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BCL2 inhibitor

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https://www.readbyqxmd.com/read/28224725/quisinostat-treatment-improves-histone-acetylation-and-developmental-competence-of-porcine-somatic-cell-nuclear-transfer-embryos
#1
Long Jin, Qing Guo, Hai-Ying Zhu, Xiao-Xu Xing, Guang-Lei Zhang, Mei-Fu Xuan, Qi-Rong Luo, Zhao-Bo Luo, Jun-Xia Wang, Xi-Jun Yin, Jin-Dan Kang
Abnormal epigenetic modifications are considered a main contributing factor to low cloning efficiency. In the present study, we explored the effects of quisinostat, a novel histone deacetylase inhibitor, on blastocyst formation rate in porcine somatic-cell nuclear transfer (SCNT) embryos, on acetylation of histone H3 lysine 9 (AcH3K9), and on expression of POU5F1 protein and apoptosis-related genes BAX and BCL2. Our results showed that treatment with 10 nM quisinostat for 24 h significantly improved the development of reconstructed embryos compared to the untreated group (19...
February 22, 2017: Molecular Reproduction and Development
https://www.readbyqxmd.com/read/28223017/novel-bcl2-inhibitor-disarib-induces-apoptosis-by-disruption-of-bcl2-bak-interaction
#2
Supriya V Vartak, Divyaanka Iyer, T R Santhoshkumar, Sheetal Sharma, Archita Mishra, Gunaseelan Goldsmith, Mrinal Srivastava, Shikha Srivastava, Subhas S Karki, Avadhesha Surolia, Bibha Choudhary, Sathees C Raghavan
Apoptosis is a highly regulated pathway of programmed cell death relying on the fine balance between pro and antiapoptotic binding partners. Overexpression of the antiapoptotic protein BCL2 in several cancers makes it an ideal target for chemotherapy, with minimum side effects. In one of our previous studies, we designed, synthesized and characterized Disarib, a BCL2-specific small molecule inhibitor. Interestingly, Disarib showed a novel mode of BCL2 inhibition, by predominantly binding to its BH1 domain, as compared to the BH3-specific action of other known BCL2 inhibitors...
February 18, 2017: Biochemical Pharmacology
https://www.readbyqxmd.com/read/28218232/corrigendum-thz1-targeting-cdk7-suppresses-stat-transcriptional-activity-and-sensitizes-t-cell-lymphomas-to-bcl2-inhibitors
#3
Florencia Cayrol, Pannee Praditsuktavorn, Tharu M Fernando, Nicholas Kwiatkowski, Rossella Marullo, M Nieves Calvo-Vidal, Jude Phillip, Benet Pera, Shao Ning Yang, Kaipol Takpradit, Lidia Roman, Marcello Gaudiano, Ramona Crescenzo, Jia Ruan, Giorgio Inghirami, Tinghu Zhang, Graciela Cremaschi, Nathanael S Gray, Leandro Cerchietti
No abstract text is available yet for this article.
February 20, 2017: Nature Communications
https://www.readbyqxmd.com/read/28216661/mir-194-5p-bclaf1-deregulation-in-aml-tumorigenesis
#4
C Dell'Aversana, C Giorgio, L D'Amato, G Lania, F Matarese, S Saeed, A Di Costanzo, V B Petrizzi, C Ingenito, J H A Martens, I Pallavicini, S Minucci, A Carissimo, H G Stunnenberg, L Altucci
Deregulation of epigenetic mechanisms, including miRNA, contributes to leukaemogenesis and drug resistance by interfering with cancer-specific molecular pathways. Here, we show that the balance between miR-194-5p and its newly discovered target BCL2-associated transcription factor 1 (BCLAF1) regulates differentiation and survival of normal haematopoietic progenitors. In acute myeloid leukaemias (AMLs) this balance is perturbed, locking cells into an immature, potentially 'immortal' state. Enhanced expression of miR-194-5p by treatment with the HDAC inhibitor SAHA or by exogenous miR-194-5p expression re-sensitizes cells to differentiation and apoptosis by inducing BCLAF1 to shuttle between nucleus and cytosol...
February 20, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28187446/targeting-of-apoptotic-pathways-by-smac-or-bh3-mimetics-distinctly-sensitizes-paclitaxel-resistant-triple-negative-breast-cancer-cells
#5
Effrosini G Panayotopoulou, Anna-Katharina Müller, Melanie Börries, Hauke Busch, Guohong Hu, Sima Lev
Standard chemotherapy is the only systemic treatment for triple-negative breast cancer (TNBC), and despite the good initial response, resistance remains a major therapeutic obstacle. Here, we employed a High-Throughput Screen to identify targeted therapies that overcome chemoresistance in TNBC. We applied short-term paclitaxel treatment and screened 320 small-molecule inhibitors of known targets to identify drugs that preferentially and efficiently target paclitaxel-treated TNBC cells. Among these compounds the SMAC mimetics (BV6, Birinapant) and BH3-mimetics (ABT-737/263) were recognized as potent targeted therapy for multiple paclitaxel-residual TNBC cell lines...
February 6, 2017: Oncotarget
https://www.readbyqxmd.com/read/28179288/aurora-b-inhibitor-tak-901-synergizes-with-bcl-xl-inhibition-by-inducing-active-bax-in-cancer-cells
#6
Saomi Murai, Jennifer Matuszkiewicz, Yuumi Okuzono, Hiroyuki Miya, Ron DE Jong
BACKGROUND: Aurora B kinase plays an essential role in chromosome segregation and cytokinesis, and is dysregulated in many cancer types, making it an attractive therapeutic target. TAK-901 is a potent aurora B inhibitor that showed efficacy in both in vitro and in vivo oncology models. MATERIALS AND METHODS: We conducted a synthetic lethal siRNA screening to identify the genes that, when silenced, can potentiate the cell growth-inhibitory effect of TAK-901. RESULTS: B-cell lymphoma-extra large (BCL-xL) depletion by siRNA or chemical inhibition synergized with TAK-901 in cancer cell lines...
2017: Anticancer Research
https://www.readbyqxmd.com/read/28178193/cearoin-induces-autophagy-erk-activation-and-apoptosis-via-ros-generation-in-sh-sy5y-neuroblastoma-cells
#7
Tonking Bastola, Ren-Bo An, Youn-Chul Kim, Jaehyo Kim, Jungwon Seo
Neuroblastomas are the most common solid extracranial tumors in childhood. We investigated the anticancer effect of cearoin isolated from Dalbergia odorifera in human neuroblastoma SH-SY5Y cells. SH-SY5Y cells were treated with various doses of cearoin. The viability was measured by MTT assay. DCFDA fluorescence assay and Griess assay were used for the measurement of intracellular reactive oxygen species (ROS) and nitric oxide (NO), respectively. Western blot analysis was performed to clarify the molecular pathway involved...
February 6, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28160853/identification-of-acetylshikonin-as-the-novel-cyp2j2-inhibitor-with-anti-cancer-activity-in-hepg2-cells
#8
See-Hyoung Park, Nguyen Minh Phuc, Jongsung Lee, Zhexue Wu, Jieun Kim, Hyunkyoung Kim, Nam Doo Kim, Taeho Lee, Kyung-Sik Song, Kwang-Hyeon Liu
BACKGROUND: Acetylshikonin is one of the biologically active compounds derived from the root of Lithospermum erythrorhizon, a medicinal plant with anti-cancer and anti-inflammation activity. Although there have been a few previous reports demonstrating that acetylshikonin exerts anti-cancer activity in vitro and in vivo, it is still not clear what is the exact molecular target protein of acetylshikonin in cancer cells. PURPOSE: The purpose of this study is to evaluate the inhibitory effect of acetylshikonin against CYP2J2 enzyme which is predominantly expressed in human tumor tissues and carcinoma cell lines...
January 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28158898/4pba-strongly-attenuates-endoplasmic-reticulum-stress-fibrosis-and-mitochondrial-apoptosis-markers-in-cyclosporine-treated-human-gingival-fibroblasts
#9
Suresh Ranga Rao, Subbarayan Rajasekaran, Supraja Ajitkumar, Murugan Girija Dinesh
Cyclosporine induces overgrowth of human gingiva. Previously we have shown (i) cyclosporine - inducing ER stress in human gingival fibroblasts, (ii) increased matrix protein expression, and (iii) interference with mitochondrial pro- and anti - apoptotic factors. This study was undertaken to assess the effects of melatonin (an antioxidant), 4PBA (an ER stress inhibitor), and simvastatin on the expression of ER Stress markers, as well as on matrix and mitochondrial markers. Human gingival fibroblasts incubated with cyclosporine, or without melatonin/4PBA/statin...
February 3, 2017: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/28157696/resveratrol-induces-mitochondria-mediated-caspase-independent-apoptosis-in-murine-prostate-cancer-cells
#10
Sanjay Kumar, Erdal Eroglu, James A Stokes, Karyn Scissum-Gunn, Sabita N Saldanha, Udai P Singh, Upender Manne, Selvarangan Ponnazhagan, Manoj K Mishra
Found in the skins of red fruits, including grapes, resveratrol (RES) is a polyphenolic compound with cancer chemopreventive activity. Because of this activity, it has gained interest for scientific investigations. RES inhibits tumor growth and progression by targeting mitochondria-dependent or -independent pathways. However, further investigations are needed to explore the underlying mechanisms.The present study is focused on examining the role of RES-induced, mitochondria-mediated, caspase-independent apoptosis of prostate cancer cells, namely transgenic adenocarcinoma of mouse prostate (TRAMP) cells...
February 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/28138710/moscatilin-induces-apoptosis-of-pancreatic-cancer-cells-via-reactive-oxygen-species-and-the-jnk-sapk-pathway
#11
Lei Zhang, Yuan Fang, Xue-Feng Xu, Da-Yong Jin
Moscatilin is a bibenzyl derivative extracted from the Dendrobium aurantiacum var. denneanum, which has traditionally been used as an immunomodulatory treatment in China. The present study was designed to determine whether moscatilin is a pro‑apoptotic agent in pancreatic cancer, and to elucidate the underlying mechanisms. The apoptotic and anti‑proliferative effects of moscatilin on pancreatic cancer cells were determined in vitro using biochemical assays, such as the MTT assay, colony formation assay, Hoechst staining and DNA fragmentation assay, and in vivo using Panc‑1 pancreatic cancer xenografts...
January 25, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28134252/thz1-targeting-cdk7-suppresses-stat-transcriptional-activity-and-sensitizes-t-cell-lymphomas-to-bcl2-inhibitors
#12
Florencia Cayrol, Pannee Praditsuktavorn, Tharu M Fernando, Nicholas Kwiatkowski, Rosella Marullo, M Nieves Calvo-Vidal, Jude Phillip, Benet Pera, Shao Ning Yang, Kaipol Takpradit, Lidia Roman, Marcello Gaudiano, Ramona Crescenzo, Jia Ruan, Giorgio Inghirami, Tinghu Zhang, Graciela Cremaschi, Nathanael S Gray, Leandro Cerchietti
Peripheral T-cell lymphomas (PTCL) are aggressive diseases with poor response to chemotherapy and dismal survival. Identification of effective strategies to target PTCL biology represents an urgent need. Here we report that PTCL are sensitive to transcription-targeting drugs, and, in particular, to THZ1, a covalent inhibitor of cyclin-dependent kinase 7 (CDK7). The STAT-signalling pathway is highly vulnerable to THZ1 even in PTCL cells that carry the activating STAT3 mutation Y640F. In mutant cells, CDK7 inhibition decreases STAT3 chromatin binding and expression of highly transcribed target genes like MYC, PIM1, MCL1, CD30, IL2RA, CDC25A and IL4R...
January 30, 2017: Nature Communications
https://www.readbyqxmd.com/read/28130250/the-bcl2-inhibitor-venetoclax-is-active-in-non-hodgkin-lymphoma
#13
(no author information available yet)
Venetoclax has single-agent antitumor activity in a range of non-Hodgkin lymphoma (NHL) subtypes.
January 27, 2017: Cancer Discovery
https://www.readbyqxmd.com/read/28122742/ex-vivo-drug-response-profiling-detects-recurrent-sensitivity-patterns-in-drug-resistant-all
#14
Viktoras Frismantas, Maria Pamela Dobay, Anna Rinaldi, Joelle Tchinda, Samuel H Dunn, Joachim Kunz, Paulina Richter-Pechanska, Blerim Marovca, Orrin Pail, Silvia Jenni, Ernesto Diaz-Flores, Bill H Chang, Timothy J Brown, Robert H Collins, Sebastian Uhrig, Gnana P Balasubramanian, Obul R Bandapalli, Salome Higi, Sabrina Eugster, Pamela Voegeli, Mauro Delorenzi, Gunnar Cario, Mignon L Loh, Martin Schrappe, Martin Stanulla, Andreas E Kulozik, Martina U Muckenthaler, Vaskar Saha, Julie A Irving, Roland Meisel, Thomas Radimerski, Arend Von Stackelberg, Cornelia Eckert, Jeffrey W Tyner, Peter Horvath, Beat C Bornhauser, Jean-Pierre Bourquin
Drug sensitivity and resistance testing on diagnostic leukemia samples should provide important functional information to guide actionable target and biomarker discovery. We provide proof of concept data by profiling 60 drugs on 68 acute lymphoblastic leukemia (ALL) samples mostly from resistant disease in co-cultures on bone marrow stromal cells. Patient-derived xenografts retained the original pattern of mutations found in the matched patient material. Stromal co-culture did not prevent leukemia cell cycle activity, while a specific sensitivity profile to cell cycle related drugs identified samples with higher cell proliferation both in vitro and in vivo as leukemia xenografts...
January 25, 2017: Blood
https://www.readbyqxmd.com/read/28111464/bruton-s-tyrosine-kinase-inhibition-increases-bcl-2-dependence-and-enhances-sensitivity-to-venetoclax-in-chronic-lymphocytic-leukemia
#15
J Deng, E Isik, S M Fernandes, J R Brown, A Letai, M S Davids
Although the BTK inhibitor ibrutinib has transformed the management of patients with chronic lymphocytic leukemia (CLL), it does not induce substantial apoptosis in vitro, and as such the mechanisms underlying its ability to kill CLL cells are not well understood. Acalabrutinib, a more specific BTK inhibitor now in development, also appears to be highly effective in CLL, but the connection of its mechanism with CLL cell death is also unclear. Using dynamic BH3 profiling, we analyzed alterations in the function of the mitochondrial apoptotic pathway induced by ibrutinib and acalabrutinib...
February 14, 2017: Leukemia: Official Journal of the Leukemia Society of America, Leukemia Research Fund, U.K
https://www.readbyqxmd.com/read/28103302/crude-extracts-flavokawain-b-and-alpinetin-compounds-from-the-rhizome-of-alpinia-mutica-induce-cell-death-via-uck2-enzyme-inhibition-and-in-turn-reduce-18s-rrna-biosynthesis-in-ht-29-cells
#16
Ibrahim Malami, Ahmad Bustamam Abdul, Rasedee Abdullah, Nur Kartinee Bt Kassim, Rozita Rosli, Swee Keong Yeap, Peter Waziri, Imaobong Christopher Etti, Muhammad Bashir Bello
Uridine-cytidine kinase 2 is an enzyme that is overexpressed in abnormal cell growth and its implication is considered a hallmark of cancer. Due to the selective expression of UCK2 in cancer cells, a selective inhibition of this key enzyme necessitates the discovery of its potential inhibitors for cancer chemotherapy. The present study was carried out to demonstrate the potentials of natural phytochemicals from the rhizome of Alpinia mutica to inhibit UCK2 useful for colorectal cancer. Here, we employed the used of in vitro to investigate the effectiveness of natural UCK2 inhibitors to cause HT-29 cell death...
2017: PloS One
https://www.readbyqxmd.com/read/28100580/venetoclax-in-patients-with-previously-treated-chronic-lymphocytic-leukemia
#17
Andrew W Roberts, Stephan Stilgenbauer, John F Seymour, David C S Huang
Venetoclax is the first BCL2 inhibitor to enter routine clinical practice. It is an orally bioavailable small molecule that binds BCL2 very specifically. Acting as a pharmacological mimic of the proteins that initiate apoptosis (a so-called BH3-mimetic), venetoclax rapidly induces apoptosis in chronic lymphocytic leukemia (CLL) cells which express high levels of BCL2 and rely on it to maintain their survival. As a single agent, daily venetoclax treatment induced durable responses in 79% of patients with relapsed or refractory CLL or small lymphocytic lymphoma in a Phase 1 study, including complete remissions in 20% of patients...
January 18, 2017: Clinical Cancer Research: An Official Journal of the American Association for Cancer Research
https://www.readbyqxmd.com/read/28099584/iodine-131-treatment-of-thyroid-cancer-cells-leads-to-suppression-of-cell-proliferation-followed-by-induction-of-cell-apoptosis-and-cell-cycle-arrest-by-regulation-of-b-cell-translocation-gene-2-mediated-jnk-nf-%C3%AE%C2%BAb-pathways
#18
L M Zhao, A X Pang
Iodine-131 (131I) is widely used for the treatment of thyroid-related diseases. This study aimed to investigate the expression of p53 and BTG2 genes following 131I therapy in thyroid cancer cell line SW579 and the possible underlying mechanism. SW579 human thyroid squamous carcinoma cells were cultured and treated with 131I. They were then assessed for 131I uptake, cell viability, apoptosis, cell cycle arrest, p53 expression, and BTG2 gene expression. SW579 cells were transfected with BTG2 siRNA, p53 siRNA and siNC and were then examined for the same aforementioned parameters...
January 16, 2017: Brazilian Journal of Medical and Biological Research, Revista Brasileira de Pesquisas Médicas e Biológicas
https://www.readbyqxmd.com/read/28057912/mir-340-inhibits-proliferation-and-induces-apoptosis-in-gastric-cancer-cell-line-sgc-7901-possibly-via-the-akt-pathway
#19
Jinzhong Yu, Ruijie Wang, Jianshe Chen, Jinfeng Wu, Zhongqin Dang, Qinsheng Zhang, Bo Li
BACKGROUND Gastric cancer is among the most common types of cancer, with high morbidity and mortality. MicroRNAs (miRNAs) play vital roles in the tumorigenesis and biology of gastric cancer. This study aimed to reveal the role of miR-340 in gastric cancer cell proliferation and apoptosis and to elucidate the potential mechanisms. MATERIAL AND METHODS Human gastric cancer cells SGC-7901 were used in this study for cell transfection with miR-340 mimic or inhibitor. After transfection, cell viability, proliferation, and apoptosis were examined by MTT, BrdU, and flow cytometry assays, respectively...
January 6, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28054503/inhibition-of-telomerase-using-bibr1532-enhances-doxorubicin-induced-apoptosis-in-pre-b-acute-lymphoblastic-leukemia-cells
#20
Davood Bashash, Mohadeseh Zareii, Ava Safaroghli-Azar, Mir Davood Omrani, Seyed H Ghaffari
OBJECTIVES: Interest into targeting telomerase in cancer has increased by the recent disclosure that elevated telomerase activity is associated with disease recurrence and poor outcome in cancers. In addition, cellular acquisition of unlimited replicative potential, which is closely related to the maintenance of telomeres mostly via the reactivation of telomerase, has been shown to confer loss of sensitivity to a wide range of anti-neoplastic agents. METHODS: To evaluate whether telomerase inhibition using non-nucleosidic inhibitor of telomerase BIBR1532 could enhance cytotoxic effect of doxorubicin in acute lymphoblastic leukemia, Nalm-6 pre-B ALL cells were subjected to combination treatment and subsequent cell viability, growth kinetics, caspase-3 activity, and transcriptional alteration of p73, p21, FOXO3a, c-Myc, hTERT, and other apoptosis-related target genes were investigated...
January 5, 2017: Hematology (Amsterdam, Netherlands)
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