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https://www.readbyqxmd.com/read/28107773/safety-and-effectiveness-of-tofogliflozin-in-elderly-japanese-patients-with-type-2-diabetes-mellitus-a-post-marketing-study-j-step-el-study
#1
Kazunori Utsunomiya, Naoki Shimmoto, Masayuki Senda, Yuji Kurihara, Ryoji Gunji, Shoko Fujii, Seigo Kakiuchi, Hisataka Fujiwara, Hiroyuki Kameda, Masahiro Tamura, Kohei Kaku
AIMS/INTRODUCTION: While sodium glucose cotransporter 2 inhibitors are a promising treatment for type 2 diabetes mellitus, they are associated with concerns about specific adverse drug reactions. We conducted a 1-year post-marketing study of tofogliflozin, a novel agent in this class, in Japanese elderly patients with type 2 diabetes mellitus. MATERIALS AND METHODS: This was a prospective, observational, and multicenter post-marketing study conducted in the context of routine clinical practice...
January 20, 2017: Journal of Diabetes Investigation
https://www.readbyqxmd.com/read/28107629/discovery-of-1-2-3-triazole-derivatives-for-multimodality-pet-ct-cryoimaging-of-myelination-in-the-central-nervous-system
#2
Chunying Wu, Brendan Eck, Sheng Zhang, Junqing Zhu, Anand Dev Tiwari, Yifan Zhang, Yunjie Zhu, Jinming Zhang, Bin Wang, Xizhen Wang, Xu Wang, Jingqiang You, Jian Wang, Yihui Guan, Xingdang Liu, Xin Yu, Bruce D Trapp, Robert Miller, Jerry Silver, David Wilson, Yanming Wang
Myelin pathology is present in many neurological conditions such as multiple sclerosis (MS) and traumatic spinal cord injury (SCI). To facilitate development of novel therapies aimed at myelin repair, we set out to develop imaging agents that permit direct quantification of myelination in vivo. In this work, we designed and synthesized a series of fluorescent fluorinated myelin imaging agents that can be used for in vivo positron emission tomography (PET) imaging combined with subsequent post-mortem fluorescent cryoimaging...
January 20, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28107519/cudraflavone-c-induces-tumor-specific-apoptosis-in-colorectal-cancer-cells-through-inhibition-of-the-phosphoinositide-3-kinase-pi3k-akt-pathway
#3
Hsien-Chuen Soo, Felicia Fei-Lei Chung, Kuan-Hon Lim, Veronica Alicia Yap, Tracey D Bradshaw, Ling-Wei Hii, Si-Hoey Tan, Sze-Jia See, Yuen-Fen Tan, Chee-Onn Leong, Chun-Wai Mai
Cudraflavone C (Cud C) is a naturally-occurring flavonol with reported anti-proliferative activities. However, the mechanisms by which Cud C induced cytotoxicity have yet to be fully elucidated. Here, we investigated the effects of Cud C on cell proliferation, caspase activation andapoptosis induction in colorectal cancer cells (CRC). We show that Cud C inhibits cell proliferation in KM12, Caco-2, HT29, HCC2998, HCT116 and SW48 CRC but not in the non-transformed colorectal epithelial cells, CCD CoN 841. Cud C induces tumor-selective apoptosis via mitochondrial depolarization and activation of the intrinsic caspase pathway...
2017: PloS One
https://www.readbyqxmd.com/read/28106982/a-novel-iron-ii-preferring-dopamine-agonist-chelator-as-potential-symptomatic-and-neuroprotective-therapeutic-agent-for-parkinson-s-disease
#4
Banibrata Das, Ashoka Kandegedara, Liping Xu, Tamara Antonio, Timothy L Stemmler, Maarten E A Reith, Aloke K Dutta
Parkinson's disease (PD) is a progressive neurodegenerative disorder and development of disease-modifying treatment is still an unmet medical need. Considering the implication of free iron (II) in PD, we report here the design and characterization of a novel hybrid iron chelator, (-)-12 (D-607) as a multitarget-directed ligand against PD. Binding and functional assays at dopamine D2/D3 receptors indicate potent agonist activity of (-)-12. The molecule displayed an efficient preferential iron (II) chelation properties along with potent in vivo activity in a reserpinized PD animal model...
January 20, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28106882/combination-of-iap-antagonist-and-ifn%C3%AE-activates-novel-caspase-10-and-ripk1-dependent-cell-death-pathways
#5
Maria C Tanzer, Nufail Khan, James A Rickard, Nima Etemadi, Najoua Lalaoui, Sukhdeep Kaur Spall, Joanne M Hildebrand, David Segal, Maria Miasari, Diep Chau, WendyWei-Lynn Wong, Mark McKinlay, Srinivas K Chunduru, Christopher A Benetatos, Stephen M Condon, James E Vince, Marco J Herold, John Silke
Peptido-mimetic inhibitor of apoptosis protein (IAP) antagonists (Smac mimetics (SMs)) can kill tumour cells by depleting endogenous IAPs and thereby inducing tumour necrosis factor (TNF) production. We found that interferon-γ (IFNγ) synergises with SMs to kill cancer cells independently of TNF- and other cell death receptor signalling pathways. Surprisingly, CRISPR/Cas9 HT29 cells doubly deficient for caspase-8 and the necroptotic pathway mediators RIPK3 or MLKL were still sensitive to IFNγ/SM-induced killing...
January 20, 2017: Cell Death and Differentiation
https://www.readbyqxmd.com/read/28106842/adenoviral-vectors-armed-with-cell-fusion-inducing-proteins-as-anti-cancer-agents
#6
REVIEW
Joshua Del Papa, Robin J Parks
Cancer is a devastating disease that affects millions of patients every year, and causes an enormous economic burden on the health care system and emotional burden on affected families. The first line of defense against solid tumors is usually extraction of the tumor, when possible, by surgical methods. In cases where solid tumors can not be safely removed, chemotherapy is often the first line of treatment. As metastatic cancers often become vigorously resistant to treatments, the development of novel, more potent and selective anti-cancer strategies is of great importance...
January 19, 2017: Viruses
https://www.readbyqxmd.com/read/28106782/from-clinical-standards-to-translating-next-generation-sequencing-research-into-patient-care-improvement-for-hepatobiliary-and-pancreatic-cancers
#7
REVIEW
Ioannis D Kyrochristos, Georgios K Glantzounis, Demosthenes E Ziogas, Ioannis Gizas, Dimitrios Schizas, Efstathios G Lykoudis, Evangelos Felekouras, Anastasios Machairas, Christos Katsios, Theodoros Liakakos, William C Cho, Dimitrios H Roukos
Hepatobiliary and pancreatic (HBP) cancers are associated with high cancer-related death rates. Surgery aiming for complete tumor resection (R0) remains the cornerstone of the treatment for HBP cancers. The current progress in the adjuvant treatment is quite slow, with gemcitabine chemotherapy available only for pancreatic ductal adenocarcinoma (PDA). In the advanced and metastatic setting, only two targeted drugs have been approved by the Food & Drug Administration (FDA), which are sorafenib for hepatocellular carcinoma and erlotinib for PDA...
January 18, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28106753/naphthalimides-selectively-inhibit-the-activity-of-bacterial-replicative-dna-ligases-and-display-bactericidal-effects-against-tubercle-bacilli
#8
Malgorzata Korycka-Machala, Marcin Nowosielski, Aneta Kuron, Sebastian Rykowski, Agnieszka Olejniczak, Marcin Hoffmann, Jaroslaw Dziadek
The DNA ligases, enzymes that seal breaks in the backbones of DNA, are essential for all organisms, however bacterial ligases essential for DNA replication use β-nicotinamide adenine dinucleotide as their co-factor, whereas those that are essential in eukaryotes and viruses use adenosine-5'-triphosphate. This fact leads to the conclusion that NAD⁺-dependent DNA ligases in bacteria could be targeted by their co-factor specific inhibitors. The development of novel alternative medical strategies, including new drugs, are a top priority focus areas for tuberculosis research due to an increase in the number of multi-drug resistant as well as totally drug resistant tubercle bacilli strains...
January 17, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28106722/using-network-extracted-ontologies-to-identify-novel-genes-with-roles-in-appressorium-development-in-the-rice-blast-fungus-magnaporthe-oryzae
#9
Ryan M Ames
Magnaporthe oryzae is the causal agent of rice blast disease, the most important infection of rice worldwide. Half the world's population depends on rice for its primary caloric intake and, as such, rice blast poses a serious threat to food security. The stages of M. oryzae infection are well defined, with the formation of an appressorium, a cell type that allows penetration of the plant cuticle, particularly well studied. However, many of the key pathways and genes involved in this disease stage are yet to be identified...
January 17, 2017: Microorganisms
https://www.readbyqxmd.com/read/28106531/preclinical-characterization-of-the-novel-hcv-ns3-protease-inhibitor-gs-9256
#10
Huiling Yang, Chris Yang, Yujin Wang, Gerry Rhodes, Margaret Robinson, Guofeng Cheng, Xiaoping Qi, Hongmei Mo, Yang Tian, Rowchanak Pakdaman, X Christopher Sheng, Choung U Kim, William E Delaney
BACKGROUND: GS-9256 is an inhibitor of hepatitis C virus (HCV) NS3 protease with a macrocyclic structure and novel phosphinic acid pharmacophore. METHODS: Key preclinical properties of GS-9256 including in vitro antiviral activity, cross-resistance, and pharmacokinetic properties were investigated in non-human species. RESULTS: In genotype (GT) 1b Huh-luc cells with a replicon encoding luciferase, GS-9256 had a mean EC50 value of 20.0 nM, with minimal cytotoxicity...
January 20, 2017: Antiviral Therapy
https://www.readbyqxmd.com/read/28106371/enhancement-of-electrode-stability-using-platinum-cobalt-nanocrystals-on-a-novel-composite-sictic-support
#11
María Millán, Hector Zamora, Manuel Andrés Rodrigo, Justo Lobato
PtCo alloy catalysts for high temperature PEMFCs (Protonic Exchange Membrane Fuel Cells) were synthesized on a novel non-carbonaceous support (SiCTiC) using the impregnation method with NaBH4 as the reducing agent at different synthesis temperatures to evaluate the effect of this variable on their physicochemical and electrochemical properties. The catalysts were characterized by inductively coupled plasma optical emission spectrometry (ICP-OES), scanning electron microscopy-energy dispersive X-ray spectroscopy (SEM-EDX), X-ray diffraction (XRD), transmission electron microscope-energy dispersive X-ray (TEM) and temperature programmed reduction (TPR)...
January 20, 2017: ACS Applied Materials & Interfaces
https://www.readbyqxmd.com/read/28106295/macrophage-polarization-anti-cancer-strategies-to-target-tumor-associated-macrophage-in-breast-cancer
#12
Muhammad Tariq, Jieqiong Zhang, Guikai Liang, Ling Ding, Qiaojun He, Bo Yang
Tumor-associated macrophages (TAMs) are the most abundant inflammatory cells and orchestrate different stages of breast cancer development. TAMs participate in the tumor angiogenesis, matrix remodeling, invasion, immunosuppression, metastasis, and chemoresistance in breast cancer. Several clinical studies indicate the association between the high influx of TAMs in tumor with poor prognosis in hepatocellular, ovarian, cervical, and breast cancer. Previously developed hypotheses have proposed that TAMs participate in antitumor responses of the body, while recently many clinical and experimental studies have revealed that TAMs in tumor microenvironment predominantly resemble with M2-like polarized macrophages and produce a high amount of anti-inflammatory factors which are directly responsible for the development of tumor...
January 20, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28106283/therapeutic-potential-of-curcumin-in-treatment-of-pancreatic-cancer-current-status-and-future-perspectives
#13
Mina Hosseini, Seyed Mahdi Hassanian, Elham Mohamamdazade, Soodabeh ShahidSales, Mina Maftouh, Hasan Fayazbakhsh, Majid Khazaei, Amir Avan
Pancreatic cancer is among the leading cause of deaths due to cancer with extremely poor prognosis. Gemcitabine is being used in the treatment of patient with pancreatic ductal adenocarcinoma (PDAC), although, the response rate is bellow 12%. A recent phase III trial revealed that FOLFIRINOX could be an option for the treatment of metastatic PDAC patients, although it is associated with increased toxicity. Therefore, identification of novel agents that either improves gemcitabine activity, within novel combinatorial approaches, or with a better efficacy than gemcitabine is warranted...
January 20, 2017: Journal of Cellular Biochemistry
https://www.readbyqxmd.com/read/28105864/expression-and-purification-of-l-asparaginase-from-escherichia-coli-and-the-inhibitory-effects-of-cyclic-dipeptides
#14
Yanan Zhang, Dan Li, Yan Li
L-asparaginase, a key enzyme involved in nitrogen metabolism, is an effective anti-tumour agent. Cyclic dipeptides, a group of compounds, contain several important biological functions. In this paper, we proposed a novel method for L-asparaginase expression and purification from Echerichia coli and determined the effect of cyclic dipeptides on the enzymatic activity of recombinant L-asparaginase. The gene ansB encoding L-asparaginase was amplified from the genome of E. coli BL21 (DE3) by polymerase chain reaction and sub-cloned into pET-15b vector to construct expressing plasmid pET-15b-ansB...
January 20, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28105861/a-novel-benzimidazole-and-other-constituents-with-antiproliferative-and-antioxidant-properties-from-thymelaea-microphylla-coss-et-dur
#15
Labib Noman, Feyza Oke-Altuntas, Amar Zellagui, Ayse Sahin Yaglioglu, Ibrahim Demirtas, Susana M Cardoso, Salah Akkal, Noureddine Gherraf, Salah Rhouati
A new compound (microphybenzimidazole, 7) along with the six known compounds matairesinol (1), prestegane B (2), umbelliferone (3), daphnoretin (4), microphynolide A (5) and microphynolide B (6) were isolated from Thymelaea microphylla. The structures of the pure compounds were elucidated by spectroscopic and mass-spectrometric analyses, including 1D-, 2D-NMR, and HPLC-TOF/MS. Compounds 2 and 4, as well as three fractions (F6, F6-C5, and F6-W42) obtained from a 50% (v:v) CH2Cl2:MeOH extract exhibited a selective activity against rat brain glioma cells (C6)...
January 20, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28105561/the-rise-and-fall-of-anticoagulation-with-bivalirudin-during-percutaneous-coronary-interventions-a-review-article
#16
REVIEW
Constantinos Andreou, Christos Maniotis, Michael Koutouzis
Bivalirudin is a direct thrombin inhibitor used during percutaneous coronary intervention (PCI). Treatment with bivalirudin compared to heparin plus glycoprotein IIb/IIIa inhibitors (GPI) reduced bleeding complications, but resulted in higher rates of ischemic events, including acute stent thrombosis in ST segment elevation myocardial infarction (STEMI) patients. Thus, it may be considered a reasonable alternative antithrombotic agent in patients at high risk of bleeding undergoing PCI. However its superiority over heparin alone is questioned particularly in the era of novel antiplatelet agents and transradial PCI...
January 19, 2017: Cardiology and Therapy
https://www.readbyqxmd.com/read/28105297/follicular-lymphoma-the-management-of-elderly-patient
#17
REVIEW
Alessia Castellino, Elisa Santambrogio, Maura Nicolosi, Barbara Botto, Carola Boccomini, Umberto Vitolo
Follicular lymphoma (FL) is the most common indolent non-Hodgkin lymphoma, which typically affects mature adults and elderly, whose median age at diagnosis is 65 years. The natural history of FL appears to have been favorably impacted by the introduction of Rituximab. Randomized clinical trials demonstrated that the addition of rituximab to standard chemotherapy induction has improved the overall survival and new strategies of chemo-immunotherapy, such as Bendamustine combined with Rituximab, showed optimal results on response and reduced hematological toxicity, becoming one of the standard treatments, particularly in elderly patients...
2017: Mediterranean Journal of Hematology and Infectious Diseases
https://www.readbyqxmd.com/read/28105284/discovery-of-novel-seven-membered-prostacyclin-analogues-as-potent-and-selective-prostaglandin-fp-and-ep3-dual-agonists
#18
Isamu Sugimoto, Tohru Kambe, Tomotaka Okino, Tetsuo Obitsu, Nobukazu Ohta, Taihei Nishiyama, Akihiro Kinoshita, Taku Fujimoto, Hiromu Egashira, Shinsaku Yamane, Satoshi Shuto, Kousuke Tani, Toru Maruyama
A novel series of prostaglandin analogues with a seven-membered ring scaffold was designed, synthesized, and evaluated for the functional activation of prostaglandin receptors to identify potent and subtype-selective FP and EP3 dual agonists. Starting from the prostacyclin derivative 5b, a nonselective agonist for prostaglandin receptors, replacement of the core structure with an octahydro-2H-cyclopenta[b]oxepine scaffold led to the discovery of the potent and selective FP and EP3 dual agonist 11b as a lead compound for the development of an antiglaucoma agent...
January 12, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28105211/diagnostic-and-therapeutic-approaches-to-multiple-myeloma-patients-real-world-data-from-representative-multicentre-treatment-surveys-in-germany-between-2008-and-2011
#19
Thomas M Moehler, Maximilian Merz, Lenka Kellermann, Hartmut Goldschmidt, Wolfgang Knauf
A survey was conducted to investigate the standard of care for multiple myeloma in Germany, in order to clarify the status of implementation of international and national treatment guidelines. In addition, the changes in disease management over time were investigated by comparison with surveys conducted in 2008 and 2009. The survey captured a representative sample of 478 myeloma patients with a mean age of 67.9 years across various stages of the disease. Diagnostic approaches, prognostic aspects and treatment decisions were evaluated based on a survey conducted in 2011 in 58 representative centres in Germany, including university and non-university hospitals and office-based haematologists...
December 2016: Oncology Letters
https://www.readbyqxmd.com/read/28105206/curcumin-enhances-temsirolimus-induced-apoptosis-in-human-renal-carcinoma-cells-through-upregulation-of-yap-p53
#20
Shan Xu, Zheng Yang, Yizeng Fan, Bing Guan, Jing Jia, Yang Gao, Ke Wang, Kaijie Wu, Xinyang Wang, Pengsheng Zheng, Dalin He, Peng Guo
Curcumin has frequently been used as a therapeutic agent in the treatment of various types of disease and is known to enhance the drug sensitivity of cells. In the present study, the combined effect of curcumin and temsirolimus treatment on apoptosis in human renal cell carcinoma (RCC) cells was investigated. Temsirolimus is an inhibitor of the mechanistic target of rapamycin signaling pathway and used in the first-line treatment of metastatic RCC. It was demonstrated that curcumin combined with temsirolimus markedly induced apoptosis in RCC cells, however this effect was not observed following curcumin or temsirolimus treatment alone...
December 2016: Oncology Letters
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