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Bcl-2 protein inhibitors

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https://www.readbyqxmd.com/read/28430601/growth-suppressive-activity-of-raloxifene-on-liver-cancer-cells-by-targeting-il-6-gp130-signaling
#1
Yina Wang, Haiyan Ma, Chongqiang Zhao, Tianshu Liu, Dan Yan, David Jou, Huameng Li, Cuntai Zhang, Jiagao Lü, Chenglong Li, Jiayuh Lin, Sheng Li, Li Lin
BACKGROUND: Interleukin-6 (IL-6) is a multifunctional cytokine, which is involved in the regulation of differentiation and growth of certain types of tumor cells. Constitutive activation of Signal Transducer and Activator of Transcription 3 (STAT3) induced by IL-6 is frequently detected in liver cancer and has emerged as a viable molecular target for liver cancer treatment. However, few inhibitors targeting up-streams of STAT3 are available for the therapy of liver cancer. We reported the discovery of EVISTA (Raloxifene HCl) as novel inhibitor of IL-6/GP130 protein-protein interactions (PPIs) using multiple ligand simultaneous docking (MLSD) and drug repositioning...
April 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28428059/the-decreased-growth-performance-and-impaired-immune-function-and-structural-integrity-by-dietary-iron-deficiency-or-excess-are-associated-with-tor-nf-%C3%AE%C2%BAb-p38mapk-nrf2-and-mlck-signaling-in-head-kidney-spleen-and-skin-of-grass-carp-ctenopharyngodon-idella
#2
Yan-Lin Guo, Wei-Dan Jiang, Pei Wu, Yang Liu, Xiao-Qiu Zhou, Sheng-Yao Kuang, Ling Tang, Wu-Neng Tang, Yong-An Zhang, Lin Feng
This study was conducted to investigate the effects of dietary iron on the growth, and immune function and structural integrity in head kidney, spleen and skin as well as the underlying signaling of young grass carp (Ctenopharyngodon idella). Total 630 grass carp (242.32 ± 0.58 g) were fed diets containing graded levels of iron at 12.15 (basal diet), 35.38, 63.47, 86.43, 111.09, 136.37 mg/kg (diets 2-6 were added with ferrous fumarate) and 73.50 mg/kg (diet 7 was added with ferrous sulfate) diet for 60 days...
April 17, 2017: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/28420864/insulin-growth-factor-1-protects-neural-stem-cells-against-apoptosis-induced-by-hypoxia-through-akt-mitogen-activated-protein-kinase-extracellular-signal-regulated-kinase-akt-mapk-erk-pathway-in-hypoxia-ishchemic-encephalopathy
#3
Bing Zhao, Zebao Zheng
BACKGROUND Insulin growth factor 1 (IGF-1) is reported to modulate cell growth and acts as potential therapy for traumatic brain injury. This study was designed to investigate the effect of IGF-1 on hypoxia-induced apoptosis in neural stem cells (NSCs). MATERIAL AND METHODS A hypoxia model was constructed using NSCs separated from the hippocampus of rat. NSCs were divided into four groups: cells under normoxic conditions that acted as controls (C group), cells under hypoxia (H group), cells under hypoxia with IGF-1 (HI group), and cells under hypoxia with IGF-1 as well as picropodophyllin (PPP), which acts as an inhibitor of the IGF-1 receptor (HIP group)...
April 19, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28419994/degradation-of-mcl-1-through-gsk-3%C3%AE-activation-regulates-apoptosis-induced-by-bufalin-in-non-small-cell-lung-cancer-h1975-cells
#4
Xiao-Hong Kang, Jing-Hang Zhang, Qing-Qin Zhang, Yan-Hui Cui, Ying Wang, Wei-Zheng Kou, Zhan-Hui Miao, Ping Lu, Li-Fang Wang, Zhen-Ye Xu, Fei Cao
BACKGROUND/AIMS: Mcl-1, an anti-apoptotic Bcl-2 family member, is often overexpressed in non-small cell lung cancer (NSCLC). Bufalin has been reported to induce apoptosis in various tumor cells. However, there is no report showing that bufalin could downregulate Mcl-1 expression in NSCLC. METHODS: Cell proliferation was analyzed by cell counting kit-8 (CCK-8) assay in H1975 cells. Cell apoptosis was detected by flow cytometry. Mcl-1 mRNA was detected by RT-PCR. The expression of apoptosis-associated proteins in H1975 cells was detected by western blotting...
April 14, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28419846/bit1-regulates-cell-migration-and-survival-in-oral-squamous-cell%C3%A2-carcinoma
#5
Yan Xiao, Yanjie Yang, Jing Wang, Wenlu Li
PURPOSE: Increasing evidence has shown that Bcl-2 inhibitor of transcription 1 (Bit1) involves a variety of biological processes in the process of tumor development and progression. We hypothesized that Bit1 would be overexpressed in oral squamous cell carcinoma (OSCC); therefore, we examined Bit1 gene expression and protein production, as well as explored the effect of elevated Bit1 levels on OSCC cells. MATERIALS AND METHODS: We investigated the use of quantitative real-time reverse transcription-polymerase chain reaction and immunohistochemistry analysis for Bit1 messenger RNA and protein levels...
March 23, 2017: Journal of Oral and Maxillofacial Surgery
https://www.readbyqxmd.com/read/28418907/bh3-mimetics-and-bet-inhibitors-elicit-enhanced-lethality-in-malignant-glioma
#6
Chiaki Tsuge Ishida, Elena Bianchetti, Chang Shu, Marc-Eric Halatsch, Mike-Andrew Westhoff, Georg Karpel-Massler, Markus D Siegelin
Drug combination therapies remain pivotal for the treatment of heterogeneous malignancies, such as glioblastomas. Here, we show a novel lethal interaction between Bcl-xL and c-myc inhibition accomplished by bromodomain protein inhibitors. Established, patient-derived xenograft and stem cell-like glioma cells were treated with the novel bromodomain protein inhibitors, JQ1 and OTX015, along with BH3-mimetics, ABT263 or Obatoclax. Synergy was assessed by calculation of CI values. Small interfering RNAs (siRNAs) were used for gene silencing and mechanistic studies...
March 18, 2017: Oncotarget
https://www.readbyqxmd.com/read/28415755/mitochondrial-matrix-chaperone-and-c-myc-inhibition-causes-enhanced-lethality-in-glioblastoma
#7
Chiaki Tsuge Ishida, Chang Shu, Marc-Eric Halatsch, Mike-Andrew Westhoff, Dario C Altieri, Georg Karpel-Massler, Markus David Siegelin
Malignant gliomas display high levels of the transcription factor c-myc and organize a tumor specific chaperone network within mitochondria. Here, we show that c-myc along with mitochondrial chaperone inhibition displays massive tumor cell death. Inhibition of mitochondrial matrix chaperones and c-myc was established by utilizing genetic as well as pharmacological approaches. Bromodomain and extraterminal (BET) family protein inhibitors, JQ1 and OTX015, were used for c-myc inhibition. Gamitrinib was applied to interfere with mitochondrial matrix chaperones...
March 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28413637/correlation-of-survivin-and-b-cell-lymphoma-2-expression-with-pathological-malignancy-and-anti-apoptotic-properties-of-glial-cell-tumors
#8
In-Suk Bae, Choong-Hyun Kim, Jae-Min Kim, Jin-Hwan Cheong, Je-Il Ryu, Myung-Hoon Han
Apoptosis, whose mechanism remains unclear, is regulated by multiple factors. B-cell lymphoma 2 (Bcl-2) is a well-known anti-apoptotic mediator. Survivin is also a recently recognized novel family inhibitor of apoptosis protein, which inhibits apoptosis via a pathway distinct from Bcl-2 family members. Survivin and Bcl-2 are expressed in various types of human cancer. In the present study, survivin and Bcl-2 expression were characterized in glial cell tumors, and the correlation with pathological malignancy and anti-apoptotic properties were investigated...
April 2017: Biomedical Reports
https://www.readbyqxmd.com/read/28411243/potent-vasoconstrictor-kisspeptin-10-induces-atherosclerotic-plaque-progression-and-instability-reversal-by-its-receptor-gpr54-antagonist
#9
Kengo Sato, Remina Shirai, Mina Hontani, Rina Shinooka, Akinori Hasegawa, Tomoki Kichise, Tomoyuki Yamashita, Hayami Yoshizawa, Rena Watanabe, Taka-Aki Matsuyama, Hatsue Ishibashi-Ueda, Shinji Koba, Youichi Kobayashi, Tsutomu Hirano, Takuya Watanabe
BACKGROUND: Kisspeptin-10 (KP-10), a potent vasoconstrictor and inhibitor of angiogenesis, and its receptor, GPR54, have currently received much attention in relation to pre-eclampsia. However, it still remains unknown whether KP-10 could affect atherogenesis. METHODS AND RESULTS: We evaluated the effects of KP-10 on human umbilical vein endothelial cells, human monocyte-derived macrophages, human aortic smooth muscle cells in vitro, and atherosclerotic lesions in apolipoprotein E-deficient (ApoE(-/-)) mice in vivo...
April 14, 2017: Journal of the American Heart Association
https://www.readbyqxmd.com/read/28411240/structural-basis-of-apoptosis-inhibition-by-the-fowlpox-virus-protein-fpv039
#10
Mohd Ishtiaq Anasir, Sofia Caria, Michael A Skinner, Marc Kvansakul
Programmed cell death or apoptosis of infected host cells is an important defense mechanism in response to viral infections. This process is regulated by pro-apoptotic and pro-survival members of the B-cell lymphoma 2 (Bcl-2) protein family. To counter premature death of a virus-infected cell, poxviruses use a range of different molecular strategies, including the mimicry of pro-survival Bcl-2 proteins. One such viral pro-survival protein is the fowlpox virus protein FPV039, which is a potent apoptosis inhibitor, but the precise molecular mechanism by which FPV039 inhibits apoptosis is unknown...
April 14, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28410209/mir-106b-inhibitors-sensitize-trail-induced-apoptosis-in-hepatocellular-carcinoma-through-increase-of-death-receptor-4
#11
Changlong Xu, Liang Shi, Weilai Chen, Peipei Fang, Jie Li, Lingxiang Jin, Zhenzhen Pan, Chenwei Pan
TNF-related apoptosis-inducing ligand (TRAIL), which is a member of the TNF superfamily, can induce tumor cell apoptosis. However, multiple types of tumor, including hepatocellular carcinoma, show tolerance to TRAIL. Previous studies have demonstrated that tumor cells usually change their expression profile of microRNA (miRNA) to obtain the ability of tolerance to drugs. However, whether such change of miRNA on TRAIL sensitivity is seen in hepatocellular carcinoma still needs to be explored. In this study, we observed overexpression of miR-106b in both HCC patients' tumor tissues and cell lines...
March 30, 2017: Oncotarget
https://www.readbyqxmd.com/read/28409209/2-acetyl-5-tetrahydroxybutyl-imidazole-thi-protects-661w-cells-against-oxidative-stress
#12
Carlotta Fabiani, Aida Zulueta, Fabiola Bonezzi, Josefina Casas, Riccardo Ghidoni, Paola Signorelli, Anna Caretti
Retinal degeneration and in particular retinitis pigmentosa (RP) is associated to ceramide (Cer) accumulation and cell death induction. Cer and sphingosine-1-phosphate (S1P) belong to the sphingolipids class and exert a pro-apoptotic and pro-survival activity, respectively. Our aim is to target sphingolipid metabolism by inhibiting S1P lyase that regulates one of the S1P degradation pathways, to reduce retinal photoreceptor damage. The murine 661W cone-like cell line was pretreated with THI, an inhibitor of S1P lyase and exposed to H2O2-induced oxidative stress...
April 13, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/28408883/alisol-a-24-acetate-and-alisol-b-23-acetate-induced-autophagy-mediates-apoptosis-and-nephrotoxicity-in-human-renal-proximal-tubular-cells
#13
Chunfei Wang, Liang Feng, Liang Ma, Haifeng Chen, Xiaobin Tan, Xuefeng Hou, Jie Song, Li Cui, Dan Liu, Juan Chen, Nan Yang, Jing Wang, Ying Liu, Bingjie Zhao, Gang Wang, Yuanli Zhou, Xiaobin Jia
Two natural compounds alisol A 24-acetate (24A) and alisol B 23-acetate (23B) are abundant in Rhizoma alismatis. In the present study, we evaluated the induction of 24A and 23B on apoptosis and possible nephrotoxicity of human renal proximal tubular (HK-2) cells by activating autophagy and also explored its regulation on PI3K/Akt/mTOR signaling pathway. Presently, Clusterin, Kim-1, and TFF-3 were considered to be new bioindicators of nephrotoxicity. Interestingly, the protein expression and mRNA levels of Clusterin, Kim-1 and TFF-3 could be significantly increased by 23B and 24A in vivo and in vitro...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28408839/dnmt1-regulates-human-endometrial-carcinoma-cell-proliferation
#14
Xinjing Wang, Bilan Li
Endometrial carcinoma (EC) is the most common gynecologic malignancy, but the molecular events involved in the development and progression of EC remain unclear. This study aimed to investigate the role of DNA methyltransferase 1 (DNMT1), a member of DNA methyltransferases, in EC. AN3CA cells were transfected with DNMT1 siRNA. The proliferation, cell cycle, and apoptosis of AN3CA cells were evaluated by Cell Counting Kit-8 (CCK-8) assay and flow cytometry. The expression of related genes was detected by polymerase chain reaction and Western blot analysis...
2017: OncoTargets and Therapy
https://www.readbyqxmd.com/read/28405681/maspin-suppresses-growth-proliferation-and-invasion-in-cutaneous-squamous-cell-carcinoma-cells
#15
Hong Zhu, Qing Mao, Weiwei Liu, Zhenhai Yang, Xiaoqing Jian, Le Qu, Chundi He
Cutaneous squamous cell carcinoma (cSCC) is a common malignant tumor. Mammary serine protease inhibitor (Maspin), a member of serpin family, has been reported as a tumor suppressor in various carcinomas. In this study, we detected the expression level of Maspin in cSCC tissues by real-time PCR and western blotting, and found that Maspin was downregulated in the cSCC tissues compared with the adjacent normal tissues. Moreover, Maspin was stably overexpressed in A431 cells, and CCK-8 assay, colony formation assay, Transwell assay, Hoechst staining and western blotting were carried out to detect the growth, proliferation, invasion, cell cycle and apoptosis of A431 cells...
May 2017: Oncology Reports
https://www.readbyqxmd.com/read/28404874/identification-of-jl1037-as-a-novel-specific-reversible-lysine-specific-demethylase-1-inhibitor-that-induce-apoptosis-and-autophagy-of-aml-cells
#16
Shuang Liu, Wenting Lu, Shouyun Li, Saisai Li, Jia Liu, Yuanyuan Xing, Shuzu Zhang, Joe Zhongxiang Zhou, Haiyan Xing, Yingxi Xu, Qing Rao, Chengjun Deng, Min Wang, Jianxiang Wang
Lysine-specific demethylase 1 (LSD1) has been recognized as a potential therapeutic target for acute myeloid leukemia (AML). Herein, we identified a novel LSD1 inhibitor, JL1037, via Computer Aided Drug Design technology. JL1037 is a potent, selective and reversible LSD1 inhibitor with IC50s of 0.1 μM and >1.5 μM for LSD1 and monoamine oxidases A/B (MAO-A/B), respectively. Treatment of THP-1 and Kasumi-1 cell lines with JL1037 resulted in dose dependent accumulation of H3K4me1 and H3K4me2, the major substrates of LSD1, as well as inhibition of cell proliferation, blockade of cell cycle and induction of apoptosis...
March 29, 2017: Oncotarget
https://www.readbyqxmd.com/read/28396364/novel-indole-based-tambjamine-analogues-induce-apoptotic-lung-cancer-cell-death-through-p38-mitogen-activated-protein-kinase-activation
#17
Pilar Manuel-Manresa, Luís Korrodi-Gregório, Elsa Hernando, Alberto Villanueva, David Martínez-García, Ananda M Rodilla, Ricard Ramos, Margarida Fardilha, Juan Moya, Roberto Quesada, Vanessa Soto-Cerrato, Ricardo Perez-Tomas
Lung cancer has become the leading killer cancer worldwide, due to late diagnosis and lack of efficient anticancer drugs. We have recently described novel natural-derived tambjamine analogues that are potent anion transporters capable of disrupting cellular ion balance, inducing acidification of the cytosol and hyperpolarization of cellular plasma membranes. Although these tambjamine analogues were able to compromise cell survival, their molecular mechanism of action remains largely unknown. Herein we characterize the molecular cell responses induced by highly active indole-based tambjamine analogues treatment in lung cancer cells...
April 10, 2017: Molecular Cancer Therapeutics
https://www.readbyqxmd.com/read/28395566/wt1-protein-is-cleaved-by-caspase-3-in-apoptotic-leukemic-cells
#18
Jichen Ruan, Shenmeng Gao, Junjun Yang, Haiying Li, He Huang, Xiaoqun Zheng
The aberrant overexpression of Wilms' tumor-1 gene (WT1) plays an important role in blast cell survival and resistance to chemotherapy in acute myeloid leukemia (AML). Here, we found in chemotherapeutic drug etoposide-induced apoptosis, WT1 protein was cleaved into smaller fragment by caspase-3 in leukemic cells. The cleavage was blocked by pan-caspase inhibitor and special caspase-3 inhibitor, suggesting that caspase-3 might cleave WT1 protein. Furthermore, recombinant active caspase-3 cleaved the Flag-WT1 and GST-WT1 proteins in vitro...
April 10, 2017: Leukemia & Lymphoma
https://www.readbyqxmd.com/read/28395449/-o-glcnac-glycosylation-influences-the-biological-behaviors-and-etoposide-induced-apoptosis-of-nalm-6-cells
#19
B Zhang, D Li, Q Shi, X L Ju
Objective: To explore the effects of O-GlcNAc glycosylation and its key enzyme OGT on the biological behaviors and etoposide (Vp16) -induced apoptosis of Nalm-6 cells. Methods: Low O-GlcNAc modified Nalm-6 cells model was established with Alloxan, an inhibitor of OGT. The influence of Alloxan on Nalm-6 cells proliferation was checked by CCK-8 assay, apoptosis and cell cycle by flow cytometry. Nalm-6 cells were treated with different concentrations of Vp16 for 12 h, and then the O-GlcNAc level and the expressions of OGT were examined by Western blot...
March 14, 2017: Zhonghua Xue Ye Xue za Zhi, Zhonghua Xueyexue Zazhi
https://www.readbyqxmd.com/read/28395284/indole-3-carbinol-induces-apoptosis-of-hepatic-stellate-cells-through-k63-de-ubiquitination-of-rip1-in-rats
#20
Bin Li, Meng Cong, Yanan Zhu, Ying Xiong, Wenyi Jin, Yang Wan, Yunjiao Zhou, Ying Ao, Hui Wang
BACKGROUND/AIMS: The apoptosis of activated hepatic stellate cells (HSCs) is the central event in the reversal of liver fibrosis. K63 de-ubiquitinated receptor-interacting protein (RIP)1 promotes apoptosis in tumor necrosis factor (TNF)-α signaling pathway. In the previous study, we have proved that indole-3-carbinol (I3C) could reverse different models of liver fibrosis in rats, but the mechanism is still unclear. Thus, the present research aimed to demonstrate the induction of I3C on apoptosis of HSCs and the underlying molecular mechanism...
March 24, 2017: Cellular Physiology and Biochemistry
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