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https://www.readbyqxmd.com/read/29786944/design-synthesis-and-evaluation-of-a-novel-series-of-inhibitors-reversing-p-glycoprotein-mediated-multidrug-resistance
#1
Hesham Ghaleb, Huilan Li, Mutta Kairuki, Qianqian Qiu, Xinzhou Bi, Chunxia Liu, Chen Liao, Jieming Li, Kamal Hezam, Wenlong Huang, Hai Qian
Multidrug resistance (MDR) is still the main barrier to attaining effective results with chemotherapy. Discovery of new chemo-reversal agents is needed to overcome MDR. Our study focused on a better way to obtain novel drugs with triazole rings that have an MDR-reversal ability through click chemistry. Among 20 developed compounds, compound 19 had a minimal cytotoxic effect compared to tariquidar and verapamil (VRP) and showed a higher reversal activity than VRP through increased accumulation in K562/A02 cells...
May 22, 2018: Chemical Biology & Drug Design
https://www.readbyqxmd.com/read/29786648/utilizing-optimized-tools-to-investigate-ptm-crosstalk-identifying-potential-ptm-crosstalk-of-acetylated-mitochondrial-proteins
#2
Henrick Horita, Andy Law, Kim Middleton
Post-translational modification (PTM) crosstalk is recognized as a major cell-regulatory mechanism, and studies of several proteins have validated the premise that PTMs work in concert. Previous work by our group investigated the potential PTM crosstalk on proteins in the EGFR-Ras-c-Fos axis by utilizing a comprehensive set of PTM reagents termed Signal-Seeker toolkits. In this study, these tools were used to investigate the potential PTM crosstalk that occurs in acetylated mitochondrial proteins in response to a mitochondrial stress-inducing agent hydrogen peroxide (H₂O₂)...
May 22, 2018: Proteomes
https://www.readbyqxmd.com/read/29786530/meta-analysis-of-safety-and-efficacy-of-oral-anti-coagulants-in-patients-requiring-catheter-ablation-for-atrial-fibrillation
#3
Hammad Rahman, Safi U Khan, Michael DePersis, Tehseen Hammad, Fahad Nasir, Edo Kaluski
BACKGROUND: The ideal oral anticoagulant agent during catheter ablation (CA) for atrial fibrillation (AF) remained unclear. HYPOTHESIS: Novel oral anticoagulants (NOACs) are safer and effective compared to uninterrupted vitamin K antagonists (U-VKA) among patients requiring CA for AF. METHODS: Four randomized controlled trials (RCTs) and 9 observational studies (OS) were selected using PubMed/Medline, EMBASE and the CENTRAL data bases (Inception-December-2017)...
May 9, 2018: Cardiovascular Revascularization Medicine: Including Molecular Interventions
https://www.readbyqxmd.com/read/29786164/air-activated-self-decontaminating-polydicyclopentadiene-polyhipe-foams-for-rapid-decontamination-of-chemical-warfare-agents
#4
Christopher L McGann, Grant C Daniels, Spencer L Giles, Robert B Balow, Jorge L Miranda-Zayas, Jeffrey G Lundin, James H Wynne
The threat of chemical warfare agents (CWA) compels research into novel self-decontaminating materials (SDM) for the continued safety of first-responders, civilians, and active service personnel. The capacity to actively detoxify, as opposed to merely sequester, offending agents under typical environmental conditions defines the added value of SDMs in comparison to traditional adsorptive materials. Porous polymers, synthesized via the high internal phase emulsion (HIPE) templating, provide a facile fabrication method for materials with permeable open cellular structures that may serve in air filtration applications...
May 22, 2018: Macromolecular Rapid Communications
https://www.readbyqxmd.com/read/29786121/genome-sequence-of-the-novel-virulent-bacteriophage-pmbt14-with-lytic-activity-against-pseudomonas-fluorescens-dsm-50090-r
#5
Sabrina Koberg, Stefanie Gieschler, Erik Brinks, Mareike Wenning, Horst Neve, Charles M A P Franz
Psychrotrophic gram-negative Pseudomonas spp. represent a serious problem in the dairy industry as they can cause spoilage of milk and dairy products. Bacteriophages have moved into focus as promising biocontrol agents for such food spoilage bacteria. The virulent Siphoviridae phage PMBT14 was isolated on a mutant variant of P. fluorescens DSM 50090 challenged with an unrelated virulent P. fluorescens DSM 50090 Podoviridae phage (i.e., mutant strain DSM 50090R ). PMBT14 has a 47,820-bp dsDNA genome with 76 predicted open reading frames (ORFs)...
May 21, 2018: Archives of Virology
https://www.readbyqxmd.com/read/29786099/cluster-to-cluster-transformation-among-au-6-au-8-and-au-11-nanoclusters
#6
Xiuqing Ren, Junhong Fu, Xinzhang Lin, Xuemei Fu, Jinghui Yan, Ren'an Wu, Chao Liu, Jiahui Huang
We present the cluster-to-cluster transformations among three gold nanoclusters, [Au6(dppp)4]2+ (Au6), [Au8(dppp)4Cl2]2+ (Au8) and [Au11(dppp)5]3+ (Au11). The conversion process follows a rule that states that the transformation of a small cluster to a large cluster is achieved through an oxidation process with an oxidizing agent (H2O2) or with heating, while the conversion of a large cluster to a small one occurs through a reduction process with a reducing agent (NaBH4). All the reactions were monitored using UV-Vis spectroscopy and ESI-MS...
May 22, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/29786070/selective-elimination-of-senescent-cells-by-mitochondrial-targeting-is-regulated-by-ant2
#7
Sona Hubackova, Eliska Davidova, Katerina Rohlenova, Jan Stursa, Lukas Werner, Ladislav Andera, LanFeng Dong, Mikkel G Terp, Zdenek Hodny, Henrik J Ditzel, Jakub Rohlena, Jiri Neuzil
Cellular senescence is a form of cell cycle arrest that limits the proliferative potential of cells, including tumour cells. However, inability of immune cells to subsequently eliminate senescent cells from the organism may lead to tissue damage, inflammation, enhanced carcinogenesis and development of age-related diseases. We found that the anticancer agent mitochondria-targeted tamoxifen (MitoTam), unlike conventional anticancer agents, kills cancer cells without inducing senescence in vitro and in vivo. Surprisingly, it also selectively eliminates both malignant and non-cancerous senescent cells...
May 21, 2018: Cell Death and Differentiation
https://www.readbyqxmd.com/read/29785557/highly-sensitive-ethanol-chemical-sensor-based-on-novel-ag-doped-mesoporous-%C3%AE-fe-2-o-3-prepared-by-modified-sol-gel-process
#8
Moteb M Alqahtani, Atif M Ali, Farid A Harraz, M Faisal, Adel A Ismail, Mahmoud A Sayed, M S Al-Assiri
Mesoporous α-Fe2 O3 has been synthesized via a simple sol-gel procedure in the presence of Pluronic (F-127) triblock copolymer as structure directing agent. Silver (Ag) nanoparticles were deposited onto α-Fe2 O3 matrix by the photochemical reduction approach. Morphological analysis revealed the formation of Ag nanoparticles with small sizes < 20 nm onto the mesoporous structure of α-Fe2 O3 possessing < 50 nm semi-spherical shape. The XRD, FTIR, Raman, UV-vis, PL, and N2 sorption isotherm studies confirmed the high crystallinity, mesoporosity, and optical characteristics of the synthesized product...
May 21, 2018: Nanoscale Research Letters
https://www.readbyqxmd.com/read/29785529/isolation-and-characterization-of-bacillus-sp-gfp-2-a-novel-bacillus-strain-with-antimicrobial-activities-from-whitespotted-bamboo-shark-intestine
#9
Jia Wu, Guoqiang Xu, Yangyang Jin, Cong Sun, Li Zhou, Guodong Lin, Rong Xu, Ling Wei, Hui Fei, Dan Wang, Jianqing Chen, Zhengbing Lv, Kuancheng Liu
The abuse of antibiotics and following rapidly increasing of antibiotic-resistant pathogens is the serious threat to our society. Natural products from microorganism are regarded as the important substitution antimicrobial agents of antibiotics. We isolated a new strain, Bacillus sp. GFP-2, from the Chiloscyllium plagiosum (Whitespotted bamboo shark) intestine, which showed great inhibitory effects on the growth of both Gram-positive and Gram-negative bacteria. Additionally, the growth of salmon was effectively promoted when fed with inactivated strain GFP-2 as the inhibition agent of pathogenic bacteria...
May 22, 2018: AMB Express
https://www.readbyqxmd.com/read/29785428/1-methyl-4-aryl-urazole-maura-labels-tyrosine-in-proximity-to-ruthenium-photocatalysts
#10
Shinichi Sato, Kensuke Hatano, Michihiko Tsushima, Hiroyuki Nakamura
We designed and synthesised peptides conjugated with proline linkers and ruthenium photocatalysts. These peptides were used as substrates to evaluate the photocatalyst-proximity dependences of candidates for tyrosine labelling reagents. The 1-methyl-4-aryl-urazole (MAUra) structure was found to be a novel tyrosyl radical trapping agent to label tyrosine residues effectively under the conditions where the ruthenium photocatalyst and tyrosine were in close proximity. Using a ruthenium photocatalyst conjugated to a carbonic anhydrase ligand, the target protein in a complex protein mixture was labelled with remarkable target selectivity by azide- or desthiobiotin-conjugated MAUra derivatives...
May 22, 2018: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/29785331/nodular-basal-cell-carcinoma-of-the-face-successfully-treated-with-ingenol-mebutate-0-015-gel
#11
Silvia S Iannazzone, Vito Ingordo
Surgical excision is the first-choice treatment for basal cell carcinoma (BCC). Other treatments with topical agents such as 5-fluorouracil or imiquimod have also been suggested for use in superficial BCC (sBCC). Ingenol mebutate (IM) is a novel agent employed in the treatment of superficial actinic keratoses. The drug has been also successfully used in the treatment of sBCC. A case of large nodular BCC (nBCC) of the face in a 100-year-old inoperable woman is described. IM 0.015% gel was applied once daily for three consecutive days...
April 2018: Dermatology Practical & Conceptual
https://www.readbyqxmd.com/read/29785244/more-than-just-an-immunosuppressant-the-emerging-role-of-fty720-as-a-novel-inducer-of-ros-and-apoptosis
#12
REVIEW
Teruaki Takasaki, Kanako Hagihara, Ryosuke Satoh, Reiko Sugiura
Fingolimod hydrochloride (FTY720) is a first-in-class of sphingosine-1-phosphate (S1P) receptor modulator approved to treat multiple sclerosis by its phosphorylated form (FTY720-P). Recently, a novel role of FTY720 as a potential anticancer drug has emerged. One of the anticancer mechanisms of FTY720 involves the induction of reactive oxygen species (ROS) and subsequent apoptosis, which is largely independent of its property as an S1P modulator. ROS have been considered as a double-edged sword in tumor initiation/progression...
2018: Oxidative Medicine and Cellular Longevity
https://www.readbyqxmd.com/read/29785182/reactive-oxygen-species-generation-in-human-cells-by-a-novel-magnetic-resonance-imaging-contrast-agent
#13
Li Wang, Eric Lin, Mary J Johansen, Timothy Madden, Edward Felix, Karen S Martirosyan, Steven J Frank
The novel positive-contrast magnetic resonance imaging (MRI) marker C4 consists of an aqueous solution of cobalt chloride (CoCl2 ) complexed with the chelator N-acetylcysteine (NAC). We evaluated whether the presence of C4 or its components would produce reactive oxygen species (ROS, including hydroxyl, peroxyl, or other reactive oxygen species) in cultured cells. Human cancer or normal cells were incubated with 1% (w/v) CoCl2 ·6H2 O or 2% NAC or a combination of both (1% CoCl2 ·6H2 O : 2% NAC in an aqueous solution, abbreviated as Co : NAC) in the presence or absence of H2 O2 ...
2018: Journal of Toxicology
https://www.readbyqxmd.com/read/29785179/nanoformulation-of-brain-derived-neurotrophic-factor-with-target-receptor-triggered-release-in-the-central-nervous-system
#14
Yuhang Jiang, James M Fay, Chi-Duen Poon, Natasha Vinod, Yuling Zhao, Kristin Bullock, Si Qin, Devika S Manickam, Xiang Yi, William A Banks, Alexander V Kabanov
Brain-derived neurotrophic factor (BDNF) is identified as a potent neuroprotective and neuroregenerative agent for many neurological diseases. Regrettably, its delivery to the brain is hampered by poor serum stability and rapid brain clearance. Here, a novel nanoformulation is reported composed of a bio-compatible polymer, poly(ethylene glycol)- b -poly(L-glutamic acid) (PEG-PLE), that hosts the BDNF molecule in a nanoscale complex, termed here Nano-BDNF. Upon simple mixture, Nano-BDNF spontaneously forms uniform spherical particles with a core-shell structure...
February 7, 2018: Advanced Functional Materials
https://www.readbyqxmd.com/read/29785122/aloperine-executes-antitumor-effects-through-the-induction-of-apoptosis-and-cell-cycle-arrest-in-prostate-cancer-in-vitro-and-in-vivo
#15
Zhixin Ling, Han Guan, Zonghao You, Can Wang, Ling Hu, Lei Zhang, Yiduo Wang, Shuqiu Chen, Bin Xu, Ming Chen
Background: Prostate cancer (PCa) is one of the most common malignant diseases among male patients. Although androgen deprivation therapy remains the main treatment for PCa, most patients would inevitably progress to castration-resistant PCa, which is the main cause of cancer-related deaths. Thus, novel antitumor agents are urgently needed. Recent studies demonstrated that aloperine (ALO) as a natural alkaloid showed antitumor effects in other cancer types. However, the biological function and underlying mechanisms of ALO in PCa have not been investigated...
2018: OncoTargets and Therapy
https://www.readbyqxmd.com/read/29785107/near-infrared-light-mediated-photodynamic-photothermal-therapy-nanoplatform-by-the-assembly-of-fe-3-o-4-carbon-dots-with-graphitic-black-phosphorus-quantum-dots
#16
Ming Zhang, Wentao Wang, Yingjun Cui, Ninglin Zhou, Jian Shen
Background: Recently, combined photodynamic therapy (PDT) and photothermal therapy (PTT) has become a desired treatment for cancer. However, the development of economic, high-efficiency, and safe photosensitizers/photothermal agents remains a significant challenge. Methods: A novel nanocomposite has been developed via the assembly of iron oxide carbon dot (Fe3 O4 -CDs) nanoparticles and black phosphorus quantum dots (genipin [GP]-polyglutamic acid [PGA]-Fe3 O4 -CDs@BPQDs), and this nanocomposite shows a broad light-absorption band and a photodegradable character...
2018: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/29784856/a-cell-surface-aggregation-promoting-factor-from-lactobacillus-gasseri-contributes-towards-inhibition-of-trichomonas-vaginalis-adhesion-to-human-vaginal-ectocervical-cells
#17
Niha Phukan, Anna E S Brooks, Augusto Simoes-Barbosa
Trichomoniasis, a prevalent sexually transmitted infection, is commonly symptomatic in women. The causative agent is Trichomonas vaginalis , an extracellular protozoan parasite. The host-protective mechanisms and molecules of vaginal lactobacilli that could counteract with this pathogen are largely unknown. This study examines the inhibition promoted by Lactobacillus gasseri against the adhesion of T. vaginalis to host cells, a critical virulence aspect of this pathogen. We observed that the vaginal L. gasseri ATCC 9857 is highly inhibitory by various contact-dependent mechanisms and surface proteins are largely responsible for this inhibitory phenotype...
May 21, 2018: Infection and Immunity
https://www.readbyqxmd.com/read/29784842/eucast-determination-of-olorofim-f901318-susceptibility-of-mould-species-method-validation-and-mics
#18
Karin Meinike Jørgensen, Karen M T Astvad, Rasmus Krøger Hare, Maiken Cavling Arendrup
Olorofim is a novel antifungal agent with in vitro activity against Aspergillus and some other moulds. Here we addressed technical aspects for EUCAST olorofim testing and generated contemporary MIC data.EUCAST E.Def 9.3.1 testing was performed comparing two plate preparation methods (serial-dilution in medium (serial-plates) versus pre-dilution in DMSO (ISO-plates)), two lots of olorofim, visual (visual-MIC) versus spectrophotometer (spec-MIC) reading and four polystyrene plates using 34-53 Aspergillus isolates from five genera...
May 21, 2018: Antimicrobial Agents and Chemotherapy
https://www.readbyqxmd.com/read/29784744/the-changing-treatment-landscape-for-metastatic-urothelial-carcinoma
#19
Thomas W Flaig
Urothelial carcinoma is the predominant histologic type of bladder cancer. After 30 years of minimal progress in the treatment of advanced-stage disease, recent advances in the genomic characterization of urothelial cancer and breakthroughs in bladder cancer therapeutics have rejuvenated the field. Nivolumab, pembrolizumab, atezolizumab, durvalumab, and avelumab are among the exciting recent novel therapeutic advances gaining approvals by the FDA for treatment of advanced-stage urothelial carcinoma. Yet the challenge for clinicians is to determine the optimal choice of agents as first-line or second-line therapy and which offers the best chance for overall survival for the individual patient in this rapidly changing field...
May 2018: Journal of the National Comprehensive Cancer Network: JNCCN
https://www.readbyqxmd.com/read/29784737/nccn-guidelines-updates-breast-cancer
#20
Sharon H Giordano, Anthony D Elias, William J Gradishar
The emergence of CDK4/6 inhibitors has changed the treatment algorithm for advanced/metastatic estrogen receptor-positive breast cancer. In pivotal trials of palbociclib, ribociclib, and abemaciclib, doubling in progression-free survival has been seen. All 3 agents in this class are now included in the NCCN Guidelines for Breast Cancer, and clinicians should be incorporating these agents into their treatment algorithms. The other important issue in this breast cancer setting is extended duration of endocrine therapy...
May 2018: Journal of the National Comprehensive Cancer Network: JNCCN
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