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Bcl-2 protein inhibitors

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https://www.readbyqxmd.com/read/28735240/therapeutic-effects-of-l-cysteine-in-newborn-mice-subjected-to-hypoxia-ischemia-brain-injury-via-the-cbs-h2s-system-role-of-oxidative-stress-and-endoplasmic-reticulum-stress
#1
Song Liu, Danqing Xin, Lingxiao Wang, Tiantian Zhang, Xuemei Bai, Tong Li, Yunkai Xie, Hao Xue, Shishi Bo, Dexiang Liu, Zhen Wang
Neonatal hypoxic-ischemic (HI) injury is a major cause of neonatal death and neurological dysfunction. H2S has been shown to protect against hypoxia-induced injury and apoptosis of neurons. L-Cysteine is catalyzed by cystathionine-β-synthase (CBS) in the brain and sequentially produces endogenous H2S. The present study was designed to investigate whether L-Cysteine could attenuate the acute brain injury and improve neurobehavioral outcomes following HI brain injury in neonatal mice by releasing endogenous H2S...
July 14, 2017: Redox Biology
https://www.readbyqxmd.com/read/28731145/piezo1-protein-induces-the-apoptosis-of-human-osteoarthritis-derived-chondrocytes-by-activating-caspase-12-the-signaling-marker-of-er-stress
#2
Xiao-Fei Li, Zhao Zhang, Zhu-Ke Chen, Zhao-Wei Cui, Hai-Ning Zhang
The present study was carried out to determine whether the mechanically activated cation channel Piezo1 protein plays a role as a signaling pathway which causes the apoptosis of human chondrocytes. The chondrocytes were isolated, cultured, and then subjected to mechanical stretch force for 0, 2, 12, 24 and 48 h, respectively. The expression levels of Piezo1 and the apoptosis-related protein caspase-12 were assessed by reverse transcription-quantitative polymerase chain reaction, as well as the apoptosis-related genes, B cell lymphoma/leukemia-2 (Bcl-2), Bcl-associated X protein (Bax) and Bcl-2-associated death promoter (BAD)...
July 19, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/28731137/phosphorylation-of-bcl-2-plays-an-important-role-in-glycochenodeoxycholate-induced-survival-and-chemoresistance-in-hcc
#3
Maojun Zhou, Qi Zhang, Jinfeng Zhao, Mingmei Liao, Sailan Wen, Manyi Yang
Hepatocellular carcinoma (HCC) is a highly malignant tumor and can evolve rapidly to resistance to chemotherapies. Glycochenodeoxycholate (GCDA), which is toxic and hydrophobic, is the main ingredient in the bile and associated with carcinogenesis of gastrointenstinal tumors. Bcl-2 is the most important anti-apoptotic protein and overexpressed in various human tumors. In the present study, we found that GCDA can induce the chemoresistance of human liver cancer cells and specific depletion of Bcl-2 by RNA interference blocks GCDA-stimulated chemoresistance, which indicate the pivotal role of Bcl-2 in such process...
July 18, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28731136/mhy451-induces-cell-cycle-arrest-and-apoptosis-by-ros-generation-in-hct116-human-colorectal-cancer-cells
#4
Na Lam Hwang, Yong Jung Kang, Bokyung Sung, Seong Yeon Hwang, Jung Yoon Jang, Hye Jin Oh, Yu Ra Ahn, Do Hyun Kim, Su Jeong Kim, Sultan Ullah, Mohammad Akbar Hossain, Hyung Ryong Moon, Hae Young Chung, Nam Deuk Kim
Colorectal cancer (CRC) is the third most frequently diagnosed cancer and cause of cancer-related deaths. Despite advancements in conventional therapeutic approaches to CRC, most patients with CRC die of their disease. There is a need to develop novel therapeutic agents for this malignancy. Therefore, the present study aimed to examine the anticancer effects and elucidate the underlying mechanism of MHY451 in HCT116 human colorectal cancer cells. Treatment with MHY451 inhibited cell growth in a time- and concentration-dependent manner...
July 18, 2017: Oncology Reports
https://www.readbyqxmd.com/read/28729825/dexmedetomidine-protects-mouse-brain-from-ischemia-reperfusion-injury-via-inhibiting-neuronal-autophagy-through-up-regulating-hif-1%C3%AE
#5
Cong Luo, Ming-Wen Ouyang, Ying-Ying Fang, Shu-Ji Li, Quan Zhou, Jun Fan, Zai-Sheng Qin, Tao Tao
Stroke is the leading cause of death in China and produces a heavy socio-economic burden in the past decades. Previous studies have shown that dexmedetomidine (DEX) is neuroprotective after cerebral ischemia. However, the role of autophagy during DEX-mediated neuroprotection after cerebral ischemia is still unknown. In this study, we found that post-conditioning with DEX and DEX+3-methyladenine (3-MA) (autophagy inhibitor) reduced brain infarct size and improved neurological deficits compared with DEX+RAPA (autophagy inducer) 24 h after transient middle cerebral artery artery occlusion (tMCAO) model in mice...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28728293/-curcumin-induces-apoptosis-and-protective-autophagy-in-human-gastric-cancer-cells-with-different-degree-of-differentiation
#6
W Li, Y Zhou, J Yang, H H Zhang, S L Zhao, T Zhang, J Huo, P Zheng
Objective: To investigate the effect of curcumin on the apoptosis and autophagy of human gastric cancer cells with different degree of differentiation. Methods: Gastric cancer cell lines BGC-823 and MKN-28 were treated with curcumin at different concentrations. The effect of curcumin on cell proliferation was measured by MTT assay. Apoptosis was assessed by flow cytometry. Autophagy status was analyzed by acridine orange staining. The expression levels of apoptotic and autophagy-related proteins were detected by Western blot...
July 23, 2017: Zhonghua Zhong Liu za Zhi [Chinese Journal of Oncology]
https://www.readbyqxmd.com/read/28724603/effects-of-microrna-136-on-melanoma-cell-proliferation-apoptosis-and-epithelial-mesenchymal-transition-by-targeting-pmel-through-the-wnt-signaling-pathway
#7
Jiu-Jiang Wang, Zhi-Feng Li, Xiao-Jing Li, Zhao Han, Ling Zhang, Zhi-Jun Liu
The study aims to evaluate the effects of miR-136 on the proliferation, apoptosis and epithelial mesenchymal transition (EMT) of melanoma cells by targeting PMEL through the Wnt signaling pathway. After establishment of melanoma mouse models, melanoma (model group) and normal tissues (normal group) were collected. Immunohistochemistry was performed to determine PMEL protein concentration. Mouse melanoma cells were assigned into control, blank, negative control (NC), miR-136 mimics, miR-136 inhibitors, siRNA-PMEL, and miR-136 inhibitors + siRNA-PMEL, LiC1 (Wnt signaling pathway activator) and siRNA-PMEL+ LiCl groups...
July 19, 2017: Bioscience Reports
https://www.readbyqxmd.com/read/28714472/targeting-the-differential-addiction-to-anti-apoptotic-bcl-2-family-for-cancer-therapy
#8
Akane Inoue-Yamauchi, Paul S Jeng, Kwanghee Kim, Hui-Chen Chen, Song Han, Yogesh Tengarai Ganesan, Kota Ishizawa, Sylvia Jebiwott, Yiyu Dong, Maria C Pietanza, Matthew D Hellmann, Mark G Kris, James J Hsieh, Emily H Cheng
BCL-2 family proteins are central regulators of mitochondrial apoptosis and validated anti-cancer targets. Using small cell lung cancer (SCLC) as a model, we demonstrated the presence of differential addiction of cancer cells to anti-apoptotic BCL-2, BCL-XL or MCL-1, which correlated with the respective protein expression ratio. ABT-263 (navitoclax), a BCL-2/BCL-XL inhibitor, prevented BCL-XL from sequestering activator BH3-only molecules (BH3s) and BAX but not BAK. Consequently, ABT-263 failed to kill BCL-XL-addicted cells with low activator BH3s and BCL-XL overabundance conferred resistance to ABT-263...
July 17, 2017: Nature Communications
https://www.readbyqxmd.com/read/28714369/sporamin-induces-apoptosis-and-inhibits-nf-%C3%AE%C2%BAb-activation-in-human-pancreatic-cancer-cells
#9
Cuijuan Qian, Xiaoying Chen, Yongxiao Qi, Sheng Zhong, Xinyan Gao, Wenjun Zheng, Zhixiang Mao, Jun Yao
Sporamin, a Kunitz-type trypsin inhibitor (TI) from sweet potato tuberous roots, has demonstrated anti-tumor activity through poorly defined mechanisms. Furthermore, the effects of sporamin on pancreatic cancer have not been explored. Herein, we studied the effects of sporamin on two human pancreatic cancer cell lines, PANC-1 and BxPC-3. Sporamin significantly inhibited the cell viability and proliferation activity and induced apoptosis in PANC-1 and BxPC-3 cells. Consistently, in sporamin-treated PANC-1 and BxPC-3 cells, the anti-apoptotic proteins Bcl-2 and Bcl-XL were downregulated and the pro-apoptotic protein Bax was upregulated...
July 2017: Tumour Biology: the Journal of the International Society for Oncodevelopmental Biology and Medicine
https://www.readbyqxmd.com/read/28714004/expression-and-function-of-transforming-growth-factor%C3%A2-%C3%AE-%C3%A2-activated-protein-kinase-1-in-gastric-cancer
#10
Yue Yang, Yudong Qiu, Mubai Tang, Zhaoshu Wu, Weidong Hu, Chaobo Chen
The present study aimed to investigate the expression and role of transforming growth factor (TGF) ‑β‑activated protein kinase 1 (TAK1) in human gastric cancer. Immunohistochemistry was performed to investigate the expression of TAK1 in surgical specimens of human gastric cancer tissue and adjacent normal tissue. The association between TAK1 and clinicopathologic factors was analyzed and the association between TAK1 expression and the overall survival rates was evaluated using Kaplan‑Meier curves. In addition, the effect of the TAK1 selective inhibitor 5Z‑7‑oxozeaenol (OZ) on the biological characteristics of MGC803 human gastric cancer cells in vitro were investigated...
September 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28713932/human-trypsin-inhibitor-reduces-the-apoptosis-of-lipopolysaccharide%C3%A2-induced-human-kidney%C3%A2-2-cells-by-promoting-mitochondrial-fusion
#11
Ning Liu, Zhiyi Jiang, Yongjun Liu, Yao Nie, Juan Chen, Bin Ouyang, Xiangdong Guan, Minying Chen
Imbalance in mitochondrial fusion/fission is one of the mechanisms leading to sepsis‑induced mitochondrial dysfunction and cell apoptosis. The present study examined the effects of human trypsin inhibitor (UTI), a well‑known antioxidant and anti‑inflammatory substance, on mitochondrial dynamics and cell apoptosis in lipopolysaccharide (LPS)‑induced human kidney‑2 (HK‑2) cells. The HK‑2 cells were incubated for 24 h either with LPS (800 ng/ml) or LPS (800 ng/ml) mixed with UTI (250 U/ml). Cell viability was assessed using a3‑(4,5‑dimethyl‑2‑thiazolyl)‑2, 5‑diphenyl‑2‑H‑tetrazolium bromide assay...
September 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28713907/roles-of-mir%C3%A2-4463-in-h2o2%C3%A2-induced-oxidative-stress-in-human-umbilical-vein-endothelial-cells
#12
Xueqin Wang, Xuemei He, Xian Deng, Yanzheng He, Xiangyu Zhou
Oxidative stress is implicated in the pathophysiology of vascular diseases, including atherosclerosis, aneurysm and arteriovenous fistula. A previous study from our lab suggested that microRNA (miR)‑4463 may be involved in the pathogenesis of vascular disease; however, the roles of oxidative stress in the molecular mechanisms underlying the actions of miR‑4463 in vascular disease have yet to be elucidated. The aim of the present study was to investigate the role of miR‑4463 in hydrogen peroxide (H2O2)‑induced oxidative stress in human umbilical vein endothelial cells (HUVECs)...
September 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28713162/abt-263-induces-g1-g0-phase-arrest-apoptosis-and-autophagy-in-human-esophageal-cancer-cells-in-vitro
#13
Qing-Huan Lin, Fu-Chang Que, Chun-Ping Gu, De-Sheng Zhong, Dan Zhou, Yi Kong, Le Yu, Shu-Wen Liu
Both the anti- and pro-apoptotic members of the Bcl-2 family are regulated by a conserved Bcl-2 homology (BH3) domain. ABT-263 (Navitoclax), a novel BH3 mimetic and orally bioavailable Bcl-2 family inhibitor with high affinity for Bcl-xL, Bcl-2 and Bcl-w has entered clinical trials for cancer treatment. But the anticancer mechanisms of ABT-263 have not been fully elucidated. In this study we investigated the effects of ABT-263 on human esophageal cancer cells in vitro and to explore its anticancer mechanisms...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28712306/targeting-intrinsic-apoptosis-and-other-forms-of-cell-death-by-bh3-mimetics-in-glioblastoma
#14
Georg Karpel-Massler, Chiaki Tsuge Ishida, Yiru Zhang, Marc-Eric Halatsch, M-Andrew Westhoff, Markus D Siegelin
Novel approaches to treat malignant brain tumors are necessary since these neoplasms still display an unfavorable prognosis. Areas covered: In this review, the authors summarize and analyze recent preclinical data that suggest that targeting intrinsic apoptosis may be a suitable strategy for the treatment of malignant gliomas. They focus on the anti-apoptotic Bcl-2 family members of proteins and the recent drug developments in that field with a special focus on BH3-mimetics. With the discovery of BH3-mimetics that interfere with anti-apoptotic Bcl-2 family members in the low nanomolar range significant excitement has been generated towards these class of inhibitors, such as ABT-737, ABT-263 and the most recent successor, ABT-199 which is most advanced with respect to clinical application...
July 17, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28710745/the-pan-bcl2-inhibitor-at101-activates-the-intrinsic-apoptotic-pathway-and-causes-dna-damage-in-acute-myeloid-leukemia-stem-like-cells
#15
Leisi Zhang, Yong Zhou, Kai Chen, Pengcheng Shi, Yin Li, Manman Deng, Zhiwu Jiang, Xiangmeng Wang, Peng Li, Bing Xu
BACKGROUND: Leukemia stem cells (LSCs) are considered to be the cause of treatment failure and relapse in acute myeloid leukemia (AML). Overexpression of the Bcl-2 family of anti-apoptotic proteins such as Bcl-2, Bcl-xl, and Mcl-1 accounts for survival and self-renewal of LSCs. AT101 binds to the BH3 motif of all Bcl-2 family anti-apoptotic proteins and demonstrates anti-tumor activity in multiple types of tumor. Thus, we hypothesized that this agent might have the potential to deplete LSCs...
July 14, 2017: Targeted Oncology
https://www.readbyqxmd.com/read/28710022/taxifolin-reduces-the-cholesterol-oxidation-product-induced-neuronal-apoptosis-by-suppressing-the-akt-and-nf-%C3%AE%C2%BAb-activation-mediated-cell-death
#16
Arum Kim, Yoon Jeong Nam, Chung Soo Lee
The taxifolin effect on the cholesterol oxidation product-induced neuronal apoptosis was investigated using differentiated PC12 cells and human neuroblastoma SH-SY5Y cells. 7-ketocholesterol induced phosphorylation of Akt, and increase in the levels of cytosolic and nuclear NF-κB p65, cytosolic NF-κB p50 and cytosolic phosphorylated-IκB-α in PC12 cells. The cholesterol oxidation products also induced a decrease in the levels of Bid and Bcl-2, increase in the levels of p53 and Bax, loss of the mitochondrial transmembrane potential, release of cytochrome c, activation of caspases (-8, -9 and -3), production of reactive oxygen species, depletion of GSH and cell death in both cell lines...
July 11, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28705421/bcl-2-inhibitors-as-anti-cancer-therapeutics-the-impact-of-and-on-calcium-signaling
#17
REVIEW
Tamara Vervloessem, Martijn Kerkhofs, Rita M La Rovere, Flore Sneyers, Jan B Parys, Geert Bultynck
Bcl-2-protein family members are essential regulators of apoptosis. Anti-apoptotic Bcl-2 proteins ensure cell survival via different mechanisms, including via binding of pro-apoptotic Bcl-2-family members and the modulation of intracellular Ca(2+)-transport systems. Many cancer cells upregulate these proteins to overcome the consequences of ongoing oncogenic stress. Bcl-2 inhibition leading to cell death, therefore emerged as a novel cancer therapy. Different Bcl-2 inhibitors have already been developed including the hydrophobic cleft-targeting BH3 mimetics, which antagonize Bcl-2's ability to scaffold and neutralize pro-apoptotic Bcl-2-family members...
June 4, 2017: Cell Calcium
https://www.readbyqxmd.com/read/28701864/induction-of-forkhead-class-box-o3a-and-apoptosis-by-a-standardized-ginsenoside-formulation-kg-135-is-potentiated-by-autophagy-blockade-in-a549-human-lung-cancer-cells
#18
Chih-Jung Yao, Jyh-Ming Chow, Shuang-En Chuang, Chia-Lun Chang, Ming-De Yan, Hsin-Lun Lee, I-Chun Lai, Pei-Chun Lin, Gi-Ming Lai
BACKGROUND: KG-135, a standardized formulation enriched with Rk1, Rg3, and Rg5 ginsenosides, has been shown to inhibit various types of cancer cells; however, the underlying mechanisms are not fully understood. In this study, we explored its effects in A549 human lung cancer cells to investigate the induction of Forkhead Class box O3a (FOXO3a) and autophagy. METHODS: Cell viability was determined by sulforhodamine B staining. Apoptosis and cell cycle distribution were analyzed using flow cytometry...
July 2017: Journal of Ginseng Research
https://www.readbyqxmd.com/read/28698127/dietary-protein-levels-regulated-antibacterial-activity-inflammatory-response-and-structural-integrity-in-the-head-kidney-spleen-and-skin-of-grass-carp-ctenopharyngodon-idella-after-challenged-with-aeromonas-hydrophila
#19
Wei-Dan Jiang, Jing Xu, Xiao-Qiu Zhou, Pei Wu, Yang Liu, Jun Jiang, Sheng-Yao Kuang, Ling Tang, Wu-Neng Tang, Yong-An Zhang, Lin Feng
This study investigated the effects of dietary protein levels on disease resistance, immune function and structural integrity in the head kidney, spleen and skin of grass carp (Ctenopharyngodon idella). A total of 540 grass carp (264.11 ± 0.76 g) were fed six diets containing graded levels of protein (143.1, 176.7, 217.2, 257.5, 292.2 and 322.8 g digestible protein kg(-1) diet) for 8 weeks. After the growth trial, fish were challenged with Aeromonas hydrophila for 14 days. The results indicated that optimal levels of dietary protein: (1) (1) increased the lysozyme (LA) and acid phosphatase (ACP) activities and the complement 3 (C3) and C4 contents, up-regulated antimicrobial peptides, anti-inflammatory cytokines, inhibitor of κBα, target of rapamycin and ribosomal protein S6 kinases 1 mRNA levels, whereas down-regulated pro-inflammatory cytokines, nuclear factor kappa B (NF-κB) P65, IKKβ, IKKγ, eIF4E-binding proteins (4E-BP) 1 and 4E-BP2 mRNA levels in the head kidney, spleen and skin of grass carp (P < 0...
July 8, 2017: Fish & Shellfish Immunology
https://www.readbyqxmd.com/read/28696828/small-molecule-inhibitor-tw-37-is-tolerable-and-synergistic-with-chemotherapy-in-nasopharyngeal-carcinoma
#20
Ying Lu, Haixin Huang, Hui Yang, Dagui Chen, Sibei Wu, Zhou Jiang, Rensheng Wang
Chemotherapy is a crucial adjuvant therapy of advanced nasopharyngeal carcinoma (NPC). However, enhancing sensitivity and tolerance of chemotherapeutics in NPC treatment have been challenging. Both Bcl-2 and Mcl-1, 2 pro-survival proteins of Bcl-2 family, play essential roles on the chemotherapy tolerance of numerous cancers. In the present study, we explored the influences of TW-37, a small molecule inhibitor of Bcl-2 and Mcl-1, on the efficiency of chemotherapy for NPC. Oncomine cancer database shows that NPC tissues have higher expression of Bcl-2 and Mcl-1 than those of normal nasopharyngeal epithelial (NPE) tissues...
July 11, 2017: Cell Cycle
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