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https://www.readbyqxmd.com/read/29039762/marine-derived-2-aminoimidazolone-alkaloids-leucettamine-b-related-polyandrocarpamines-inhibit-mammalian-and-protozoan-dyrk-clk-kinases
#1
Nadège Loaëc, Eletta Attanasio, Benoît Villiers, Emilie Durieu, Tania Tahtouh, Morgane Cam, Rohan A Davis, Aline Alencar, Mélanie Roué, Marie-Lise Bourguet-Kondracki, Peter Proksch, Emmanuelle Limanton, Solène Guiheneuf, François Carreaux, Jean-Pierre Bazureau, Michelle Klautau, Laurent Meijer
A large diversity of 2-aminoimidazolone alkaloids is produced by various marine invertebrates, especially by the marine Calcareous sponges Leucetta and Clathrina. The phylogeny of these sponges and the wide scope of 2-aminoimidazolone alkaloids they produce are reviewed in this article. The origin (invertebrate cells, associated microorganisms, or filtered plankton), physiological functions, and natural molecular targets of these alkaloids are largely unknown. Following the identification of leucettamine B as an inhibitor of selected protein kinases, we synthesized a family of analogues, collectively named leucettines, as potent inhibitors of DYRKs (dual-specificity, tyrosine phosphorylation regulated kinases) and CLKs (cdc2-like kinases) and potential pharmacological leads for the treatment of several diseases, including Alzheimer's disease and Down syndrome...
October 17, 2017: Marine Drugs
https://www.readbyqxmd.com/read/29039458/dna-polymerase-5-acetylation-by-eso1-is-essential-for-schizosaccharomyces-pombe-viability
#2
Zhiming Chen, Hongshi Cao, Yingqiang Lu, Qiang Ren, Liankun Sun
Eco1/Eso1 protein plays an important role in chromosome segregation, DNA repair and gene regulation. Eco1 mutation induces Roberts syndrome clinically and rDNA transcription disorders in vivo. In this study, we examined the role of Eso1 protein binding to polymerase 5 (Pol5) and the acetylation of Pol5 protein in the regulation of Schizosaccharomyces pombe (S. pombe) viability. Immunoprecipitation and mass spectrometry assays identified Eso1 protein binding to Cdc2, Pol5 and Cdc21, as well as other proteins...
October 16, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29029413/targeting-shp-1-stat3-signaling-a-promising-therapeutic-approach-for-the-treatment-of-cholangiocarcinoma
#3
Ming-Hung Hu, Li-Ju Chen, Yen-Lin Chen, Ming-Shen Tsai, Chung-Wai Shiau, Tzu-I Chao, Chun-Yu Liu, Jia-Horng Kao, Kuen-Feng Chen
Sorafenib is a multiple kinase inhibitor which targets Raf kinases, VEGFR, and PDGFR and is approved for the treatment of hepatocellular carcinoma (HCC). Previously, we found that p-STAT3 is a major target of SC-43, a sorafenib derivative. In this study, we report that SC-43-induced apoptosis in cholangiocarcinoma (CCA) via a novel mechanism. Three CCA cell lines (HuCCT-1, KKU-100 and CGCCA) were treated with SC-43 to determine their sensitivity to SC-43-induced cell death and apoptosis. We found that SC-43 activated SH2 domain-containing phosphatase 1 (SHP-1) activity, leading to p-STAT3 and downstream cyclin B1 and Cdc2 downregulation, which induced G2-M arrest and apoptotic cell death...
September 12, 2017: Oncotarget
https://www.readbyqxmd.com/read/29016926/activation-of-wee1-confers-resistance-to-pi3k-inhibition-in-glioblastoma
#4
Shaofang Wu, Shuzhen Wang, Feng Gao, Luyuan Li, Siyuan Zheng, W K Alfred Yung, Dimpy Koul
Background: Oncogenic activation of phosphatidylinositol-3 kinase (PI3K) signaling plays a pivotal role in the development of glioblastoma (GBM). However, pharmacological inhibition of PI3K has so far not been therapeutically successful due to adaptive resistance through a rapid rewiring of cancer cell signaling. Here we identified that WEE1 is activated after transient exposure to PI3K inhibition and confers resistance to PI3K inhibition in GBM. Methods: Patient-derived glioma-initiating cells and established GBM cells were treated with PI3K inhibitor or WEE1 inhibitor alone or in combination, and cell proliferation was evaluated by CellTiter-Blue assay...
July 7, 2017: Neuro-oncology
https://www.readbyqxmd.com/read/28991472/the-discovery-of-a-dual-ttk-protein-kinase-cdc2-like-kinase-clk2-inhibitor-for-the-treatment-of-triple-negative-breast-cancer-initiated-from-a-phenotypic-screen
#5
Jennifer R Riggs, Mark Nagy, Jan Elsner, Paul Erdman, Dan Cashion, Dale Robinson, Roy Harris, Dehua Huang, Lida Tehrani, Gordafaried Deyanat-Yazdi, Rama Krishna Narla, Xiaohui Peng, Tam Tran, Leo Barnes, Terra Miller, Jason Katz, Yang Tang, Ming Chen, Mehran F Moghaddam, Sogole Bahmanyar, Barbra Pagarigan, Silvia L Delker, Laurie LeBrun, Philip Paul Chamberlain, Andrew Calabrese, Stacie S Canan, Katerina Leftheris, Dan Zhu, John F Boylan
Triple negative breast cancer (TNBC) remains a serious unmet medical need with discouragingly high relapse rates. We report here the synthesis and structure-activity relationship (SAR) of a novel series of 2,4,5-trisubstituted-7H-pyrrolo[2,3-d]pyrimidines with potent activity against TNBC tumor cell lines. These compounds were discovered from a TNBC phenotypic screen and possess a unique dual inhibition profile targeting TTK (mitotic exit) and CLK2 (mRNA splicing). Design and optimization, driven with a TNBC tumor cell assay, identified potent and selective compounds with favorable in vitro and in vivo activity profiles and good iv PK properties...
October 9, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28988508/immunological-effects-of-everolimus-in-patients-with-metastatic-renal-cell-cancer
#6
Charlotte M Huijts, Saskia J Santegoets, Tamarah D de Jong, Henk M Verheul, Tanja D de Gruijl, Hans J van der Vliet
The mammalian target of rapamycin (mTOR) is a crucial kinase present in all cells. Besides its role in the regulation of cell-growth, proliferation, angiogenesis, and survival of malignant tumors, mTOR additionally plays an important role in immune regulation by controlling the balance between effector T cells and regulatory T cells (Tregs). This critically affects the suppressive state of the immune system. Here, the systemic immunological effects of everolimus treatment were comprehensively investigated in five patients with metastatic renal cell cancer...
October 1, 2017: International Journal of Immunopathology and Pharmacology
https://www.readbyqxmd.com/read/28983768/low-dose-combined-exposure-of-nanoparticles-and-heavy-metal-compared-with-pm2-5-in-human-myocardial-ac16-cells
#7
Lin Feng, Xiaozhe Yang, Collins Otieno Asweto, Jing Wu, Yannan Zhang, Hejing Hu, Yanfeng Shi, Junchao Duan, Zhiwei Sun
The co-exposure toxicity mechanism of ultrafine particles and pollutants on human cardiovascular system are still unclear. In this study, the combined effects of silica nanoparticles (SiNPs) and/or carbon black nanoparticles (CBNPs) with Pb(AC)2 compared with particulate matter (PM)2.5 were investigated in human myocardial cells (AC16). Our study detected three different combinations of SiNPs and Pb(AC)2, CBNPs and Pb(AC)2, and SiNPs and CBNPs compared with PM2.5 at low-dose exposure. Using PM2.5 as positive control, our results suggested that the combination of SiNPs and Pb(AC)2/CBNPs could increase the production of reactive oxygen species (ROS), lactate dehydrogenase leakage (LDH), and malondialdehyde (MDA) and decrease the activities of superoxide dismutase (SOD) and glutathione (GSH); induce inflammation by the upregulation of protein CRP and TNF-α, and apoptosis by the upregulation of protein caspase-3, caspase-9, and Bax while the downregulation of protein Bcl-2; and trigger G2/M phase arrest by the upregulation of protein Chk2 and downregulation of protein Cdc2 and cyclin B1...
October 5, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28963110/development-diversity-and-function-of-dendritic-cells-in-mouse-and-human
#8
David A Anderson, Kenneth M Murphy, Carlos G Briseño
The study of murine dendritic cell (DC) development has been integral to the identification of specialized DC subsets that have unique requirements for their form and function. Advances in the field have also provided a framework for the identification of human DC counterparts, which appear to have conserved mechanisms of development and function. Multiple transcription factors are expressed in unique combinations that direct the development of classical DCs (cDCs), which include two major subsets known as cDC1s and cDC2s, and plasmacytoid DCs (pDCs)...
September 29, 2017: Cold Spring Harbor Perspectives in Biology
https://www.readbyqxmd.com/read/28935563/oridonin-induces-g2-m-cell-cycle-arrest-and-apoptosis-in-human-oral-squamous-cell-carcinoma
#9
Han Wang, Liping Zhu, Xiaodong Feng, Han Zhang, Qingqiong Luo, Fuxiang Chen
Oridonin, an active diterpeniod isolated from Rabdosia rubescens, has been reported for its anti-tumor activity on several cancers, however, its effect on oral squamous cell carcinoma (OSCC) remains unclear. In this study, we demonstrated for the first time that oridonin inhibited the growth of OSCC cells both in vitro and in vivo. Oridonin decreased the proliferation and clonal formation of cultured OSCC cells in a dose-dependent manner. Further study indicated that oridonin induced G2/M phase arrest in OSCC cells, which was associated with the downregulation of proteins related to G2/M transition including cdc25C, cdc2 and cyclin B1, as well as the upregulation of p53 and phosphorylated-cdc2...
September 19, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28915612/the-roles-of-ing5-in-gliomas-a-good-marker-for-tumorigenesis-and-a-potential-target-for-gene-therapy
#10
Shuang Zhao, Zhi-Juan Zhao, Hao-Yu He, Ji-Cheng Wu, Xiao-Qing Ding, Lei Yang, Ning Jia, Zhi-Jie Li, Hua-Chuan Zheng
To elucidate the anti-tumor effects and molecular mechanisms of ING5 on glioma cells, we overexpressed it in U87 cells, and examined the phenotypes and their relevant molecules. It was found that ING5 overexpression suppressed proliferation, energy metabolism, migration, invasion, and induced G2/M arrest, apoptosis, dedifferentiation, senescence, mesenchymal- epithelial transition and chemoresistance to cisplatin, MG132, paclitaxel and SAHA in U87 cells. There appeared a lower expression of N-cadherin, Twist, Slug, Zeb1, Zeb2, Snail, Ac-H3, Ac-H4, Cdc2, Cdk4 and XIAP, but a higher expression of Claudin 1, Histones 3 and 4, p21, p53, Bax, β-catenin, PI3K, Akt, and p-Akt in ING5 transfectants...
August 22, 2017: Oncotarget
https://www.readbyqxmd.com/read/28902363/ginkgetin-induces-g2-phase-arrest-in-hct116-colon-cancer-cells-through-the-modulation-of-b%C3%A2-myb-and-mirna34a-expression
#11
Yu-Jin Lee, Yeong-Rim Kang, So Young Lee, Yena Jin, Dong Cho Han, Byoung-Mog Kwon
Ginkgetin has been reported to display antitumor activity. However, the relevant pathway integrating cell cycle regulation and signaling pathways involved in growth inhibition in CRC cells remains to be identified. In this study, ginkgetin-treated HCT116 CRC cells exhibited significant dose-dependent growth inhibition with a GI50 value of 4.0 µM for 48-h treatment, together with apoptosis, via G2-phase cell cycle arrest. When HCT116 cells were treated with 10 µM ginkgetin for 48 h, the percentage of cells in G2/M phase increased by 2...
September 5, 2017: International Journal of Oncology
https://www.readbyqxmd.com/read/28895052/the-effects-of-periostin-in-a-rat-model-of-isoproterenol-mediated-cardiotoxicity
#12
Mahmut Sözmen, Alparslan K Devrim, Yonca B Kabak, Tuba Devrim, Mert Sudagidan
Periostin is an extracellular matrix protein from fasciclin family, and it plays an important role in the cell adhesion, migration, and growth of the organism. Periostin prevents apoptosis while stimulating cardiomyocytes. The present study was designed to investigate cardioprotective effects of the recombinant murine periostin peptide administration in a rat model of isoproterenol (ISO)-induced myocardial injury. The experiment was performed on 84 adult male Sprague Dawley rats in 4 groups (n = 21): control group (1), periostin-treated group (2), ISO-treated group (3), and ISO + periostin-treated group (4)...
September 11, 2017: Cardiovascular Toxicology
https://www.readbyqxmd.com/read/28878767/human-blood-cd1c-dendritic-cells-promote-th1-and-th17-effector-function-in-memory-cd4-t-cells
#13
Ingrid M Leal Rojas, Wai-Hong Mok, Frances E Pearson, Yoshihito Minoda, Tony J Kenna, Ross T Barnard, Kristen J Radford
Dendritic cells (DC) initiate the differentiation of CD4(+) helper T cells into effector cells including Th1 and Th17 responses that play an important role in inflammation and autoimmune disease pathogenesis. In mice, Th1 and Th17 responses are regulated by different conventional (c) DC subsets, with cDC1 being the main producers of IL-12p70 and inducers of Th1 responses, while cDC2 produce IL-23 to promote Th17 responses. The role that human DC subsets play in memory CD4(+) T cell activation is not known. This study investigated production of Th1 promoting cytokine IL-12p70, and Th17 promoting cytokines, IL-1β, IL-6, and IL-23, by human blood monocytes, CD1c(+) DC, CD141(+) DC, and plasmacytoid DC and examined their ability to induce Th1 and Th17 responses in memory CD4(+) T cells...
2017: Frontiers in Immunology
https://www.readbyqxmd.com/read/28865368/sweroside-eradicated-leukemia-cells-and-attenuated-pathogenic-processes-in-mice-by-inducing-apoptosis
#14
Xiao-Lin Han, Jing-Dong Li, Wan-Ling Wang, Cui Yang, Zhi-Ying Li
Acute myeloid leukemia (AML), characterized by extremely heterogeneous molecular and biologic abnormalities, is an aggressive hematologic malignancy, hampering the research and development of effective targeted treatment modalities. Sweroside (SWE), an iridoid glycoside, is isolated from Lonicera japonIca. It has diverse biological activities, but little is known in human leukemia. Here, our study showed the potential of sweroside as an effective agent against human leukemia using in vitro and in vivo approaches...
August 30, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28806997/stathmin-is-overexpressed-and-regulated-by-mutant-p53-in-oral-squamous-cell-carcinoma
#15
Hai-Long Ma, Shu-Fang Jin, Wu-Tong Ju, Yong Fu, Yao-Yao Tu, Li-Zhen Wang, Jiang-Li, Zhi-Yuan Zhang, Lai-Ping Zhong
BACKGROUND: The aim of this study was to investigate the oncogenic function and regulatory mechanism of stathmin in oral squamous cell carcinoma (OSCC). METHODS: Two-dimensional electrophoresis and liquid chromatography-tandem mass chromatography were applied to screen differentiated proteins during carcinogenesis in OSCC. Cell Counting Kit-8 (CCK-8) assays, colony formation, migration, flow cytometry, immunofluorescence and a xenograft model were used to detect the function of stathmin...
August 14, 2017: Journal of Experimental & Clinical Cancer Research: CR
https://www.readbyqxmd.com/read/28805696/licochalcone-a-inhibits-the-proliferation-of-human-lung-cancer-cell-lines-a549-and-h460-by-inducing-g2-m-cell-cycle-arrest-and-er-stress
#16
Chenyu Qiu, Tingting Zhang, Wenxin Zhang, Lina Zhou, Bin Yu, Wei Wang, Zhihong Yang, Zhiguo Liu, Peng Zou, Guang Liang
Licochalcone A (LicA), a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch, has wide spectrum of pharmacological activities. In this study, the anti-cancer effects and potential mechanisms of LicA in non-small cell lung cancer (NSCLC) cells were studied. LicA decreased cell viability and induced apoptosis in a dose-dependent manner in NSCLC cells. LicA inhibited lung cancer cells growth by blocking cell cycle progression at the G2/M transition and inducing apoptosis. LicA treatment decreased the expression of MDM2, Cyclin B1, Cdc2 and Cdc25C in H460 and A549 cancer cell lines...
August 12, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28797724/the-effect-of-newly-synthesized-progesterone-derivatives-on-apoptotic-and-angiogenic-pathway-in-mcf-7-breast-cancer-cells
#17
Shaymaa M M Yahya, Abdou O Abdelhamid, Mervat M Abd-Elhalim, Ghada H Elsayed, Emad F Eskander
Due to its high potency and selectivity, anticancer agents consisting of combined molecules have gained great interests. The current study introduces newly synthesized progesterone derivatives of promising anticancer effect. Moreover, the pro-apoptotic and anti-angiogenic effects of these compounds were studied extensively. Several thiazole, pyridine, pyrazole, thiazolopyridine and pyrazolopyridine progesterone derivatives were synthesized. The structure of the novel progesterone derivatives was elucidated and confirmed using the analytical and spectral data...
October 2017: Steroids
https://www.readbyqxmd.com/read/28783692/human-lymphoid-organ-dendritic-cell-identity-is-predominantly-dictated-by-ontogeny-not-tissue-microenvironment
#18
Gordon F Heidkamp, Jil Sander, Christian H K Lehmann, Lukas Heger, Nathalie Eissing, Anna Baranska, Jennifer J Lühr, Alana Hoffmann, Katharina C Reimer, Anja Lux, Stephan Söder, Arndt Hartmann, Johannes Zenk, Thomas Ulas, Naomi McGovern, Christoph Alexiou, Bernd Spriewald, Andreas Mackensen, Gerold Schuler, Burkhard Schauf, Anja Forster, Roland Repp, Peter A Fasching, Ariawan Purbojo, Robert Cesnjevar, Evelyn Ullrich, Florent Ginhoux, Andreas Schlitzer, Falk Nimmerjahn, Joachim L Schultze, Diana Dudziak
In mice, conventional and plasmacytoid dendritic cells (DCs) derive from separate hematopoietic precursors before they migrate to peripheral tissues. Moreover, two classes of conventional DCs (cDC1 and cDC2 DCs) and one class of plasmacytoid DCs (pDCs) have been shown to be transcriptionally and functionally distinct entities. In humans, these three DC subtypes can be identified using the cell surface markers CD1c (cDC2), CD141 (cDC1), and CD303 (pDCs), albeit it remains elusive whether DC functionality is mainly determined by ontogeny or the tissue microenvironment...
December 16, 2016: Science Immunology
https://www.readbyqxmd.com/read/28737827/cytotoxic-and-chemosensitization-effects-of-scutellarin-from-traditional-chinese-herb-scutellaria%C3%A2-altissima%C3%A2-l-in-human-prostate-cancer-cells
#19
Chen Gao, Yinglu Zhou, Zhongling Jiang, Yuan Zhao, Dongjun Zhang, Xia Cong, Rongfeng Cao, Huatao Li, Wenru Tian
Scutellaria altissima L. is a common traditional Chinese medicine used to treat inflammation in some countries. Scutellarin, an active major flavone glycoside isolated from the traditional Chinese medicine Scutellaria altissima L., has been shown to offer various beneficial biochemical effects on cerebrovascular diseases and inflammation. However, the antiproliferative effects of Scutellarin in prostate cancer and the underlying mechanism are not fully elucidated. In the present study, we aimed to ascertain whether Scutellarin inhibits cancer cell growth and to further explore the molecular mechanism...
September 2017: Oncology Reports
https://www.readbyqxmd.com/read/28733545/a-small-molecule-inhibitor-targeting-the-aurkc-i%C3%AE%C2%BAb%C3%AE-interaction-decreases-transformed-growth-of-mda-mb-231-breast-cancer-cells
#20
Eun Hee Han, Jin-Young Min, Shin-Ae Yoo, Sung-Joon Park, Yun-Jeong Choe, Hee Sub Yun, Zee-Won Lee, Sun Woo Jin, Hyung Gyun Kim, Hye Gwang Jeong, Hyun Kyoung Kim, Nam Doo Kim, Young-Ho Chung
The Aurora kinases, Aurora A (AURKA), Aurora B (AURKB), and Aurora C (AURKC), are serine/threonine kinases required for the control of mitosis (AURKA and AURKB) or meiosis (AURKC). Several Aurora kinase inhibitors are being investigated as novel anticancer therapeutics. Recent studies demonstrated that AURKC activation contributes to breast cancer cell transformation. Therefore, AURKC is both a promising marker and therapeutic target for breast cancer; however, its signaling network has not been fully characterized...
June 29, 2017: Oncotarget
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