial, type 5 Homo sapiens 36-39 15771957-7 2005 Additionally, tumor cell killing by Ad5-TRAIL was higher following depsipeptide pretreatment. Depsipeptides 67-79 TNF superfamily member 10 Homo sapiens 40-45 15771957-9 2005 Investigation into the mechanism responsible for increased TRAIL responsiveness revealed increased levels of TRAIL-R1 and -R2 in membrane lipid rafts following depsipeptide treatment. Depsipeptides 160-172 TNF superfamily member 10 Homo sapiens 59-64 15771957-9 2005 Investigation into the mechanism responsible for increased TRAIL responsiveness revealed increased levels of TRAIL-R1 and -R2 in membrane lipid rafts following depsipeptide treatment. Depsipeptides 160-172 TNF receptor superfamily member 10a Homo sapiens 109-125 15771957-10 2005 These results indicate that depsipeptide is a potent agent for enhancing the activity of Ad5-TRAIL by multiple mechanisms, allowing for a more efficient use of Ad5-TRAIL as an antitumor therapy. Depsipeptides 28-40 Alzheimer disease, familial, type 5 Homo sapiens 89-92 15771957-10 2005 These results indicate that depsipeptide is a potent agent for enhancing the activity of Ad5-TRAIL by multiple mechanisms, allowing for a more efficient use of Ad5-TRAIL as an antitumor therapy. Depsipeptides 28-40 TNF superfamily member 10 Homo sapiens 93-98 15771957-10 2005 These results indicate that depsipeptide is a potent agent for enhancing the activity of Ad5-TRAIL by multiple mechanisms, allowing for a more efficient use of Ad5-TRAIL as an antitumor therapy. Depsipeptides 28-40 Alzheimer disease, familial, type 5 Homo sapiens 160-163 15771957-10 2005 These results indicate that depsipeptide is a potent agent for enhancing the activity of Ad5-TRAIL by multiple mechanisms, allowing for a more efficient use of Ad5-TRAIL as an antitumor therapy. Depsipeptides 28-40 TNF superfamily member 10 Homo sapiens 164-169 16223781-0 2006 Up-regulation of MDR1 and induction of doxorubicin resistance by histone deacetylase inhibitor depsipeptide (FK228) and ATRA in acute promyelocytic leukemia cells. Depsipeptides 95-107 ATP binding cassette subfamily B member 1 Homo sapiens 17-21 16223781-3 2006 The combination of ATRA and the novel histone deacetylase inhibitor (HDACI) depsipeptide (FK228) induced P-gp expression and prevented growth inhibition and apoptosis in NB4 APL cells subsequently exposed to doxorubicin (DOX). Depsipeptides 76-88 ATP binding cassette subfamily B member 1 Homo sapiens 105-109 16676400-0 2006 Histone deacetylase inhibitor depsipeptide represses nicotinamide N-methyltransferase and hepatocyte nuclear factor-1beta gene expression in human papillary thyroid cancer cells. Depsipeptides 30-42 nicotinamide N-methyltransferase Homo sapiens 53-85 16676400-0 2006 Histone deacetylase inhibitor depsipeptide represses nicotinamide N-methyltransferase and hepatocyte nuclear factor-1beta gene expression in human papillary thyroid cancer cells. Depsipeptides 30-42 HNF1 homeobox B Homo sapiens 90-121 16676400-3 2006 In this work, we studied the effects of depsipeptide, a histone deacetylase inhibitor, on NNMT gene expression in BHP 18-21 papillary thyroid cancer cells. Depsipeptides 40-52 nicotinamide N-methyltransferase Homo sapiens 90-94 16676400-6 2006 NNMT protein level determined by Western blot analysis and NNMT catalytic activity was also reduced significantly in the depsipeptide-treated cells. Depsipeptides 121-133 nicotinamide N-methyltransferase Homo sapiens 0-4 16676400-6 2006 NNMT protein level determined by Western blot analysis and NNMT catalytic activity was also reduced significantly in the depsipeptide-treated cells. Depsipeptides 121-133 nicotinamide N-methyltransferase Homo sapiens 59-63 16424655-0 2006 Histone deacetylase inhibitor depsipeptide (FK228) induces apoptosis in leukemic cells by facilitating mitochondrial translocation of Bax, which is enhanced by the proteasome inhibitor bortezomib. Depsipeptides 30-42 histone deacetylase 9 Homo sapiens 0-19 16424655-0 2006 Histone deacetylase inhibitor depsipeptide (FK228) induces apoptosis in leukemic cells by facilitating mitochondrial translocation of Bax, which is enhanced by the proteasome inhibitor bortezomib. Depsipeptides 30-42 BCL2 associated X, apoptosis regulator Homo sapiens 134-137 16424655-2 2006 In this study, we investigated the mechanisms of cytotoxic effects of depsipeptide (FK228), one of the most effective HDAC inhibitors against leukemia, using human myeloid leukemic cell lines HL-60 and K562. Depsipeptides 70-82 histone deacetylase 9 Homo sapiens 118-122 16140944-6 2005 Quantitative reverse transcription-PCR analysis revealed robust, coincident induction of BORIS and NY-ESO-1 expression in lung cancer cells, but not normal human bronchial epithelial cells following 5-aza-2"-deoxycytidine (5-azadC), Depsipeptide FK228 (DP), or sequential 5-azadC/DP exposure under clinically relevant conditions. Depsipeptides 233-245 CCCTC-binding factor like Homo sapiens 89-94 16140944-6 2005 Quantitative reverse transcription-PCR analysis revealed robust, coincident induction of BORIS and NY-ESO-1 expression in lung cancer cells, but not normal human bronchial epithelial cells following 5-aza-2"-deoxycytidine (5-azadC), Depsipeptide FK228 (DP), or sequential 5-azadC/DP exposure under clinically relevant conditions. Depsipeptides 233-245 cancer/testis antigen 1A Homo sapiens 99-107 15735751-0 2005 Sequential 5-Aza 2"-deoxycytidine/depsipeptide FK228 treatment induces tissue factor pathway inhibitor 2 (TFPI-2) expression in cancer cells. Depsipeptides 34-46 tissue factor pathway inhibitor 2 Homo sapiens 106-112 15735013-6 2005 Furthermore, RUNX1/MTG8 and DNMT1 were concurrently released from the IL-3 promoter by exposure to depsipeptide or stabilized on the promoter by decitabine treatment. Depsipeptides 99-111 interleukin 3 Homo sapiens 70-74 15738394-6 2005 APAF-1, a gene central to the intrinsic apoptotic pathway, was induced by SAHA and depsipeptide and shown to be important, but not essential, for HDACi-induced cell death. Depsipeptides 83-95 apoptotic peptidase activating factor 1 Homo sapiens 0-6 15735013-6 2005 Furthermore, RUNX1/MTG8 and DNMT1 were concurrently released from the IL-3 promoter by exposure to depsipeptide or stabilized on the promoter by decitabine treatment. Depsipeptides 99-111 RUNX family transcription factor 1 Homo sapiens 13-18 15735013-6 2005 Furthermore, RUNX1/MTG8 and DNMT1 were concurrently released from the IL-3 promoter by exposure to depsipeptide or stabilized on the promoter by decitabine treatment. Depsipeptides 99-111 RUNX1 partner transcriptional co-repressor 1 Homo sapiens 19-23 15735013-6 2005 Furthermore, RUNX1/MTG8 and DNMT1 were concurrently released from the IL-3 promoter by exposure to depsipeptide or stabilized on the promoter by decitabine treatment. Depsipeptides 99-111 DNA methyltransferase 1 Homo sapiens 28-33 14996704-4 2004 Treatment with depsipeptide, as well as other histone deacetylase inhibitors, caused induction of histone acetylation, induction of p21 expression, and substantial apoptosis without significant cell cycle arrest. Depsipeptides 15-27 H3 histone pseudogene 16 Homo sapiens 132-135 15608694-4 2004 We report that low concentrations of histone deacetylase (HDAC) inhibitors, such as depsipeptide, which alone failed to induce apoptosis, markedly sensitize CLL cells and other primary lymphoid malignancies to TRAIL-induced apoptosis. Depsipeptides 84-96 TNF superfamily member 10 Homo sapiens 210-215 15467034-11 2004 Depsipeptide-mediated apoptosis was associated with a 12-fold increased level of active caspase 3, but some apoptosis persisted despite z-VAD-fmk treatment to inhibit caspase activity. Depsipeptides 0-12 caspase 3 Homo sapiens 88-97 14996704-6 2004 Treatment with depsipeptide increased expression of the interleukin-2 (IL-2) receptor, and combination with the IL-2 toxin conjugate denileukin diftitox resulted in more than additive toxicity. Depsipeptides 15-27 interleukin 2 Homo sapiens 56-69 14996704-6 2004 Treatment with depsipeptide increased expression of the interleukin-2 (IL-2) receptor, and combination with the IL-2 toxin conjugate denileukin diftitox resulted in more than additive toxicity. Depsipeptides 15-27 interleukin 2 receptor subunit beta Homo sapiens 71-85 14996704-6 2004 Treatment with depsipeptide increased expression of the interleukin-2 (IL-2) receptor, and combination with the IL-2 toxin conjugate denileukin diftitox resulted in more than additive toxicity. Depsipeptides 15-27 interleukin 2 Homo sapiens 71-75 14996704-8 2004 However, cells selected for resistance to depsipeptide in the presence of a Pgp inhibitor had a Pgp-independent mechanism of resistance. Depsipeptides 42-54 ATP binding cassette subfamily B member 1 Homo sapiens 76-79 14996704-8 2004 However, cells selected for resistance to depsipeptide in the presence of a Pgp inhibitor had a Pgp-independent mechanism of resistance. Depsipeptides 42-54 ATP binding cassette subfamily B member 1 Homo sapiens 96-99 15059137-3 2004 Depsipeptide, a new member of the HDAC inhibitors, was found to be safe in humans and has been shown to induce apoptosis in various cancers. Depsipeptides 0-12 histone deacetylase 9 Homo sapiens 34-38 15109660-1 2004 Two analogues possessing steric hindered substituents on C-15 of arenastatin A (1), a potent cytotoxic spongean depsipeptide, were synthesized and shown to enhance stability in mouse serum. Depsipeptides 112-124 placenta associated 8 Homo sapiens 57-61 15078940-2 2004 FR901228, FK228, or depsipeptide, is an HDAC inhibitor effective in T-cell lymphomas. Depsipeptides 20-32 histone deacetylase 9 Homo sapiens 40-44 15059137-9 2004 BCL-2, BCL-XL and MCL-1 showed decreased expression in depsipeptide-treated samples. Depsipeptides 55-67 BCL2 apoptosis regulator Homo sapiens 0-5 15059137-9 2004 BCL-2, BCL-XL and MCL-1 showed decreased expression in depsipeptide-treated samples. Depsipeptides 55-67 BCL2 like 1 Homo sapiens 7-13 15059137-9 2004 BCL-2, BCL-XL and MCL-1 showed decreased expression in depsipeptide-treated samples. Depsipeptides 55-67 MCL1 apoptosis regulator, BCL2 family member Homo sapiens 18-23 15014036-0 2004 Abrogation of p21 expression by flavopiridol enhances depsipeptide-mediated apoptosis in malignant pleural mesothelioma cells. Depsipeptides 54-66 cyclin dependent kinase inhibitor 1A Homo sapiens 14-17 15014036-11 2004 Calphostin C abrogated p21 induction mediated by DP and enhanced DP-mediated apoptosis in a manner comparable with FLA in MPM cells; in contrast, phorbol-12,13-dibutyrate blocked FLA-mediated inhibition of p21 induction by DP and markedly protected these cells from the apoptotic effects of sequential DP/FLA. Depsipeptides 49-51 cyclin dependent kinase inhibitor 1A Homo sapiens 23-26 15014036-8 2004 The proapoptotic effects of DP/FLA treatment coincided with inhibition of DP-mediated induction of p21 by FLA. Overexpression of p21 by adenoviral gene transfer techniques rendered MPM cells refractory to the cytotoxic effects of this treatment regimen. Depsipeptides 28-30 cyclin dependent kinase inhibitor 1A Homo sapiens 99-102 15014036-12 2004 CONCLUSIONS: FLA abrogates DP-mediated induction of p21 expression, in part, via inhibition of protein kinase C signaling and markedly potentiates the cytotoxic effects of DP in MPM cells. Depsipeptides 27-29 cyclin dependent kinase inhibitor 1A Homo sapiens 52-55 15014036-8 2004 The proapoptotic effects of DP/FLA treatment coincided with inhibition of DP-mediated induction of p21 by FLA. Overexpression of p21 by adenoviral gene transfer techniques rendered MPM cells refractory to the cytotoxic effects of this treatment regimen. Depsipeptides 28-30 cyclin dependent kinase inhibitor 1A Homo sapiens 129-132 15014036-9 2004 In p21 reporter assays, promoter activation by DP was antagonized by FLA. Depsipeptides 47-49 cyclin dependent kinase inhibitor 1A Homo sapiens 3-6 15148683-5 2004 This review gives an overview of the occurrence and importance of beta2-amino acids in nature, placing emphasis on the metabolic pathways of beta-aminoisobutyric acid (beta-Aib) and the appearance of beta2-amino acids as secondary metabolites or as components of more complex natural products, such as peptides, depsipeptides, lactones, and alkaloids. Depsipeptides 312-325 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 66-71 15148683-5 2004 This review gives an overview of the occurrence and importance of beta2-amino acids in nature, placing emphasis on the metabolic pathways of beta-aminoisobutyric acid (beta-Aib) and the appearance of beta2-amino acids as secondary metabolites or as components of more complex natural products, such as peptides, depsipeptides, lactones, and alkaloids. Depsipeptides 312-325 potassium calcium-activated channel subfamily M regulatory beta subunit 2 Homo sapiens 200-205 15264661-1 2004 Poly(ester amide) copolymers based on L-lactide (2) and a new depsipeptide (1) were prepared by ring opening polymerization in the presence of Sn(Oct)2 as the catalyst. Depsipeptides 62-74 POU domain, class 2, transcription factor 2 Mus musculus 143-151 14698558-10 2004 These results were validated in primary leukemia cells from patients with refractory or relapsed AML or chronic lymphocytic leukemia (CLL) treated on a Phase I clinical trial of the HDAC inhibitor depsipeptide. Depsipeptides 197-209 histone deacetylase 9 Homo sapiens 182-186 14695142-7 2003 HRK expression was restored by treatment with a methyltransferase inhibitor, 5-aza-deoxycytidine, and enhanced further by addition of histone deacetylase inhibitor trichostatin A or depsipeptide. Depsipeptides 182-194 harakiri, BCL2 interacting protein Homo sapiens 0-3 15171260-2 2004 A number of structural classes of HDAC inhibitors have been developed of which several are in clinical trials, including phenylbutyrate (PB) and related compounds; the hydroxamic acids, suberoylanilide hydroxamic acid (SAHA) and depsipeptide (FK-228); and the benzamides, MS-275 and C1-994. Depsipeptides 229-241 histone deacetylase 9 Homo sapiens 34-38 18521390-5 2004 Changes in CAR and alpha(v) integrin expression RMS in response to pretreatment with depsipeptide (FR901128) was determined using RT-PCR.Results. Depsipeptides 85-97 CXADR Ig-like cell adhesion molecule Homo sapiens 11-14 18521390-7 2004 RT-PCR analysis for CAR showed that in four of these five cell lines, CAR expression was increased 2.8-8.1-fold in cells treated with depsipeptide (FR901228) as compared to control. Depsipeptides 134-146 CXADR Ig-like cell adhesion molecule Homo sapiens 20-23 18521390-7 2004 RT-PCR analysis for CAR showed that in four of these five cell lines, CAR expression was increased 2.8-8.1-fold in cells treated with depsipeptide (FR901228) as compared to control. Depsipeptides 134-146 CXADR Ig-like cell adhesion molecule Homo sapiens 70-73 14528273-9 2003 Histone deacetylases (HDACs) can be inhibited by numerous compounds (sodium phenylbutyrate, valproic acid, novel compounds such as depsipeptide), which have entered the clinical arena in similar indications as Dnmt inhibitors. Depsipeptides 131-143 DNA methyltransferase 1 Homo sapiens 210-214 12773551-9 2003 Depsipeptide induced p21(Cip1) expression was reconstituted when cells were pretreated with 5-aza-2"-deoxycytidine. Depsipeptides 0-12 H3 histone pseudogene 16 Homo sapiens 21-24 12649137-0 2003 Depsipeptide (FR901228) induces histone acetylation and inhibition of histone deacetylase in chronic lymphocytic leukemia cells concurrent with activation of caspase 8-mediated apoptosis and down-regulation of c-FLIP protein. Depsipeptides 0-12 caspase 8 Homo sapiens 158-167 12649137-0 2003 Depsipeptide (FR901228) induces histone acetylation and inhibition of histone deacetylase in chronic lymphocytic leukemia cells concurrent with activation of caspase 8-mediated apoptosis and down-regulation of c-FLIP protein. Depsipeptides 0-12 CASP8 and FADD like apoptosis regulator Homo sapiens 210-216 12649137-5 2003 Depsipeptide-induced apoptosis is caspase dependent, selectively involving the tumor necrosis factor (TNF) receptor (extrinsic pathway) initiating caspase 8 and effector caspase 3. Depsipeptides 0-12 caspase 8 Homo sapiens 147-156 12782595-2 2003 In this work, we show that p21(WAF1) induction by HDAC inhibitors (depsipeptide and trichostatin A) is defective in Ataxia telangiectasia (AT) cells but normal in matched wild-type (WT) cells (human diploid fibroblasts). Depsipeptides 67-79 cyclin dependent kinase inhibitor 1A Homo sapiens 27-30 12782595-2 2003 In this work, we show that p21(WAF1) induction by HDAC inhibitors (depsipeptide and trichostatin A) is defective in Ataxia telangiectasia (AT) cells but normal in matched wild-type (WT) cells (human diploid fibroblasts). Depsipeptides 67-79 cyclin dependent kinase inhibitor 1A Homo sapiens 31-35 12782595-2 2003 In this work, we show that p21(WAF1) induction by HDAC inhibitors (depsipeptide and trichostatin A) is defective in Ataxia telangiectasia (AT) cells but normal in matched wild-type (WT) cells (human diploid fibroblasts). Depsipeptides 67-79 histone deacetylase 9 Homo sapiens 50-54 12773551-9 2003 Depsipeptide induced p21(Cip1) expression was reconstituted when cells were pretreated with 5-aza-2"-deoxycytidine. Depsipeptides 0-12 cyclin dependent kinase inhibitor 1A Homo sapiens 25-29 12678732-4 2002 In the class of HDAC inhibitors, now included a short-chain fatty acids, such as 4-phenylbutyrate and valporic acid, hydroxamic acids, such as suberoylanilide hydroxamic acid (SAHA), pyroxamide, trichostatin A, oxamflatin and CHAPSs, cyclic tetrapeptides, such as trapoxin, apicidin and depsipeptide-also known as FK-228 or FR 901228, and benzamides, such as MS-275. Depsipeptides 287-299 histone deacetylase 9 Homo sapiens 16-20 12634613-0 2003 Interaction of 5-aza-2"-deoxycytidine and depsipeptide on antineoplastic activity and activation of 14-3-3sigma, E-cadherin and tissue inhibitor of metalloproteinase 3 expression in human breast carcinoma cells. Depsipeptides 42-54 stratifin Homo sapiens 100-111 12634613-0 2003 Interaction of 5-aza-2"-deoxycytidine and depsipeptide on antineoplastic activity and activation of 14-3-3sigma, E-cadherin and tissue inhibitor of metalloproteinase 3 expression in human breast carcinoma cells. Depsipeptides 42-54 cadherin 1 Homo sapiens 113-123 12634613-0 2003 Interaction of 5-aza-2"-deoxycytidine and depsipeptide on antineoplastic activity and activation of 14-3-3sigma, E-cadherin and tissue inhibitor of metalloproteinase 3 expression in human breast carcinoma cells. Depsipeptides 42-54 TIMP metallopeptidase inhibitor 3 Homo sapiens 128-167 12455031-7 2003 Using semi-quantitative RT-PCR, we observed that 5-aza-2"-deoxycytidine in combination with depsipeptide produced a greater reactivation of both maspin and gelsolin as compared to each agent alone. Depsipeptides 92-104 serpin family B member 5 Homo sapiens 145-151 12455031-7 2003 Using semi-quantitative RT-PCR, we observed that 5-aza-2"-deoxycytidine in combination with depsipeptide produced a greater reactivation of both maspin and gelsolin as compared to each agent alone. Depsipeptides 92-104 gelsolin Homo sapiens 156-164 12481415-2 2002 Here we show that the HDIs sodium butyrate (Bu), trichostatin A (TSA) and depsipeptide (FR901228) all induced p21, but only TSA and FR901228 caused mitotic arrest (in addition to arrest in G1 and G2). Depsipeptides 74-86 H3 histone pseudogene 16 Homo sapiens 110-113 12115133-3 2002 The structure of an 11-residue peptide Boc-Val-Ala-Leu-Aib-Val-Ala-Leu-Aib-Val-Ala-Leu-OMe (2), analog of a which is an amide previously determined Lac-containing depsipeptide, Boc-Val-Ala-Leu-Aib-Val-Lac-Leu-Aib-Val-Ala-Leu-OMe I. L. Karle, C. Das, and P. Balaram, Biopolymers, Vol. Depsipeptides 163-175 ANIB1 Homo sapiens 71-74 12115133-3 2002 The structure of an 11-residue peptide Boc-Val-Ala-Leu-Aib-Val-Ala-Leu-Aib-Val-Ala-Leu-OMe (2), analog of a which is an amide previously determined Lac-containing depsipeptide, Boc-Val-Ala-Leu-Aib-Val-Lac-Leu-Aib-Val-Ala-Leu-OMe I. L. Karle, C. Das, and P. Balaram, Biopolymers, Vol. Depsipeptides 163-175 ANIB1 Homo sapiens 71-74 12115133-3 2002 The structure of an 11-residue peptide Boc-Val-Ala-Leu-Aib-Val-Ala-Leu-Aib-Val-Ala-Leu-OMe (2), analog of a which is an amide previously determined Lac-containing depsipeptide, Boc-Val-Ala-Leu-Aib-Val-Lac-Leu-Aib-Val-Ala-Leu-OMe I. L. Karle, C. Das, and P. Balaram, Biopolymers, Vol. Depsipeptides 163-175 ANIB1 Homo sapiens 71-74 12771887-1 2003 OBJECTIVE: Treating cancer cells with depsipeptide, a novel antitumor agent currently in a phase II clinical trial, causes potent upregulation of p21/WAF1 expression and cell arrest at G1 and G2 checkpoints. Depsipeptides 38-50 cyclin dependent kinase inhibitor 1A Homo sapiens 146-149 12771887-1 2003 OBJECTIVE: Treating cancer cells with depsipeptide, a novel antitumor agent currently in a phase II clinical trial, causes potent upregulation of p21/WAF1 expression and cell arrest at G1 and G2 checkpoints. Depsipeptides 38-50 cyclin dependent kinase inhibitor 1A Homo sapiens 150-154 12771887-7 2003 RESULTS: Flavopiridol completely abolished depsipeptide-mediated dose-dependent upregulation of p21/WAF1 expression. Depsipeptides 43-55 cyclin dependent kinase inhibitor 1A Homo sapiens 96-99 12771887-7 2003 RESULTS: Flavopiridol completely abolished depsipeptide-mediated dose-dependent upregulation of p21/WAF1 expression. Depsipeptides 43-55 cyclin dependent kinase inhibitor 1A Homo sapiens 100-104 12592335-0 2003 Depsipeptide (FR 901228) promotes histone acetylation, gene transcription, apoptosis and its activity is enhanced by DNA methyltransferase inhibitors in AML1/ETO-positive leukemic cells. Depsipeptides 0-12 RUNX family transcription factor 1 Homo sapiens 153-157 12592335-0 2003 Depsipeptide (FR 901228) promotes histone acetylation, gene transcription, apoptosis and its activity is enhanced by DNA methyltransferase inhibitors in AML1/ETO-positive leukemic cells. Depsipeptides 0-12 RUNX1 partner transcriptional co-repressor 1 Homo sapiens 158-161 12592335-2 2003 We hypothesized that depsipeptide (FR901228), a novel HDAC inhibitor evaluated in ongoing clinical trials, restores gene transcription and cell differentiation in AML1/ETO-positive cells. Depsipeptides 21-33 RUNX family transcription factor 1 Homo sapiens 163-167 12592335-2 2003 We hypothesized that depsipeptide (FR901228), a novel HDAC inhibitor evaluated in ongoing clinical trials, restores gene transcription and cell differentiation in AML1/ETO-positive cells. Depsipeptides 21-33 RUNX1 partner transcriptional co-repressor 1 Homo sapiens 168-171 12592335-3 2003 A dose-dependent increase in H3 and H4 histone acetylation was noted in depsipeptide-treated AML1/ETO-positive Kasumi-1 cells and blasts from a patient with t(8;21) AML. Depsipeptides 72-84 RUNX family transcription factor 1 Homo sapiens 93-97 12592335-3 2003 A dose-dependent increase in H3 and H4 histone acetylation was noted in depsipeptide-treated AML1/ETO-positive Kasumi-1 cells and blasts from a patient with t(8;21) AML. Depsipeptides 72-84 RUNX1 partner transcriptional co-repressor 1 Homo sapiens 98-101 12592335-6 2003 Notably, the activity of depsipeptide was enhanced by 5-aza-2"-deoxycytidine, a DNA methyltransferase inhibitor (DNMT). Depsipeptides 25-37 DNA methyltransferase 1 Homo sapiens 80-111 12592335-6 2003 Notably, the activity of depsipeptide was enhanced by 5-aza-2"-deoxycytidine, a DNA methyltransferase inhibitor (DNMT). Depsipeptides 25-37 DNA methyltransferase 1 Homo sapiens 113-117 12115133-3 2002 The structure of an 11-residue peptide Boc-Val-Ala-Leu-Aib-Val-Ala-Leu-Aib-Val-Ala-Leu-OMe (2), analog of a which is an amide previously determined Lac-containing depsipeptide, Boc-Val-Ala-Leu-Aib-Val-Lac-Leu-Aib-Val-Ala-Leu-OMe I. L. Karle, C. Das, and P. Balaram, Biopolymers, Vol. Depsipeptides 163-175 ANIB1 Homo sapiens 55-58 11753657-8 2001 Depsipeptide, an inhibitor of histone deacetylase, acts synergistically with 5-Aza-CdR in inducing expression of p16(INK4a) and p19(INK4d). Depsipeptides 0-12 cyclin dependent kinase inhibitor 2A Homo sapiens 113-116 11753657-8 2001 Depsipeptide, an inhibitor of histone deacetylase, acts synergistically with 5-Aza-CdR in inducing expression of p16(INK4a) and p19(INK4d). Depsipeptides 0-12 cyclin dependent kinase inhibitor 2A Homo sapiens 117-122 11753657-8 2001 Depsipeptide, an inhibitor of histone deacetylase, acts synergistically with 5-Aza-CdR in inducing expression of p16(INK4a) and p19(INK4d). Depsipeptides 0-12 cyclin dependent kinase inhibitor 2D Homo sapiens 128-131 11753657-8 2001 Depsipeptide, an inhibitor of histone deacetylase, acts synergistically with 5-Aza-CdR in inducing expression of p16(INK4a) and p19(INK4d). Depsipeptides 0-12 cyclin dependent kinase inhibitor 2D Homo sapiens 132-137 11753657-9 2001 However, when cells were treated with higher concentrations of 5-Aza-CdR and depsipeptide, p16(INK4a) expression was decreased together with significant suppression of cell growth. Depsipeptides 77-89 cyclin dependent kinase inhibitor 2A Homo sapiens 91-94 11753657-9 2001 However, when cells were treated with higher concentrations of 5-Aza-CdR and depsipeptide, p16(INK4a) expression was decreased together with significant suppression of cell growth. Depsipeptides 77-89 cyclin dependent kinase inhibitor 2A Homo sapiens 95-100 11753657-10 2001 Interestingly, p19(INK4d) expression was enhanced even more by the higher concentrations of 5-Aza-CdR and depsipeptide. Depsipeptides 106-118 cyclin dependent kinase inhibitor 2D Homo sapiens 15-18 11753657-10 2001 Interestingly, p19(INK4d) expression was enhanced even more by the higher concentrations of 5-Aza-CdR and depsipeptide. Depsipeptides 106-118 cyclin dependent kinase inhibitor 2D Homo sapiens 19-24 11472266-3 2001 The mechanism of anticancer activity of the cryptophycins has been associated with their destabilization of microtubules and with their induction of bcl-2 phosphorylation leading to apoptosis. Depsipeptides 44-57 BCL2 apoptosis regulator Homo sapiens 149-154 11592497-0 2001 SW-163C and E, novel antitumor depsipeptides produced by Streptomyces sp. Depsipeptides 31-44 solute carrier family 9 (sodium/hydrogen exchanger), member 1 Mus musculus 0-13 11443220-0 2001 Low concentrations of the histone deacetylase inhibitor, depsipeptide (FR901228), increase expression of the Na(+)/I(-) symporter and iodine accumulation in poorly differentiated thyroid carcinoma cells. Depsipeptides 57-69 histone deacetylase 9 Homo sapiens 26-45 11443220-0 2001 Low concentrations of the histone deacetylase inhibitor, depsipeptide (FR901228), increase expression of the Na(+)/I(-) symporter and iodine accumulation in poorly differentiated thyroid carcinoma cells. Depsipeptides 57-69 solute carrier family 5 member 5 Homo sapiens 109-129 11443220-4 2001 We examined the ability of the novel histone deacetylase (HDAC) inhibitor, depsipeptide (FR901228), to modulate the expression of thyroid-specific genes. Depsipeptides 75-87 histone deacetylase 9 Homo sapiens 37-56 11443220-4 2001 We examined the ability of the novel histone deacetylase (HDAC) inhibitor, depsipeptide (FR901228), to modulate the expression of thyroid-specific genes. Depsipeptides 75-87 histone deacetylase 9 Homo sapiens 58-62 11443220-6 2001 In these four cell lines, a very low concentration of depsipeptide (1 ng/mL) increased histone acetylation and expression of both thyroglobulin and the Na(+)/I(-) symporter messenger RNAs. Depsipeptides 54-66 solute carrier family 5 member 5 Homo sapiens 152-172 11443220-8 2001 Depsipeptide induced increases in (125)I accumulation indicated that a functional Na(+)/I(-) symporter protein was induced. Depsipeptides 0-12 solute carrier family 5 member 5 Homo sapiens 82-102 8811880-6 1996 We have used the same principle to synthesize internally quenched depsipeptide fluorogenic substrates based on resonance energy transfer between the donor/acceptor couple 5-[(2"-aminoethyl)amino]naphthalene sulfonic acid/4-[[4"-(dimethylamino)phenyl]azo]benzoic acid, and developed a continuous assay for NS3 activity. Depsipeptides 66-78 KRAS proto-oncogene, GTPase Homo sapiens 305-308 11265773-3 2001 The authors designed the current study to determine whether the histone deacetylase inhibitor, depsipeptide FR901228 (DP), could enhance NY-ESO-1 induction mediated by the DNA demethylating agent 5-Aza-2"-deoxycytidine (DAC) in cell lines established primarily from thoracic cancers. Depsipeptides 95-107 cancer/testis antigen 1A Homo sapiens 137-145 11269744-13 2001 Thus, cryptophycins are potent inducers of Bcl-2 phosphorylation. Depsipeptides 6-19 BCL2 apoptosis regulator Homo sapiens 43-48 11269744-14 2001 The cryptophycins were more potent cytotoxic agents in Bcl-2-negative Calu-6 cells than in Bcl-2-positive H460 cells indicating that pathways triggered by Bcl-2 phosphorylation are involved in cryptophycin-induced lethality. Depsipeptides 4-17 BCL2 apoptosis regulator Homo sapiens 55-60 11269744-14 2001 The cryptophycins were more potent cytotoxic agents in Bcl-2-negative Calu-6 cells than in Bcl-2-positive H460 cells indicating that pathways triggered by Bcl-2 phosphorylation are involved in cryptophycin-induced lethality. Depsipeptides 4-17 BCL2 apoptosis regulator Homo sapiens 91-96 11269744-14 2001 The cryptophycins were more potent cytotoxic agents in Bcl-2-negative Calu-6 cells than in Bcl-2-positive H460 cells indicating that pathways triggered by Bcl-2 phosphorylation are involved in cryptophycin-induced lethality. Depsipeptides 4-17 BCL2 apoptosis regulator Homo sapiens 91-96 10091686-1 1999 Analogs of the antitumor agents cryptophycins 1 and 8 with dialkyl substitution at C-6 (fragment C) were synthesized and evaluated for in vitro cytotoxicity against human leukemia cells (CCRF-CEM). Depsipeptides 32-45 complement C6 Homo sapiens 83-86 8980113-0 1996 Aureobasidin A, an antifungal cyclic depsipeptide antibiotic, is a substrate for both human MDR1 and MDR2/P-glycoproteins. Depsipeptides 30-49 ATP binding cassette subfamily B member 1 Homo sapiens 92-96 8980113-0 1996 Aureobasidin A, an antifungal cyclic depsipeptide antibiotic, is a substrate for both human MDR1 and MDR2/P-glycoproteins. Depsipeptides 30-49 ATP binding cassette subfamily B member 4 Homo sapiens 101-105 8980113-4 1996 The human MDR1/Pgp conferred about 4-fold resistance to aureobasidin A, a cyclic depsipeptide antifungal antibiotic, on the drug-sensitive yeast strains. Depsipeptides 81-93 ATP binding cassette subfamily B member 1 Homo sapiens 10-14 8980113-4 1996 The human MDR1/Pgp conferred about 4-fold resistance to aureobasidin A, a cyclic depsipeptide antifungal antibiotic, on the drug-sensitive yeast strains. Depsipeptides 81-93 ATP binding cassette subfamily B member 1 Homo sapiens 15-18 7854121-2 1994 The vanX gene was located downstream from genes encoding the VanA ligase and the VanH dehydrogenase which synthesize the depsipeptide D-alanyl-D-lactate (D-Ala-D-Lac). Depsipeptides 121-133 VanX Enterococcus faecalis 4-8 34463219-0 2021 Myxobacterial depsipeptide chondramides interrupt SARS-CoV-2 entry by targeting its broad, cell tropic spike protein. Depsipeptides 14-26 surface glycoprotein Severe acute respiratory syndrome coronavirus 2 103-108 8349413-7 1993 The possible use of Hib as an isosteric replacement for Aib in the design of conformationally constrained depsipeptides is briefly discussed. Depsipeptides 106-119 ANIB1 Homo sapiens 56-59 1391633-0 1992 Crystal and molecular structure of the depsipeptide ionophore hexadecaisoleucinomycin, cyclo-[(D-Ile-L-Lac-L-Ile-D-Hyi)4-] (C80H136N8O24). Depsipeptides 39-51 lactase Homo sapiens 103-106 1391633-1 1992 The crystal structure of a synthetic depsipeptide ionophore hexadecaisoleucinomycin, cyclo [-(D-Ile-L-Lac-L-Ile-D-Hyi)4-] (C80H136N8O24), has been determined by single crystal x-ray diffraction techniques. Depsipeptides 37-49 lactase Homo sapiens 102-105 2386810-3 1990 Depsipeptide analogues of the repeating sequences of elastin in which this 4----1 hydrogen bond cannot exist were synthesized. Depsipeptides 0-12 elastin Homo sapiens 53-60 1724618-3 1990 The cyclic peptide microcystin-LR (MLR) and the depsipeptides, valinomycin (VLM) and enniatin-B (ENB), bind to CaM and inhibit PDE activity. Depsipeptides 48-61 calmodulin 1 Homo sapiens 111-114 1510448-5 1992 VanY released the C-terminal D-hydroxy acid from depsipeptides produced by the vancomycin resistance protein VanA. Depsipeptides 49-62 VanY protein Enterococcus faecium 0-4 1510448-6 1992 These results demonstrate that VanY should contribute in vivo to the hydrolysis of both the D-alanyl-D-alanine- and the depsipeptide-containing peptidoglycan precursors. Depsipeptides 120-132 VanY protein Enterococcus faecium 31-35 915907-2 1977 A series of peptides and depsipeptides containing 2-methylcarbazic acid (H-Mec-OH), the 2-aza analogue of alanine, was prepared and tested as inhibitors of pancreatic and human granulocyte elastases. Depsipeptides 25-38 C-C motif chemokine ligand 28 Homo sapiens 75-78 34141065-6 2021 Herein we describe our first efforts in natural product inhibitor discovery leading to the identification of a depsipeptide class of natural products as RNA-binding inhibitors of Dicer-mediated miRNA processing. Depsipeptides 111-123 dicer 1, ribonuclease III Homo sapiens 179-184 6654588-4 1983 Starting from Hyb-Phe-Pro-ONp (V) two epimeric N(3-hydroxybutyryl)diketopiperazines (VI) and (VII) and the corresponding 10-membered cyclodepsipeptide (VIII) could be isolated. Depsipeptides 133-150 cytochrome c oxidase subunit 8A Homo sapiens 152-156 4634303-0 1972 [Biological activity of peptide and depsipeptide analogs of ophthalmic and norophthalmic acids in glyoxalase I and formaldehyde:NAD-oxidoreductase enzyme systems]. Depsipeptides 36-48 glyoxalase I Homo sapiens 98-110 32202785-0 2020 Design, Synthesis, and Conformation-Activity Study of Unnatural Bridged Bicyclic Depsipeptides as Highly Potent HIF-1 Inhibitors and Antitumor Agents. Depsipeptides 81-94 hypoxia inducible factor 1 subunit alpha Homo sapiens 112-117 33515365-4 2021 In the present work the effect of jasplakinolide, an actin-binding cyclodepsipeptide, on the SNTA1 protein activity and SNTA1 mediated downstream cellular events was studied in MDA-MB-231 breast cancer cell line. Depsipeptides 67-84 syntrophin alpha 1 Homo sapiens 93-98 33639168-1 2021 Heterotrimeric G protein subunits Galphaq and Galpha11 are inhibited by two cyclic depsipeptides, FR900359 (FR) and YM-254890 (YM), both of which are being used widely to implicate Gq/11 proteins in the regulation of diverse biological processes. Depsipeptides 76-96 G protein subunit alpha q Homo sapiens 34-41 33639168-1 2021 Heterotrimeric G protein subunits Galphaq and Galpha11 are inhibited by two cyclic depsipeptides, FR900359 (FR) and YM-254890 (YM), both of which are being used widely to implicate Gq/11 proteins in the regulation of diverse biological processes. Depsipeptides 76-96 G protein subunit alpha 11 Homo sapiens 46-54 28514117-5 2017 The suitability of the Ahp-cyclodepsipeptide scaffold for tailored inhibitor synthesis is showcased by the generation of the most potent human HTRA protease inhibitors to date. Depsipeptides 27-44 HtrA serine peptidase 1 Homo sapiens 143-147 30909817-8 2020 Thus, the study revealed new depsipeptides as potential HDAC8 inhibitors. Depsipeptides 29-42 histone deacetylase 8 Homo sapiens 56-61 31163697-2 2019 This natural 16-membered macrocyclic depsipeptide features an interesting side chain unit, namely 3-hydroxy-7-mercaptohept-4-enoic acid, which occurs in many other natural sulfur-containing HDAC inhibitors. Depsipeptides 37-49 histone deacetylase 9 Homo sapiens 190-194 30212625-0 2018 Depsipeptides Featuring a Neutral P1 Are Potent Inhibitors of Kallikrein-Related Peptidase 6 with On-Target Cellular Activity. Depsipeptides 0-13 kallikrein related peptidase 6 Homo sapiens 62-92 29265814-2 2018 The highly cytotoxic cyclodepsipeptides of the nannocystin family are known to bind to the eukaryotic translation elongation factor 1alpha (EF-1alpha). Depsipeptides 21-39 eukaryotic translation elongation factor 1 alpha 2 Homo sapiens 140-149 29494533-0 2018 ATG5 Promotes Death Signaling in Response to the Cyclic Depsipeptides Coibamide A and Apratoxin A. Depsipeptides 49-69 autophagy related 5 Mus musculus 0-4 30083689-0 2018 Chiral beta3-isocyanopropionates for multicomponent synthesis of peptides and depsipeptides containing a beta-amino acid fragment. Depsipeptides 78-91 eukaryotic translation elongation factor 1 beta 2 pseudogene 2 Homo sapiens 7-12 29235036-4 2018 Moreover, Alox15 expression was markedly upregulated by Class I HDAC inhibitors, MS-275 and depsipeptide. Depsipeptides 92-104 arachidonate 15-lipoxygenase Homo sapiens 10-16 28541699-2 2017 Kohamamides A, B, and C (1-3), new cyclic depsipeptides that belong to the kulolide superfamily, were isolated from an Okeania sp. Depsipeptides 35-55 homeobox C13 Homo sapiens 0-28 27509880-2 2016 In the present study, we found that a very low concentration of depsipeptide, an HDAC inhibitor, potentiated the antitumor activity of 5-fluorouracil (5-FU) in a human colon cancer cell model using HCT-116, HT29, and SW48 cells via the inhibition of colony formation ability or cellular viability. Depsipeptides 64-76 histone deacetylase 9 Homo sapiens 81-85 27509880-0 2016 Combination of the histone deacetylase inhibitor depsipeptide and 5-fluorouracil upregulates major histocompatibility complex class II and p21 genes and activates caspase-3/7 in human colon cancer HCT-116 cells. Depsipeptides 49-61 histone deacetylase 9 Homo sapiens 19-38 27509880-0 2016 Combination of the histone deacetylase inhibitor depsipeptide and 5-fluorouracil upregulates major histocompatibility complex class II and p21 genes and activates caspase-3/7 in human colon cancer HCT-116 cells. Depsipeptides 49-61 H3 histone pseudogene 16 Homo sapiens 139-142 27509880-3 2016 Exposure to a combination of 5-FU (1.75 microM) and 1 nM depsipeptide for 24 and 48 h resulted in a 3- to 4-fold increase in activated caspase-3/7, while 5-FU alone failed to activate caspase-3/7. Depsipeptides 57-69 caspase 3 Homo sapiens 135-144 27509880-0 2016 Combination of the histone deacetylase inhibitor depsipeptide and 5-fluorouracil upregulates major histocompatibility complex class II and p21 genes and activates caspase-3/7 in human colon cancer HCT-116 cells. Depsipeptides 49-61 caspase 3 Homo sapiens 163-174 27509880-3 2016 Exposure to a combination of 5-FU (1.75 microM) and 1 nM depsipeptide for 24 and 48 h resulted in a 3- to 4-fold increase in activated caspase-3/7, while 5-FU alone failed to activate caspase-3/7. Depsipeptides 57-69 caspase 3 Homo sapiens 135-146 26036758-9 2015 Importantly, increasing FOXO1 acetylation by a HDAC inhibitor, depsipeptide, overcomes TKI resistance to effectively induce TKI-resistant NSCLC cell apoptosis. Depsipeptides 63-75 forkhead box O1 Homo sapiens 24-29 27183222-2 2016 Pap-A is a cyclic depsipeptide that binds to PS in the membrane of wild-type Candida albicans, and permeabilizes its plasma membrane, ultimately causing cell death. Depsipeptides 11-30 pappalysin 1 Homo sapiens 0-5 26625202-2 2016 The pan-HDAC inhibitors AR-42 and SAHA, and the class I HDAC inhibitor depsipeptide, suppressed mammosphere formation and other CSC markers by reducing Notch1 expression in MDA-MB-231 and SUM-159 cells. Depsipeptides 71-83 histone deacetylase 9 Homo sapiens 56-60 26625202-2 2016 The pan-HDAC inhibitors AR-42 and SAHA, and the class I HDAC inhibitor depsipeptide, suppressed mammosphere formation and other CSC markers by reducing Notch1 expression in MDA-MB-231 and SUM-159 cells. Depsipeptides 71-83 notch receptor 1 Homo sapiens 152-158 27020600-1 2016 Beauveriolides I and III, which are naturally occurring cyclodepsipeptides, have been reported to bind to sterol O-acyltransferase (SOAT), inhibiting its ability to synthesize cholesteryl esters. Depsipeptides 56-74 sterol O-acyltransferase 1 Homo sapiens 106-130 27020600-1 2016 Beauveriolides I and III, which are naturally occurring cyclodepsipeptides, have been reported to bind to sterol O-acyltransferase (SOAT), inhibiting its ability to synthesize cholesteryl esters. Depsipeptides 56-74 sterol O-acyltransferase 1 Homo sapiens 132-136 24438145-0 2014 Depsipeptide and roxithromycin induce apoptosis of lymphoma cells by blocking extracellular signal-regulated kinase activation. Depsipeptides 0-12 mitogen-activated protein kinase 1 Mus musculus 78-115 25721083-6 2015 Other HDAC inhibitors, including trichostatin A, sodium butyrate, and depsipeptide, also activated IGF-1R signaling in vorinostat-resistant NSCLC cells. Depsipeptides 70-82 insulin like growth factor 1 receptor Homo sapiens 99-105 25128875-2 2014 Therefore a sensitive and specific bioanalytical high-throughput UHPLC-MS/MS method was developed for the quantitative and simultaneous determination of cyclic depsipeptide mycotoxins beauvericin and enniatins (A, A1, B, B1, D, E, C/F) in human skin Franz diffusion cell samples. Depsipeptides 153-172 immunoglobulin kappa variable 2D-30 Homo sapiens 214-234 22748705-1 2012 The linear depsipeptide grassystatin A, a valuable probe for the study of cathepsin E function, has been synthesized by a [4+6] strategy. Depsipeptides 11-23 cathepsin E Homo sapiens 74-85 23894374-2 2013 In fact, two histone deacetylase inhibitors (HDIs), SAHA and Depsipeptide, are FDA approved for single-agent treatment of refractory cutaneous T cell lymphoma (CTCL). Depsipeptides 61-73 TSPY like 2 Homo sapiens 160-164 23989727-2 2013 The antimycin-type depsipeptides are one such grouping, with a significant level of diversity and members that have noted activities against key targets governing human cellular apoptosis (e.g. Bcl-xL and GRP78). Depsipeptides 19-32 BCL2 like 1 Homo sapiens 194-200 23989727-2 2013 The antimycin-type depsipeptides are one such grouping, with a significant level of diversity and members that have noted activities against key targets governing human cellular apoptosis (e.g. Bcl-xL and GRP78). Depsipeptides 19-32 heat shock protein family A (Hsp70) member 5 Homo sapiens 205-210 24900634-3 2013 Here, we describe the design and preparation of a series of PYY(3-36) depsipeptide analogues, in which backbone amide-to-ester modifications were systematically introduced in the C-terminal. Depsipeptides 70-82 peptide YY Homo sapiens 60-63 21855532-0 2011 Glutathione-S-transferase pi 1(GSTP1) gene silencing in prostate cancer cells is reversed by the histone deacetylase inhibitor depsipeptide. Depsipeptides 127-139 glutathione S-transferase pi 1 Homo sapiens 0-30 22112863-5 2012 Depsipeptide induced oxidative stress was confirmed to relate to a disturbance in reduction-oxidation (redox) reactions through inhibition of the transactivation of thioredoxin reductase (TrxR) in human cancer cells. Depsipeptides 0-12 peroxiredoxin 5 Homo sapiens 165-186 22112863-5 2012 Depsipeptide induced oxidative stress was confirmed to relate to a disturbance in reduction-oxidation (redox) reactions through inhibition of the transactivation of thioredoxin reductase (TrxR) in human cancer cells. Depsipeptides 0-12 peroxiredoxin 5 Homo sapiens 188-192 22112863-6 2012 Upon treatment with depsipeptide, p53 phosphorylation at threonine 18 (Thr18) was specifically induced. Depsipeptides 20-32 tumor protein p53 Homo sapiens 34-37 22112863-8 2012 Our results demonstrate that depsipeptide plays an anti-neoplastic role by generating ROS to elicit p53/p21 pathway activation. Depsipeptides 29-41 tumor protein p53 Homo sapiens 100-103 22112863-8 2012 Our results demonstrate that depsipeptide plays an anti-neoplastic role by generating ROS to elicit p53/p21 pathway activation. Depsipeptides 29-41 H3 histone pseudogene 16 Homo sapiens 104-107 21987446-0 2011 The seminoma cell line TCam-2 is sensitive to HDAC inhibitor depsipeptide but tolerates various other chemotherapeutic drugs and loss of NANOG expression. Depsipeptides 61-73 histone deacetylase 9 Homo sapiens 46-50 21987446-6 2011 Here, we treated the seminoma-like cell line TCam-2 with the HDAC-inhibitor Depsipeptide, the global demethylating agent 5-aza-2"-deocycytidine, all-trans retinoic acid and the monaminooxidase inhibitor Tranylcipromine and also used knock down approaches to reduce expression of the pluripotency marker NANOG and/or the inhibitor of primordial germ cell differentiation TFAP2C. Depsipeptides 76-88 histone deacetylase 9 Homo sapiens 61-65 21362133-7 2011 In fact, two actively studied HDAC inhibitors, vorinostat and depsipeptide, were recently approved for the treatment of refractory cutaneous T cell lymphoma. Depsipeptides 62-74 histone deacetylase 9 Homo sapiens 30-34 21705224-6 2011 The porpoisamides are a unique pair of cyclic depsipeptides that are epimeric at C-2 of the beta-amino acid, 3-amino-2-methyloctanoic acid. Depsipeptides 39-59 complement C2 Homo sapiens 81-84 21855532-0 2011 Glutathione-S-transferase pi 1(GSTP1) gene silencing in prostate cancer cells is reversed by the histone deacetylase inhibitor depsipeptide. Depsipeptides 127-139 glutathione S-transferase pi 1 Homo sapiens 31-36 21855532-3 2011 We chose the GSTP1 gene which is silenced by hypermethylation to analyze the effect of the histone deacetylase inhibitor depsipeptide on DNA methylation and histone modifications at the GSTP1 promoter site. Depsipeptides 121-133 glutathione S-transferase pi 1 Homo sapiens 186-191 20361469-6 2010 In fact, vorinostat and depsipeptide, two actively studied HDAC inhibitors, were recently approved for the treatment of refractory cutaneous T-cell lymphoma. Depsipeptides 24-36 histone deacetylase 9 Homo sapiens 59-63 20811718-5 2010 In addition, we found that the combination of 30 microM zebularine and 6 or 7 nM depsipeptide resulted in a synergistic inhibition of cell growth in tumor cells with silenced CDKN2A (p<0.001, CI=0.70 and 0.57, respectively) but not in tumor cells with deleted CDKN2A. Depsipeptides 81-93 cyclin dependent kinase inhibitor 2A Homo sapiens 175-181 20811718-5 2010 In addition, we found that the combination of 30 microM zebularine and 6 or 7 nM depsipeptide resulted in a synergistic inhibition of cell growth in tumor cells with silenced CDKN2A (p<0.001, CI=0.70 and 0.57, respectively) but not in tumor cells with deleted CDKN2A. Depsipeptides 81-93 cyclin dependent kinase inhibitor 2A Homo sapiens 263-269 21879444-5 2011 Recently, the two HDAC inhibitors suberoylanilide hydroxamic acid (SAHA, Vorinostat) and Romidepsin (Depsipeptide, FK228) were FDA approved for the treatment of cutaneous T-cell lymphoma (CTCL). Depsipeptides 101-113 TSPY like 2 Homo sapiens 188-192 20811699-0 2010 Histone deacetylase inhibitors valproic acid and depsipeptide sensitize retinoblastoma cells to radiotherapy by increasing H2AX phosphorylation and p53 acetylation-phosphorylation. Depsipeptides 49-61 H2A.X variant histone Mus musculus 123-127 20811699-0 2010 Histone deacetylase inhibitors valproic acid and depsipeptide sensitize retinoblastoma cells to radiotherapy by increasing H2AX phosphorylation and p53 acetylation-phosphorylation. Depsipeptides 49-61 transformation related protein 53, pseudogene Mus musculus 148-151 20811699-2 2010 The present study showed that the histone deacetylase (HDAC) inhibitors valproic acid (VPA) and depsipeptide (FK228) synergistically enhanced ionizing radiation (IR)-induced apoptosis, associated with activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase in Y79 and WER1-Rb1 human retinoblastoma cells. Depsipeptides 96-108 caspase 3 Homo sapiens 215-224 20811699-2 2010 The present study showed that the histone deacetylase (HDAC) inhibitors valproic acid (VPA) and depsipeptide (FK228) synergistically enhanced ionizing radiation (IR)-induced apoptosis, associated with activation of caspase-3 and cleavage of poly(ADP-ribose) polymerase in Y79 and WER1-Rb1 human retinoblastoma cells. Depsipeptides 96-108 poly(ADP-ribose) polymerase 1 Homo sapiens 241-268 19233470-5 2009 It is shown that depsipeptide is effective at submicromolar concentrations and acts mainly by apoptosis induction, upregulation of p21 and cell cycle inhibition in G2/M. Depsipeptides 17-29 H3 histone pseudogene 16 Homo sapiens 131-134 19233470-7 2009 In summary, depsipeptide induced protein acetylation results in transcriptional changes of a large number of pathogenetically relevant genes and increased RelA/p65 binding activity in cHL cell lines. Depsipeptides 12-24 RELA proto-oncogene, NF-kB subunit Homo sapiens 155-159 19233470-7 2009 In summary, depsipeptide induced protein acetylation results in transcriptional changes of a large number of pathogenetically relevant genes and increased RelA/p65 binding activity in cHL cell lines. Depsipeptides 12-24 RELA proto-oncogene, NF-kB subunit Homo sapiens 160-163