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https://www.readbyqxmd.com/read/28641157/design-synthesis-and-structure-activity-relationship-studies-of-a-novel-focused-library-of-2-3-4-substituted-oxazolidines-with-antiproliferative-activity-against-cancer-cell-lines
#1
Saulo F Andrade, Bárbara G Oliveira, Larissa C Pereira, Jonas P Ramos, Angélica R Joaquim, Martin Steppe, Elaine M Souza-Fagundes, Ricardo J Alves
In the present work we describe the synthesis and antiproliferative evaluation of a focused library of 30 novel oxazolidines designed by modification of N-substituent, by ring variation, by alkyl variation or by extension of the structure. It was noted that carbamate and N,O-aminal groups were essential for activity. In general, replacement of the phenyl ring with pyridinyl was not tolerated. However, the introduction of a second phenyl ring with an appropriate spacer at the 3- or 4-position of the first phenyl ring generally enhanced the cytotoxic profile...
June 12, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28641100/bruton-s-tyrosine-kinase-btk-as-a-promising-target-in-solid-tumors
#2
REVIEW
J Molina-Cerrillo, T Alonso-Gordoa, P Gajate, E Grande
Bruton's tyrosine kinase (BTK) is a non-receptor intracellular kinase that belongs to the TEC-family tyrosine kinases together with bone marrow-expressed kinase (BMX), redundant-resting lymphocyte kinase (RLK), and IL-2 inducible T-Cell kinase (ITK). All these proteins play a key role in the intracellular signaling of both B and T lymphocytes. Recently, some preclinical data have demonstrated that BTK is present in certain tumor subtypes and in other relevant cells that are contributing to the tumor microenvironment such as dendritic cells, macrophages, myeloid derived suppressor cells and endothelial cells...
June 9, 2017: Cancer Treatment Reviews
https://www.readbyqxmd.com/read/28641053/the-discovery-and-development-of-romidepsin-for-the-treatment-of-t-cell-lymphoma
#3
Piotr Smolewski, Tadeusz Robak
Romidepsin is a potent and selective inhibitor of histone deacetylases (HDCAi). It is also the only bicyclic inhibitor to undergo clinical assessment and is considered a promising drug for the treatment of T-cell lymphomas. The cellular action of romidepsin results in enhanced histone acetylation, as well as the acetylation of other nuclear or cytoplasmic proteins, influencing cell cycle, apoptosis, and angiogenesis. In phase II studies involving patients with relapsed or refractory of cutaneous T-cell lymphoma (CTCL) and peripheral T-cell lymphoma (PTCL), romidepsin produced overall response rates (ORR) of 34-35% and 25-38%, with complete response (CR) rates of 6% and 15-18%, respectively...
June 22, 2017: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/28640990/opiate-antagonists-do-not-interfere-with-the-clinical-benefits-of-stimulants-in-adhd-a-double-blind-placebo-controlled-trial-of-the-mixed-opioid-receptor-antagonist-naltrexone
#4
Thomas J Spencer, Pradeep Bhide, Jinmin Zhu, Stephen V Faraone, Maura Fitzgerald, Amy M Yule, Mai Uchida, Andrea E Spencer, Anna M Hall, Ariana J Koster, Joseph Biederman
OBJECTIVE: Methylphenidate activates μ-opioid receptors, which are linked to euphoria. μ-Opioid antagonists, such as naltrexone, may attenuate the euphoric effects of stimulants, thereby minimizing their abuse potential. This study assessed whether the combination of naltrexone with methylphenidate is well-tolerated while preserving the clinical benefits of stimulants in subjects with attention-deficit/hyperactivity disorder (ADHD). METHODS: We conducted a 6-week, double-blind, placebo-controlled, randomized clinical trial of naltrexone in adults with DSM-IV ADHD receiving open treatment with a long-acting formulation of methylphenidate from January 2013 to July 2015...
June 20, 2017: Journal of Clinical Psychiatry
https://www.readbyqxmd.com/read/28640934/substrate-specificity-and-safener-inducibility-of-the-plant-udp-glucose-dependent-family-1-glycosyltransferases-super-family
#5
Melissa Brazier-Hicks, Markus Gershater, David Dixon, Robert Edwards
Plants contain large numbers of family 1 UDP-glucose dependent glycosyltransferases (UGTs), including members that conjugate xenobiotics. Arabidopsis contains 107 UGT genes with 99 family members successfully expressed as glutathione transferase (GST)-fusion proteins in E.coli. A high-throughput catalytic screen was developed based on quantification of the fusion by measuring GST activity. UGT activity using UDP-glucose as donor was then determined using 11 synthetic acceptors bearing hydroxyl, amino and thiol groups that had been shown to undergo conjugation in plant extracts...
June 22, 2017: Plant Biotechnology Journal
https://www.readbyqxmd.com/read/28640868/functional-metabolomics-as-a-tool-to-analyze-mediator-function-and-structure-in-plants
#6
Celine Davoine, Ilka N Abreu, Khalil Khajeh, Jeanette Blomberg, Brendan N Kidd, Kemal Kazan, Peer M Schenk, Lorenz Gerber, Ove Nilsson, Thomas Moritz, Stefan Björklund
Mediator is a multiprotein transcriptional co-regulator complex composed of four modules; Head, Middle, Tail, and Kinase. It conveys signals from promoter-bound transcriptional regulators to RNA polymerase II and thus plays an essential role in eukaryotic gene regulation. We describe subunit localization and activities of Mediator in Arabidopsis through metabolome and transcriptome analyses from a set of Mediator mutants. Functional metabolomic analysis based on the metabolite profiles of Mediator mutants using multivariate statistical analysis and heat-map visualization shows that different subunit mutants display distinct metabolite profiles, which cluster according to the reported localization of the corresponding subunits in yeast...
2017: PloS One
https://www.readbyqxmd.com/read/28640834/overexpression-of-gmfdl19-enhances-tolerance-to-drought-and-salt-stresses-in-soybean
#7
Yuanyuan Li, Quanzhen Chen, Haiyang Nan, Xiaoming Li, Sijia Lu, Xiaohui Zhao, Baohui Liu, Changhong Guo, Fanjiang Kong, Dong Cao
The basic leucine zipper (bZIP) family of transcription factors plays an important role in the growth and developmental process as well as responds to various abiotic stresses, such as drought and high salinity. Our previous work identified GmFDL19, a bZIP transcription factor, as a flowering promoter in soybean, and the overexpression of GmFDL19 caused early flowering in transgenic soybean plants. Here, we report that GmFDL19 also enhances tolerance to drought and salt stress in soybean. GmFDL19 was determined to be a group A member, and its transcription expression was highly induced by abscisic acid (ABA), polyethylene glycol (PEG 6000) and high salt stresses...
2017: PloS One
https://www.readbyqxmd.com/read/28637347/mechanisms-underlying-the-long-term-survival-of-the-monocot-dracaena-marginata-under-drought-conditions
#8
Radek Jupa, Roman Plichta, Zuzana Paschová, Nadezhda Nadezhdina, Roman Gebauer
Efficient water management is essential for the survival of vascular plants under drought stress. While interrelations among drought stress, plant anatomy and physiological functions have been described in woody dicots, similar research is very limited for non-palm arborescent and shrubby monocots despite their generally high drought tolerance. In this study, potted transplants of Dracaena marginata Lam. in primary growth stage were exposed to several short- and long-term drought periods. Continuous measurements of sap flow and stem diameter, the evaluation of capacitance and leaf conductance, the quantification of non-structural carbohydrates (NSC), and organ-specific anatomical analyses were performed to reveal the mechanisms promoting plant resistance to limited soil moisture...
June 14, 2017: Tree Physiology
https://www.readbyqxmd.com/read/28636538/phase-i-dose-escalation-study-of-the-c-met-tyrosine-kinase-inhibitor-sar125844-in-asian-patients-with-advanced-solid-tumors-including-patients-with-met-amplified-gastric-cancer
#9
Kohei Shitara, Tae Min Kim, Tomoya Yokota, Masahiro Goto, Taroh Satoh, Jin-Hee Ahn, Hyo Song Kim, Sylvie Assadourian, Corinne Gomez, Marzia Harnois, Satoshi Hamauchi, Toshihiro Kudo, Toshihido Doi, Yung-Jue Bang
SAR125844 is a potent and selective inhibitor of the c-Met kinase receptor. This was an open-label, phase I, multicenter, dose-escalation, and dose-expansion trial of SAR125844 in Asian patients with solid tumors, a subgroup of whom had gastric cancer and MET amplification (NCT01657214). SAR125844 was administered by intravenous infusion (260-570 mg/m2) on days 1, 8, 15, and 22 of each 28-day cycle. Objectives were to determine the maximum tolerated dose (MTD) and to evaluate SAR125844 safety and pharmacokinetic profile...
June 16, 2017: Oncotarget
https://www.readbyqxmd.com/read/28636366/oxygenation-via-c-h-c-c-bond-activation-with-molecular-oxygen
#10
Yu-Feng Liang, Ning Jiao
The selective oxidation of organic molecules is a fundamentally important component of modern synthetic chemistry. In the past decades, direct oxidative C-H and C-C bond functionalization has proved to be one of the most efficient and straightforward methods to synthesize complex products from simple and readily available starting materials. Among these oxidative processes, the use of molecular oxygen as a green and sustainable oxidant has attracted considerable attention because of its highly atom-economical, abundant, and environmentally friendly characteristics...
June 21, 2017: Accounts of Chemical Research
https://www.readbyqxmd.com/read/28636266/marap2-4-a-waterlogging-responsive-erf-from-mentha-regulates-bidirectional-sugar-transporter-atsweet10-to-modulate-stress-response-in-arabidopsis
#11
Ujjal J Phukan, Gajendra Singh Jeena, Vineeta Tripathi, Rakesh Kumar Shukla
As waterlogging and successive events severely influence growth and development of economically important plants, we attempted to characterize the role of a waterlogging-responsive Group I (A-6) Ethylene response factor (MaRAP2-4) from Mentha arvensis. Waterlogging, ethylene and Methyl jasmonate rapidly induced the expression of MaRAP2-4. MaRAP2-4 interacted with multiple cis-elements like Dehydration response elements (DRE1/2), Anoxia/Jasmonic acid response element (JARE) and GCC box showing its involvement in multiple responses...
June 21, 2017: Plant Biotechnology Journal
https://www.readbyqxmd.com/read/28636208/a-phase-i-trial-of-prn1008-a-novel-reversible-covalent-inhibitor-of-bruton-s-tyrosine-kinase-in-healthy-volunteers
#12
Patrick F Smith, Janakan Krishnarajah, Philip A Nunn, Ron J Hill, Dane Karr, D Tam, Mohammad Masjedizadeh, Jens O Funk, Steve G Gourlay
AIM: To evaluate the safety, tolerability, and PK/PD of PRN1008, a novel BTK inhibitor, in healthy volunteers, and thus determine the dose range for future clinical studies. METHODS: This was a two-part randomized, placebo controlled study in healthy volunteers using a liquid formulation. Part I was a single ascending dose design with dose levels of 50 to 1200 mg (n=6 active, 2 placebo per cohort); Part II was a multiple ascending dose design, with dose regimens ranging from 300 mg to 900 mg daily, either qd or bd for 10 days...
June 21, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28636204/aerobic-exercise-training-for-adults-with-fibromyalgia
#13
REVIEW
Julia Bidonde, Angela J Busch, Candice L Schachter, Tom J Overend, Soo Y Kim, Suelen M Góes, Catherine Boden, Heather Ja Foulds
BACKGROUND: Exercise training is commonly recommended for individuals with fibromyalgia. This review is one of a series of reviews about exercise training for people with fibromyalgia that will replace the "Exercise for treating fibromyalgia syndrome" review first published in 2002. OBJECTIVES: • To evaluate the benefits and harms of aerobic exercise training for adults with fibromyalgia• To assess the following specific comparisons ० Aerobic versus control conditions (eg, treatment as usual, wait list control, physical activity as usual) ० Aerobic versus aerobic interventions (eg, running vs brisk walking) ० Aerobic versus non-exercise interventions (eg, medications, education) We did not assess specific comparisons involving aerobic exercise versus other exercise interventions (eg, resistance exercise, aquatic exercise, flexibility exercise, mixed exercise)...
June 21, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28636035/development-of-air-stable-hydrogen-evolution-catalysts
#14
Biswajit Mondal, Abhishek Dey
Obtaining abundant pure hydrogen by reduction of water has an important implication in the development of clean and renewable energy. Hence research focused on the development of non-noble metal based facile and energy efficient catalysts for proton reduction is on the rise. However, for practical utilization, it is necessary that these complexes function unabated in the presence of atmospheric oxygen and other common contaminants in abundant water sources. There has been very little activity towards the development of oxygen-tolerant hydrogen producing catalysts...
June 21, 2017: Chemical Communications: Chem Comm
https://www.readbyqxmd.com/read/28635957/itk-signalling-via-the-ras-irf4-pathway-regulates-the-development-and-function-of-tr1-cells
#15
Weishan Huang, Sabrina Solouki, Nicholas Koylass, Song-Guo Zheng, Avery August
Type 1 regulatory T (Tr1) cells differentiate in response to signals engaging the T cell receptor (TCR), express high levels of the immunosuppressive cytokine IL-10, but not Foxp3, and can suppress inflammation and promote immune tolerance. Here we show that ITK, an important modulator of TCR signalling, is required for the TCR-induced development of Tr1 cells in various organs, and in the mucosal system during parasitic and viral infections. ITK kinase activity is required for mouse and human Tr1 cell differentiation...
June 21, 2017: Nature Communications
https://www.readbyqxmd.com/read/28635194/volitional-rehabilitative-assessments-in-patients-admitted-in-a-post-intensive-care-step-down-unit-a-feasibility-study
#16
Mara Paneroni, Francesco D' Abrosca, Georges Fokom, Laura Comini, Michele Vitacca
A high variability in functional tests and activities used during the pulmonary rehabilitation has been observed in post-intensive care unit (ICU) patients, and the best battery of tests to adopt has not been described yet. We tested in patients admitted in a post-ICU Step Down Unit the ability to perform the more frequent functional volitional tests. The relations of each single volitional test with general disability and dyspnea at discharge were also evaluated. Ten volitional tests including: bedside spirometry test (ST: FEV1%, FVC%), maximal inspiratory pressure (MIP), maximal expiratory pressure (MEP), Peak Expiratory Flow during Cough (PCEF), Quadriceps Muscle Strength (QMS), latissimus Dorsi and teres Major Strength (DMS), Brachial biceps Muscle Strength (BMS), effort tolerance measured by sit-to-stand test, Takahashi test and 6-Min Walking Test (6MWT), were evaluated in post-ICU patients at entry and discharge from in-hospital rehabilitation...
May 18, 2017: Monaldi Archives for Chest Disease, Archivio Monaldi Per le Malattie del Torace
https://www.readbyqxmd.com/read/28634850/novel-vitamin-b12-producing-enterococcus-spp-and-preliminary-in-vitro-evaluation-of-probiotic-potentials
#17
Ping Li, Qing Gu, Yuejiao Wang, Yue Yu, Lanlan Yang, Jieyan V Chen
Vitamin B12 is an essential nutrient required for crucial metabolic processes in humans. Vitamin B12-producing lactic acid bacteria (LAB) have been attracting increased attentions currently because of the generally recognized as safe (GRAS) status. Most of recent studies focused on Lactobacillus, and little is known about B12-producing Enterococcus. In the present study, five Enterococcus strains isolated from infant feces were identified as vitamin B12 producers. Among them, Enterococcus faecium LZ86 had the highest B12 production (499...
June 20, 2017: Applied Microbiology and Biotechnology
https://www.readbyqxmd.com/read/28634812/semi-industrial-scale-production-of-a-new-yeast-with-probiotic-traits-cryptococcus-sp-ymhs-isolated-from-the-red-sea
#18
Ashraf F El-Baz, Hesham A El-Enshasy, Yousseria M Shetaia, Hoda Mahrous, Nor Zalina Othman, Ahmed E Yousef
A new yeast strain with promising probiotic traits was isolated from the Red Sea water samples. The isolate (YMHS) was subjected to genetic characterization and identified as Cryptococcus sp. Nucleotide sequence analysis of the rRNA gene internal transcribed spacer regions showed 95% sequence similarity between the isolate and Cryptococcus albidus. Cryptococcus sp. YMHS exhibited desirable characteristics of probiotic microorganisms; it has tolerance to low pH in simulated gastric juice, resistance to bile salts, hydrophobic characteristics, broad antimicrobial activity, and in vitro ability to degrade cholesterol...
June 20, 2017: Probiotics and Antimicrobial Proteins
https://www.readbyqxmd.com/read/28634682/searching-for-the-sweet-spot-the-foot-rotation-and-parallel-engagement-of-ankle-ligaments-in-maximizing-injury-tolerance
#19
Bingbing Nie, Jason L Forman, Alexander R Mait, John-Paul Donlon, Matthew B Panzer, Richard W Kent
Ligament sprains, defined as tearing of bands of fibrous tissues within ligaments, account for a majority of injuries to the foot and ankle complex in field-based sports. External rotation of the foot is considered the primary injury mechanism of syndesmotic ankle sprains with concomitant flexion and inversion/eversion associated with particular patterns of ligament trauma. However, the influence of the magnitude and direction of loading vectors to the ankle on the in situ stress state of the ligaments has not been quantified in the literature...
June 20, 2017: Biomechanics and Modeling in Mechanobiology
https://www.readbyqxmd.com/read/28634536/telavancin-a-novel-semisynthetic-lipoglycopeptide-agent-to-counter-the-challenge-of-resistant-gram-positive-pathogens
#20
REVIEW
Biswadeep Das, Chayna Sarkar, Debasmita Das, Amit Gupta, Arnav Kalra, Shubham Sahni
Telavancin (TD-6424), a semisynthetic lipoglycopeptide vancomycin-derivative, is a novel antimicrobial agent developed by Theravance for overcoming resistant Gram-positive bacterial infections, specifically methicillin-resistant Staphylococcus aureus (MRSA). The US Food and Drug Administration (USFDA) had approved telavancin in 2009 for the treatment of complicated skin and skin structure infections (cSSSIs) caused by Gram-positive bacteria, including MRSA (S. aureus, Streptococcus agalactiae, Streptococcus pyogenes, Streptococcus anginosus group, or Enterococcus faecalis)...
March 2017: Therapeutic Advances in Infectious Disease
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