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https://www.readbyqxmd.com/read/28910973/lycorine-inhibits-the-growth-and-metastasis-of-breast-cancer-through-the-blockage-of-stat3-signaling-pathway
#1
Jian Wang, Jie Xu, Guoqiang Xing
Signal transducer and activator of transcription 3 (STAT3) is involved in the growth and metastasis of breast cancer, and represents a potential target for developing new anti-tumor drugs. The purpose of this study is to investigate whether Lycorine, a pyrrolo[de]phenanthridine ring-type alkaloid extracted from Amaryllidaceae genera, could inhibit breast cancer by targeting STAT3 signaling pathway. The human breast cancer cell lines were incubated with various concentrations of Lycorine, and cell proliferation, colony formation, cell cycle distribution, apoptosis, migration and invasion were assayed by several in vitro approaches...
September 1, 2017: Acta Biochimica et Biophysica Sinica
https://www.readbyqxmd.com/read/28905990/the-mtor-kinase-inhibitor-everolimus-synergistically-enhances-the-anti-tumor-effect-of-the-bruton-s-tyrosine-kinase-btk-inhibitor-pls-123-on-mantle-cell-lymphoma
#2
Jiao Li, Xiaogan Wang, Yan Xie, Zhitao Ying, Weiping Liu, Lingyan Ping, Chen Zhang, Zhengying Pan, Ning Ding, Yuqin Song, Jun Zhu
Mantle cell lymphoma (MCL) is an aggressive and incurable malignant disease. Despite of general chemotherapy, relapse and mortality are common, highlighting the need for the development of novel targeted drugs or combination of therapeutic regimens. Recently, several drugs that target the B-cell receptor (BCR) signaling pathway, especially the Bruton's tyrosine kinase (BTK) inhibitor ibrutinib, have demonstrated notable therapeutic effects in relapsed/refractory patients, which indicate that pharmacological inhibition of BCR pathway holds promise in MCL treatment...
September 14, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28903337/targeting-the-apoptotic-mcl-1-puma-interface-with-a-dual-acting-compound
#3
Jiyuan Liu, Zhen Tian, Nan Zhou, Xueying Liu, Chenyi Liao, Beilei Lei, Jianing Li, Shengyong Zhang, Hui Chen
Despite intensive efforts in the search for small molecules with anti-cancer activity, it remains challenging to achieve both high effectiveness and safety, since many agents lack the selectivity to only act on cancer cells. The interface of two apoptotic proteins, myeloid cell leukemia-1 (Mcl-1) and p53 upregulated modulator of apoptosis (PUMA), has been recently affirmed as a target for treating cancers, as the disruption of Mcl-1-PUMA binding can reduce cancer cell survival and protect normal cells from apoptosis...
August 15, 2017: Oncotarget
https://www.readbyqxmd.com/read/28901269/recent-advances-in-cancer-drug-development-targeting-induced-myeloid-cell-leukemia-1-mcl-1-differentiation-protein
#4
Mohammad Abid, Yogesh A Sonawane, Jacob I Contreras, Sandeep Rana, Amarnath Natarajan
BACKGROUND: Anti-apoptotic members of the Bcl-2 family of proteins are upregulated in a majority of cancers and are potential therapeutic targets. Fragment-based design led to the development of clinical candidates that target Bcl-xL/Bcl-2. Although these Bcl-xL/Bcl-2 inhibitors showed promise in pre-clinical studies, resistance was observed to several Bcl-xL inhibitors, when used alone. This has been attributed to the over-expression of Mcl-1, another member of the Bcl-2 family of proteins...
September 11, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28892004/arenobufagin-induces-apoptotic-cell-death-in-human-non-small-cell-lung-cancer-cells-via-the-noxa-related-pathway
#5
Liang Ma, Yindi Zhu, Sheng Fang, Hongyan Long, Xiang Liu, Zi Liu
Arenobufagin, an active component isolated from the traditional Chinese medicine Chan Su, exhibits anticancer influences in several human malignancies. However, the effects and action mechanisms of arenobufagin on non-small-cell lung cancer (NSCLC) are still unknown. In this study, we reported that arenobufagin acted through activation of Noxa-related pathways and promoted apoptotic cell death in human NSCLC cells. Our results revealed that arenobufagin-induced apoptosis was caspase-dependent, as evidenced by the fact that caspase-9, caspase-3 and poly (ADP-ribose) polymerase (PARP) were cleaved, and pretreatment with a pan-caspase inhibitor Z-VAD-FMK inhibited the pro-apoptosis effect of arenobufagin...
September 11, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28885268/n1-guanyl-1-7-diaminoheptane-enhances-the-chemosensitivity-of-acute-lymphoblastic-leukemia-cells-to-vincristine-through-inhibition-of-eif5a-2-activation
#6
Yanhui Liu, Fei Xue, Yin Zhang, Pingchong Lei, Zhen Wang, Zunmin Zhu, Kai Sun
N1-guanyl-1,7-diaminoheptane (GC7), a deoxyhypusine synthase inhibitor, has been shown to exert antiproliferation effects in many solid tumors by regulating eukaryotic translation initiation factor 5a2 (eif5a-2). However, little is known about the role of GC7 and eif5a-2 in drug resistance in acute lymphoblastic leukemia (ALL). In the present study, we investigated the effect of GC7 on drug-resistant ALL and its potential mechanism. We found that using the CCK-8 assay that combined treatment with GC7 and vincristine (VCR) significantly inhibited the cell viability of two ALL cell lines...
September 6, 2017: Anti-cancer Drugs
https://www.readbyqxmd.com/read/28881742/eribulin-alone-or-in-combination-with-the-plk1-inhibitor-bi-6727-triggers-intrinsic-apoptosis-in-ewing-sarcoma-cell-lines
#7
Lilly Magdalena WeiΔ, Manuela Hugle, Simone Fulda
In this study, we investigated the molecular mechanisms of eribulin-induced cell death and its therapeutic potential in combination with the PLK1 inhibitor BI 6727 in Ewing sarcoma (ES). Here, we show that eribulin triggers cell death in a dose-dependent manner in a panel of ES cell lines. In addition, eribulin at subtoxic, low nanomolar concentrations acts in concert with BI 6727 to induce cell death and to suppress long-term clonogenic survival. Mechanistic studies reveal that eribulin monotherapy at cytotoxic concentrations and co-treatment with eribulin at subtoxic concentrations together with BI 6727 arrest cells in the M phase of the cell cycle prior to the onset of cell death...
August 8, 2017: Oncotarget
https://www.readbyqxmd.com/read/28881661/combination-of-fe-cu-chelators-and-docosahexaenoic-acid-an-exploration-for-the-treatment-of-colorectal-cancer
#8
Nanhui Yu, Hong Zhu, Yuan Yang, Yiming Tao, Fengbo Tan, Qian Pei, Yuan Zhou, Xiangping Song, Qiurong Tan, Haiping Pei
Colorectal cancer (CRC) is one of the major causes of cancer deaths in the world. 5-fluorouracil (5-FU) -based chemotherapy is a common choice for patients with CRC; unfortunately, the benefit is rather limited due to the acquisition of drug resistance. Therefore, the alternative therapeutic strategies are required. The activation of autophagic mechanism was considered as the main cause of the acquisition of drug resistance in 5-FU treatment. Docosahexaenoic acid (DHA), a fatty acid, has been regarded as an efficient anticancer agent and can improve the drug resistance in conventional cancer therapy by a low basal level of autophagy in colon cancer cells...
August 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/28881582/metformin-requires-4e-bps-to-induce-apoptosis-and-repress-translation-of-mcl-1-in-hepatocellular-carcinoma-cells
#9
Mamatha Bhat, Akiko Yanagiya, Tyson Graber, Nataliya Razumilava, Steve Bronk, Domenick Zammit, Yunhao Zhao, Chadi Zakaria, Peter Metrakos, Michael Pollak, Nahum Sonenberg, Gregory Gores, Maritza Jaramillo, Masahiro Morita, Tommy Alain
Metformin inhibits the mammalian target of rapamycin complex 1 (mTORC1) signaling pathway, which is frequently upregulated in hepatocellular carcinoma (HCC). Metformin has also been shown to induce apoptosis in this cancer. Here, we investigate whether metformin-induced apoptosis in HCC is mediated by the downstream mTORC1 effectors eukaryotic initiation factor 4E and (eIF4E)-binding proteins (4E-BPs). Further, we ask whether changes in 4E-BPs activity during metformin treatment negatively regulate translation of the anti-apoptotic myeloid cell leukemia 1 (Mcl-1) mRNA...
August 1, 2017: Oncotarget
https://www.readbyqxmd.com/read/28875977/the-life-and-death-of-immune-cell-types-the-role-of-bcl-2-anti-apoptotic-molecules
#10
REVIEW
Emma M Carrington, David M Tarlinton, Daniel H Gray, Nicholas D Huntington, Yifan Zhan, Andrew M Lew
Targeting survival mechanisms of immune cells may provide an avenue for immune intervention to dampen unwanted responses (e.g. autoimmunity, immunopathology and transplant rejection) or enhance beneficial ones (e.g. immune deficiency, microbial defence and cancer immunotherapy). The selective survival mechanisms of the various immune cell types also avails the possibility of specific tailoring of such interventions. Here, we review the role of the BCL-2 anti-apoptotic family members (BCL-2, BCL-XL, BCL-W, MCL-1 and A1) on cell death/survival of the major immune cell types e...
September 6, 2017: Immunology and Cell Biology
https://www.readbyqxmd.com/read/28873083/sklb188-inhibits-the-growth-of-head-and-neck-squamous-cell-carcinoma-by-suppressing-egfr-signalling
#11
Mansoureh Barzegar, Shuang Ma, Chao Zhang, Xin Chen, Ying Gu, Chaowei Shang, Xiaojuan Jiang, Jiao Yang, Cherie-Ann Nathan, Shengyong Yang, Shile Huang
BACKGROUND: Overexpression of epidermal growth factor receptor (EGFR) occurs in approximately 90% of head and neck squamous cell carcinoma (HNSCC), and is correlated with poor prognosis. Thus, targeting EGFR is a promising strategy for treatment of HNSCC. Several small molecule EGFR inhibitors have been tested in clinical trials for treatment of HNSCC, but none of them are more effective than the current chemotherapeutic drugs. Thus, it is urgently needed to develop novel EGFR inhibitors for HNSCC treatment...
September 5, 2017: British Journal of Cancer
https://www.readbyqxmd.com/read/28866374/1-phenyl-1h-indole-derivatives-as-a-new-class-of-bcl-2-mcl-1-dual-inhibitors-design-synthesis-and-preliminary-biological-evaluation
#12
Guangsen Xu, Tingting Liu, Yi Zhou, Xinying Yang, Hao Fang
Bcl-2 proteins, such as B-cell lymphoma (Bcl-2) protein, myeloid cell leukemia sequence 1 (Mcl-1) protein, has been implicated in the progression and survival of multiple tumor types and become a validated and attractive target for cancer therapy. In this work, a series of 1-phenyl-1H-indole derivatives has been designed and synthesized. The preliminary biological studies (binding assay for Bcl-2 proteins and MTT assay) suggested that some active compounds showed potent inhibitory activities on Bcl-2/Mcl-1 without binding on Bcl-XL...
August 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28863158/c-flip-and-the-noxa-mcl-1-axis-participate-in-the-synergistic-effect-of-pemetrexed-plus-cisplatin-in-human-choroidal-melanoma-cells
#13
Xiaofei Zhao, Feng Kong, Lei Wang, Han Zhang
Choroidal melanoma is the most common primary malignant intraocular tumor, and very few effective therapies are available to treat it. Our study aimed to understand whether pemetrexed plus cisplatin exerts a beneficial synergistic effect in human choroidal melanoma cells and to delineate the underlying molecular mechanism. To accomplish these aims, we treated choroidal melanoma cells with pemetrexed and cisplatin and assessed cell survival with SRB and MTT assays. Proteins were detected using western blotting analysis...
2017: PloS One
https://www.readbyqxmd.com/read/28859986/kribb11-accelerates-mcl-1-degradation-through-an-hsf1-independent-mule-dependent-pathway-in-a549-non-small-cell-lung-cancer-cells
#14
Min-Jung Kang, Hye Hyeon Yun, Jeong-Hwa Lee
The Bcl-2 family protein, Mcl-1 is known to have anti-apoptotic functions, and depletion of Mcl-1 by cellular stresses favors the apoptotic process. Moreover, Mcl-1 levels are frequently increased in various cancer cells, including non-small cell lung cancer (NSCLC), and is implicated in resistance to conventional chemotherapy and in cancer metastasis. In this study, we demonstrated that KRIBB11 accelerates the proteasomal degradation of Mcl-1 in the NSCLC cell line, A549. While KRIBB11 is an inhibitor of HSF1, we found that KRIBB11 induced Mcl-1 degradation in an HSF1-independent manner...
August 29, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28845295/apoptotic-resistance-of-human-skin-mast-cells-is-mediated-by-mcl-1
#15
Tarek Hazzan, Jürgen Eberle, Margitta Worm, Magda Babina
Mast cells (MCs) are major effector cells of allergic reactions and contribute to multiple other pathophysiological processes. MCs are long-lived in the tissue microenvironment, in which they matured, but it remains ill-defined how longevity is established by the natural habitat, as research on human MCs chiefly employs cells generated and expanded in culture. In this study, we report that naturally differentiated skin MCs exhibit substantial resilience to cell death with considerable portions surviving up to 3 days in the complete absence of growth factors (GF)...
2017: Cell Death Discovery
https://www.readbyqxmd.com/read/28843487/stat3-mediates-nilotinib-response-in-kit-altered-melanoma-a-phase-ii-multicenter-trial-of-the-french-skin-cancer-network
#16
Julie Delyon, Sylvie Chevret, Thomas Jouary, Sophie Dalac, Stephane Dalle, Bernard Guillot, Jean-Philippe Arnault, Marie-Françoise Avril, Christophe Bedane, Guido Bens, Anne Pham-Ledard, Sandrine Mansard, Florent Grange, Laurent Machet, Nicolas Meyer, Delphine Legoupil, Philippe Saiag, Zakia Idir, Victor Renault, Jean-François Deleuze, Elif Hindie, Maxime Battistella, Nicolas Dumaz, Samia Mourah, Celeste Lebbe
Mutated oncogenic KIT is a therapeutic target in melanoma. We conducted a multicenter phase II trial on the KIT inhibitor nilotinib in patients with unresectable melanomas harboring KIT alteration. The primary endpoint was the response rate (complete response (CR) or partial response (PR) following RECIST criteria) at 6 months. Pharmacodynamic studies using KIT sequencing, qPCR array and immunostaining of downstream KIT effectors were performed during treatment. Twenty-five patients were included and received 400 mg oral nilotinib twice daily...
August 23, 2017: Journal of Investigative Dermatology
https://www.readbyqxmd.com/read/28838991/syk-inhibition-thwarts-the-baff-b-cell-receptor-crosstalk-and-thereby-antagonizes-mcl-1-in-chronic-lymphocytic-leukemia
#17
Cody Paiva, Taylor A Rowland, Bhargava Sreekantham, Claire Godbersen, Scott R Best, Prabhjot Kaur, Marc M Loriaux, Stephen E F Spurgeon, Olga V Danilova, Alexey V Danilov
Although small molecule inhibitors of B-cell receptor-associated kinases revolutionized therapy in chronic lymphocytic leukemia, they provide for incomplete responses. Pro-survival signaling emanating from the microenvironment may foster therapeutic resistance of the malignant B-cells resident in the protective lymphoid niches. BAFF is critical in survival of both healthy and neoplastic B-cells. However, the pro-survival pathways triggered by BAFF have not been fully characterized. Here we show that BAFF elicited resistance to spontaneous and drug-induced apoptosis in stromal co-cultures, induced activation of both canonical and non-canonical NFκB signaling pathways and triggered B-cell receptor signaling in chronic lymphocytic leukemia cells, independent of IGHV mutational status...
August 24, 2017: Haematologica
https://www.readbyqxmd.com/read/28838268/rational-combination-strategies-to-enhance-venetoclax-activity-and-overcome-resistance-in-hematologic-malignancies
#18
Steven Grant
Venetoclax (ABT-199) is a Bcl-2-specific BH3-mimetic that has shown significant promise in certain subtypes of CLL as well as in several other hematologic malignancies. As in the case of essentially all targeted agents, intrinsic or acquired resistance to this agent generally occurs, prompting the search for new strategies capable of circumventing this problem. A logical approach to this challenge involves rational combination strategies designed to disable preexisting or induced compensatory survival pathways...
August 24, 2017: Leukemia & Lymphoma
https://www.readbyqxmd.com/read/28837922/development-of-glut4-selective-antagonists-for-multiple-myeloma-therapy
#19
Changyong Wei, Richa Bajpai, Horrick Sharma, Monique Heitmeier, Atul D Jain, Shannon M Matulis, Ajay K Nooka, Rama K Mishra, Paul W Hruz, Gary E Schiltz, Mala Shanmugam
Cancer cells consume more glucose to fuel metabolic programs fundamental to sustaining their survival, growth and proliferation. Among the fourteen SLC2A family members, GLUTs 1 and 4 are high-affinity glucose transporters. GLUT4 (SLC2A4) is highly expressed in muscle and adipose tissue. Basally retained within the cell, GLUT4 traffics to the plasma membrane (PM) in response to insulin and exercise-stimulation. The plasma cell malignancy multiple myeloma (MM) exhibits increased constitutive expression of GLUT4 on the PM, co-opting use of GLUT4 for survival and proliferation...
October 20, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28835385/targeting-phosphatidylinositol-3-kinase-signaling-pathway-for-therapeutic-enhancement-of-vascular-targeted-photodynamic-therapy
#20
Daniel Kraus, Pratheeba Palasuberniam, Bin Chen
Vascular-targeted photodynamic therapy (PDT) selectively disrupts vascular function by inducing oxidative damages to the vasculature, particularly endothelial cells. Although effective tumor eradication and excellent safety profile are well demonstrated in both preclinical and clinical studies, incomplete vascular shutdown and angiogenesis are known to cause tumor recurrence after vascular-targeted PDT. We have explored therapeutic enhancement of vascular-targeted PDT with phosphatidylinositol 3-kinase (PI3K) signaling pathway inhibitors because the activation of PI3K pathway was involved in promoting endothelial cell survival and proliferation after PDT...
August 23, 2017: Molecular Cancer Therapeutics
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