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https://www.readbyqxmd.com/read/28221770/the-triple-salt-sr14-ta4n13-tan4-o-a-nitridotantalate-oxide-with-19-fold-rock-salt-superstructure
#1
Matthias Wörsching, Martin Daiger, Constantin Hoch
A new structure motif in nitridometalate chemistry is the tetracatena-nitridotantalate anion [Ta4N13](19-). It occurs in the crystal structure of the triple salt Sr14[Ta4N13][TaN4]O (monoclinic, space group P21/c with a = 15.062(2) Å, b = 7.2484(6) Å, c = 24.266(3) Å, and β = 97.280(10)(o)) together with ortho-tantalate and isolated oxide anions. Synthesis followed a new approach with employment of Sr surplus and reductive conditions aimed at the preparation of subvalent compounds. The new structure type was established on the basis of single-crystal X-ray diffraction data and also Rietveld refinement...
February 21, 2017: Inorganic Chemistry
https://www.readbyqxmd.com/read/28219046/synthesis-and-biological-evaluation-of-novel-pyrazolic-chalcone-derivatives-as-novel-hepatocellular-carcinoma-therapeutics
#2
Mohammed M A Hawash, Deniz Cansen Kahraman, Fikriye Eren, Rengul Cetin Atalay, Sultan Nacak Baytas
Despite having the second highest mortality associated with cancer, currently Sorafenib is the only FDA-approved chemotherapeutic agent available for liver cancer patients which can only improve survival for few months. In this study, various pyrazolic chalcone analogous compounds were synthesized and evaluated as potential chemotherapeutic agents for the treatment of hepatocellular carcinoma (HCC). Modifying the central pyrazole ring at the C(3)-position with different heteroaryl rings and substituting the C(4)-position of pyrazole with differently substituted chalcone moiety produced fouthy two variant compounds...
February 10, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28219005/a-rhodium-iii-based-inhibitor-of-lysine-specific-histone-demethylase-1-as-an-epigenetic-modulator-in-prostate-cancer-cells
#3
Chao Yang, Wanhe Wang, Jiaxin Liang, Guodong Li, Kasipandi Vellaisamy, Chun-Yuen Wong, Dik-Lung Ma, Chung-Hang Leung
We report herein a novel rhodium(III) complex 1 as a new LSD1 targeting agent and epigenetic modulator. Complex 1 disrupted the interaction of LSD1-H3K4me2 in human prostate carcinoma cells, and enhanced the amplification of p21, FOXA2 and BMP2 gene promoters. Complex 1 was selective for LSD1 over other histone demethylases, such as KDM2b, KDM7 and MAO activities, and also showed anti-proliferative activity towards human cancer cells. To date, complex 1 is the first metal-based inhibitor of LSD1 activity.
February 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28218424/p16-ink4a-enhances-the-transcriptional-and-the-apoptotic-functions-of-p53-through-dna-dependent-interaction
#4
Huda H Al-Khalaf, Shreeram C Nallar, Dhananjaya V Kalvakolanu, Abdelilah Aboussekhra
p16(INK4A) and p53 are two important tumor suppressor proteins that play essential roles during cell proliferation and aging through regulating the expression of several genes. Here, we report that p16(INK4A) and p53 co-regulate a plethora of transcripts. Furthermore, both proteins colocalize in the nucleus of human primary skin fibroblasts and breast luminal cells, and form a heteromer whose level increases in response to genotoxic stress as well as aging of human fibroblasts and various mouse organs. CDK4 is also present in this heteromeric complex, which is formed only in the presence of DNA both in vitro using pure recombinant proteins and in vivo...
February 20, 2017: Molecular Carcinogenesis
https://www.readbyqxmd.com/read/28217805/-induction-of-robust-senescence-associated-secretory-phenotype-in-mouse-nih-3t3-cells-by-mitomycin-c
#5
Wei-Xing Huang, Xiao-Xuan Guo, Zhong-Zhi Peng, Chun-Liang Weng, Chun-Yan Huang, Ben-Yan Shi, Jie Yang, Xiao-Xin Liao, Xiao-Yi Li, Hui-Ling Zheng, Xin-Guang Liu, Xue-Rong Sun
Senescence-associated secretory phenotype (SASP) is often a concomitant result of cell senescence, embodied by the enhanced function of secretion. The SASP factors secreted by senescent cells include cytokines, proteases and chemokines, etc, which can exert great influence on local as well as systemic environment and participate in the process of cell senescence, immunoregulation, angiogenesis, cell proliferation and tumor invasion, etc. Relative to the abundance of SASP models in human cells, the in vitro SASP model derived from mouse cells is scarce at present...
February 25, 2017: Sheng Li Xue Bao: [Acta Physiologica Sinica]
https://www.readbyqxmd.com/read/28217363/crystal-structures-of-n-2-n-3-n-5-n-6-tetra-kis-pyridin-2-ylmeth-yl-pyrazine-2-3-5-6-tetra-carboxamide-and-n-2-n-3-n-5-n-6-tetra-kis-pyridin-4-ylmeth-yl-pyrazine-2-3-5-6-tetra-carboxamide
#6
Dilovan S Cati, Helen Stoeckli-Evans
The title compounds, C32H28N10O4· unknown solvent, (I), and C32H28N10O4, (II), are pyrazine-2,3,5,6-tetra-carboxamide derivatives. In (I), the substituents are (pyridin-2-ylmeth-yl)carboxamide, while in (II), the substituents are (pyridin-4-ylmeth-yl)carboxamide. Both compounds crystallize in the monoclinic space group P21/n, with Z' = 1 for (I), and Z' = 0.5 for (II). The whole mol-ecule of (II) is generated by inversion symmetry, the pyrazine ring being situated about a center of inversion. In (I), the four pyridine rings are inclined to the pyrazine ring by 83...
February 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28217338/5-amino-1-2-3-o-iso-propyl-idene-d-ribit-yl-1h-imidazole-4-carboxamide-a-crystal-structure-with-z-4
#7
Vincenzo Piccialli, Nicola Borbone, Giorgia Oliviero, Gennaro Piccialli, Stefano D'Errico, Roberto Centore
The title compound, C12H20N4O5, crystallizes in the monoclinic space group P21, with four crystallographically independent mol-ecules in the asymmetric unit. The four mol-ecules have a very similar conformation that is basically determined by the formation of two intra-molecular hydrogen bonds between the amino NH2 donors and the carbonyl and ring O-atom acceptors, forming, respectively, R(6) and R(7) ring motifs.. In the crystal, inter-molecular hydrogen bonding leads to the formation of R2(2)(10) ring patterns, involving one amide CONH2 donor and an imidazole N-atom acceptor...
February 1, 2017: Acta Crystallographica. Section E, Crystallographic Communications
https://www.readbyqxmd.com/read/28216618/1-2-5-6-dianhydrogalactitol-inhibits-human-glioma-cell-growth-in-vivo-and-in-vitro-by-arresting-the-cell-cycle-at-g2-m-phase
#8
Chun Peng, Xin-Ming Qi, Ling-Ling Miao, Jin Ren
1,2:5,6-dianhydrogalactitol (DAG) is a hexitol epoxide with marked antitumor activity against multiple types of cancer cells, but the molecular mechanisms by which DAG functions as an antitumor agent is largely unknown. In this study, we investigated the inhibitory effects of DAG on human glioma cell growth in vitro and in vivo and uncovered the underlying molecular mechanisms. Treatment with DAG (120 μmol/L) dose-dependently inhibited the proliferation and colony formation in human glioma cell lines LN229, U251, and U87MG in vitro...
February 20, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28216611/long-non-coding-rna-reprogramming-ror-promotes-cell-proliferation-in-colorectal-cancer-via-affecting-p53
#9
Hong Li, Xiumei Jiang, Xuemei Niu
BACKGROUND Colorectal cancer (CRC) remains one of the most common lethal malignant tumors worldwide. The correlation between lncRNAs expression and CRC development has not been well identified in the recent literature. This study focused on the role of lncRNA-ROR on CRC progression and development. MATERIAL AND METHODS Quantitative real-time PCR (qRT-PCR) assay was conducted to identify the expression level of lncRNA-ROR. Cell proliferation and viability were examined by MTT assay and colony formation assay...
February 20, 2017: Medical Science Monitor: International Medical Journal of Experimental and Clinical Research
https://www.readbyqxmd.com/read/28216291/ovarian-tumor-domain-containing-protein-1-deubiquitinates-and-stabilizes-p53
#10
Shudong Piao, Han Zhong Pei, Bin Huang, Suk-Hwan Baek
Ubiquitination and deubiquitination pathways play important roles in the regulation of p53 stability and activity. p53 is ubiquitinated and destabilized by E3 ubiquitin ligases and is deubiquitinated and stabilized by deubiquitinases (DUBs). We screened ovarian tumor (OTU) subfamily proteins to identify novel DUBs that stabilized p53. OTU domain-containing protein 1 (OTUD1) is a DUB belonging to the OTU family; however, its substrates and its role in cells are unknown. Here, we used an overexpression and knockdown system to show that OTUD1 is a novel regulator of p53 stability...
February 13, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28216158/resveratrol-regulates-neuronal-glucose-uptake-and-insulin-sensitivity-via-p21-activated-kinase-2-pak2
#11
Pallavi Varshney, Chinmoy Sankar Dey
We have recently reported P21-activated kinase 2 (PAK2), a serine/threonine kinase as a negative regulator of neuronal glucose uptake and insulin sensitivity. Resveratrol (RSV), a natural polyphenol with anti-oxidative, anti-inflammatory and anti-diabetic properties, regulates PAK2 activity in HepG2 and ESC-B5 cell apoptosis. However, regulation of PAK2 by RSV in neuronal insulin signaling pathway, if any, is still unknown. In the present study, RSV treatment significantly increased PAK2 activity under insulin-sensitive and insulin-resistant condition, along with a marked decrease in glucose uptake in differentiated N2A cells...
February 16, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28214890/a-new-perspective-for-osteosarcoma-therapy-proteasome-inhibition-by-mln9708-2238-successfully-induces-apoptosis-and-cell-cycle-arrest-and-attenuates-the-invasion-ability-of-osteosarcoma-cells-in-vitro
#12
Renhao Liu, Chunjiang Fu, Jiabing Sun, Xvming Wang, Shuo Geng, Xiaoyu Wang, Jilong Zou, Zhenggang Bi, Chenglin Yang
BACKGROUND: The proteasome exists in all eukaryotic cells and provides the main route of intracellular proteins degradation involved in cell growth and apoptosis. Proteasome inhibition could block protein degradation pathways and disturb regulatory networks, possibly leading to profound effects on cell growth, particularly in cancer cells. A proteasome inhibitor with an appropriate toxicity index for malignant cells rather than normal cells would be an attractive anticancer therapy. METHODS: The human osteosarcoma (OS) cell lines MG-63 and Saos-2 and normal osteoblast cells were used to study the antitumour activity of the proteasome inhibitor MLN9708/2238...
January 27, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28214592/role-of-a-p53-polymorphism-in-the-development-of-nonfunctional-pituitary-adenomas
#13
Garima Yagnik, Arman Jahangiri, Rebecca Chen, Jeffrey R Wagner, Manish K Aghi
Non-functional pituitary adenomas (NFPAs) are among the commonest intracranial neoplasms. While histologically benign, NFPAs sometimes become large enough to limit therapeutic options and reduce quality of life. Investigations of the molecular etiology of NFPAs have failed to identify prevalent genetic changes and, while a role for p53 has been suggested, TP53 gene alterations have yet to be described in NFPAs. We found that the polymorphism rs1042522:C > G in codon 72 of exon 4 of the TP53 gene, whose C variant produces a proline and is more common in most ethnicities, has a G variant producing an arginine in 79...
February 15, 2017: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/28214231/mechanisms-of-action-and-structure-activity-relationships-of-cytotoxic-flavokawain-derivatives
#14
Charlotte Thieury, Nicolas Lebouvier, Rémy Le Guével, Yann Barguil, Gaëtan Herbette, Cyril Antheaume, Edouard Hnawia, Yoshinori Asakawa, Mohammed Nour, Thierry Guillaudeux
22 Flavokawain derivatives (FKd) were obtained by one step syntheses in order to conduct a SAR study to understand the structural requirements for optimum and selective cytotoxicity. FKd and natural flavokawains A and B found into kava, a South Pacific traditional beverage, were evaluated against nine cancer and one healthy cell lines. The targeted cell cycle phases as well as the effects on the induction of apoptosis and cell cycle protein levels were investigated. Therapeutic improvements (more activity and selectivity) were achieved with FKd compared to natural flavokawains and notably with the 2',3,4',6'-tetramethoxychalcone (FKd 19)...
February 6, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28213701/ursolic-acid-mediated-changes-in-glycolytic-pathway-promote-cytotoxic-autophagy-and-apoptosis-in-phenotypically-different-breast-cancer-cells
#15
Anna Lewinska, Jagoda Adamczyk-Grochala, Ewa Kwasniewicz, Anna Deregowska, Maciej Wnuk
Plant-derived pentacyclic triterpenotids with multiple biological activities are considered as promising candidates for cancer therapy and prevention. However, their mechanisms of action are not fully understood. In the present study, we have analyzed the effects of low dose treatment (5-20 µM) of ursolic acid (UA) and betulinic acid (BA) on breast cancer cells of different receptor status, namely MCF-7 (ER(+), PR(+/-), HER2(-)), MDA-MB-231 (ER(-), PR(-), HER2(-)) and SK-BR-3 (ER(-), PR(-), HER2(+)). UA-mediated response was more potent than BA-mediated response...
February 17, 2017: Apoptosis: An International Journal on Programmed Cell Death
https://www.readbyqxmd.com/read/28213471/attenuation-of-endoplasmic-reticulum-stress-by-caffeine-ameliorates-hyperoxia-induced-lung-injury
#16
Ru-Jeng Teng, Xigang Jing, Teresa Michalkiewicz, Adeleye J Afolayan, Tzong-Jin Wu, Girija G Konduri
Rodent pups exposed to hyperoxia develop lung changes similar to bronchopulmonary dysplasia (BPD) in extremely premature infants. Oxidative stress from hyperoxia can injure developing lungs through endoplasmic reticulum (ER) stress. Early caffeine treatment decreases the rate of BPD, but the mechanisms remain unclear. We hypothesized that caffeine attenuates hyperoxia-induced lung injury through its chemical chaperone property. Sprague-Dawley rat pups were raised either in 90% (hyperoxia) or 21% (normoxia) oxygen from postnatal day 1 (P1) to postnatal day 10 (P10) and then recovered in 21% oxygen until P21...
February 17, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28212889/inhibition-of-proliferation-and-invasion-in-2d-and-3d-models-by-2-methoxyestradiol-in-human-melanoma-cells
#17
R R Massaro, F Faião-Flores, V W Rebecca, S Sandri, D K Alves-Fernandes, P C Pennacchi, K S M Smalley, S S Maria-Engler
Despite the recent advances in the clinical management of melanoma, there remains a need for new pharmacological approaches to treat this cancer. 2-methoxyestradiol (2ME) is a metabolite of estrogen that has shown anti-tumor effects in many cancer types. In this study we show that 2ME treatment leads to growth inhibition in melanoma cells, an effect associated with entry into senescence, decreased pRb and CyclinB1 expression, increased p21/Cip1 expression and G2/M cell cycle arrest. 2ME treatment also inhibits melanoma cell growth in colony formation assays, including cell lines with acquired resistance to BRAF and BRAF+MEK inhibitors...
February 14, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28212270/antitumor-effects-of-laminaria-extract-fucoxanthin-on-lung-cancer
#18
ChengHan Mei, ShunChang Zhou, Lin Zhu, JiaXiong Ming, FanDian Zeng, Rong Xu
Lung cancer is the leading cause of cancer mortality worldwide and non-small-cell lung cancer (NSCLC) is the most common type. Marine plants provide rich resources for anticancer drug discovery. Fucoxanthin (FX), a Laminaria japonica extract, has attracted great research interest for its antitumor activities. Accumulating evidence suggests anti-proliferative effects of FX on many cancer cell lines including NSCLCs, but the detailed mechanisms remain unclear. In the present investigation, we confirmed molecular mechanisms and in vivo anti-lung cancer effect of FX at the first time...
February 15, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28211114/magnesium-lithospermate-b-from-salvia-miltiorrhiza-bunge-ameliorates-aging-induced-renal-inflammation-and-senescence-via-nadph-oxidase-mediated-reactive-oxygen-generation
#19
Chan Hum Park, Sung Ho Shin, Eun Kyeong Lee, Dae Hyun Kim, Min-Jo Kim, Seong-Soo Roh, Takako Yokozawa, Hae Young Chung
The present study was conducted to examine whether magnesium lithospermate B (MLB) extracted from Salviae miltiorrhizae radix was renoprotective in pathways related to age-related oxidative stress in aged rats. Magnesium lithospermate B was orally administered at a dose of 2- or 8-mg/kg body weight for 16 consecutive days, and the effects were compared with those of vehicle in old and young rats. Magnesium lithospermate B administration to old rats ameliorated renal oxidative stress through reduction of reactive oxygen species...
February 16, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28209205/long-noncoding-agap2-as1-is-activated-by-sp1-and-promotes-cell-proliferation-and-invasion-in-gastric-cancer
#20
Fuzhen Qi, Xianghua Liu, Hao Wu, Xiang Yu, Chenchen Wei, Xiaodan Huang, Guozhong Ji, Fengqi Nie, Keming Wang
BACKGROUND: Long noncoding RNAs (lncRNAs) have emerged as important regulators of tumorigenesis and cancer progression. Recently, the lncRNA AGAP2-AS1 was identified as an oncogenic lncRNA in human non-small cell lung cancer (NSCLC) and its elevated expression was linked to NSCLC development and progression. However, the expression pattern and molecular mechanism of AGAP2-AS1 in gastric cancer (GC) have not been characterized. METHODS: Bioinformatic analysis was performed to determine AGAP2-AS1 expression levels in the GC and normal tissues using gene profiling data from the Gene Expression Omnibus...
February 16, 2017: Journal of Hematology & Oncology
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