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https://www.readbyqxmd.com/read/27915169/replacing-the-terminal-piperidine-in-ceritinib-with-aliphatic-amines-confers-activities-against-crizotinib-resistant-mutants-including-g1202r
#1
Gangadhar Rao Mathi, Chung Hyo Kang, Heung Kyoung Lee, Raghavendra Achary, Ha-Yeon Lee, Joo-Youn Lee, Jae Du Ha, Sunjoo Ahn, Chi Hoon Park, Chong Ock Lee, Jong Yeon Hwang, Chang-Soo Yun, Hee Jung Jung, Sung Yun Cho, Hyoung Rae Kim, Pilho Kim
The piperidine fragment in ceritinib was replaced with diverse aliphatic amines to improve inherent resistance issues of ceritinib. While most of the prepared compounds exhibit as similar in vitro activities as ceritinib, compound 10 shows encouraging activities against wild-type ALK as well as crizotinib-resistant mutants including extremely resistant G1202R mutant with an IC50 of 1.8 nM. Furthermore, pharmacokinetic profiles of 10 is apparently better than that of ceritinib. In murine xenograft studies, compound 10 turns out to be as active as ceritinib, suggesting that further optimization of 10 may lead to clinical candidates overcoming ALK mutant issues...
November 24, 2016: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27915140/two-zinc-aminoclays-in-vitro-cytotoxicity-assessment-in-hela-cells-and-in-vivo-embryotoxicity-assay-in-zebrafish
#2
Hang-Suk Chun, Duckshin Park, Song Eun Lim, Kwang-Hun Jeong, Ji-Seon Park, Han-Jin Park, Shinyoung Kang, Kyoung Suk Kang, Hyun Gyu Park, Ha-Rim An, Yun Suk Huh, Young-Chul Lee
Two zinc-aminoclays [ZnACs] with functionalized primary amines [(-CH2)3NH2] were prepared by a simple sol-gel reaction using cationic metal precursors of ZnCl2 and Zn(NO3)2 with 3-aminopropyl triethoxysilane [APTES] under ambient conditions. Due to the facile interaction of heavy metals with primary amine sites and Zn-related intrinsic antimicrobial activity, toxicity assays of ZnACs nanoparticles (NPs) prior to their environmental and human-health applications are essential. However, such reports remain rare...
December 1, 2016: Ecotoxicology and Environmental Safety
https://www.readbyqxmd.com/read/27915078/analgesic-effect-of-coumarins-from-radix-angelicae-pubescentis-is-mediated-by-inflammatory-factors-and-trpv1-in-a-spared-nerve-injury-model-of-neuropathic-pain
#3
Ruili Li, Chao Zhao, Minna Yao, Ying Song, Yin Wu, Aidong Wen
ETHNOPHARMACOLOGICAL RELEVANCE: Coumarins from Radix angelicae pubescentis (CRAP) are a major active component that are isolated from dried roots of Angelica biserrata Yuan et Shan, which has been used clinically to cure headaches for a long period of time, and it is an effective treatment for pain. The aim of the present study was to investigate the analgesic effect of CRAP on a spared nerve injury (SNI) model of neuropathy. MATERIALS AND METHODS: Antinociceptive effects of CRAP were assessed in Sprague-Dawley male rats using a spared nerve injury model of neuropathic pain...
November 30, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/27914985/combination-therapy-with-doxorubicin-loaded-galactosylated-poly-ethyleneglycol-lithocholic-acid-to-suppress-the-tumor-growth-in-an-orthotopic-mouse-model-of-liver-cancer
#4
Bijay Singh, Yoonjeong Jang, Sushila Maharjan, Hyeon-Jeong Kim, Ah Young Lee, Sanghwa Kim, Nomundelger Gankhuyag, Myeon-Sik Yang, Yun-Jaie Choi, Myung-Haing Cho, Chong-Su Cho
Despite advances in technology, neither conventional anti-cancer drugs nor current nanoparticle (NP) drugs have gained substantial success in cancer treatment. While conventional chemotherapy drugs have several limitations such as low potency, poor in vivo stability and limited bioavailability, non-specific targeting of NP drugs diminishes their potency at actual target sites. In addition, the development of drug resistance to anti-cancer drugs is another challenging problem. To overcome these limitations, we aimed to develop a polymer-drug conjugate, which functions as an active NP drug and drug carrier both, to deliver a chemotherapeutic drug for combination therapy...
November 24, 2016: Biomaterials
https://www.readbyqxmd.com/read/27914972/experience-of-primary-care-services-among-early-adolescents-in-england-and-association-with-health-outcomes
#5
Arrash A Yassaee, Dougal S Hargreaves, Kayleigh Chester, Stephanie Lamb, Ann Hagell, Fiona M Brooks
PURPOSE: The aim of this study was to investigate adolescents' (11-15 years) experience of their general practitioner (GP), whether poor reported GP experience was associated with worse physical and mental health measures and whether poor previous GP experience was linked to lower utilization of these services. METHODS: We used logistic regression to analyze data from the 2014 Health Behaviour in School-aged Children study. Four aspects of recent care experience were studied: feeling at ease, feeling treated with respect, satisfaction with doctor's explanation, and feeling able to discuss personal matters...
December 1, 2016: Journal of Adolescent Health: Official Publication of the Society for Adolescent Medicine
https://www.readbyqxmd.com/read/27914909/benefits-pitfalls-and-risks-of-phytotherapy-in-clinical-practice-in-otorhinolaryngology
#6
O Laccourreye, A Werner, L Laccourreye, P Bonfils
OBJECTIVES: To elucidate the benefits, pitfalls and risks of phytotherapy in the clinical practice of otorhinolaryngology. MATERIAL AND METHODS: The PubMed and Cochrane databases were searched using the following keywords: phytotherapy, phytomedicine, herbs, otology, rhinology, laryngology, otitis, rhinitis, laryngitis and otorhinolaryngology. Seventy-two articles (18 prospective randomized studies, 4 Cochrane analyses, 4 meta-analysis and 15 reviews of the literature) devoted to clinical studies were analyzed...
November 30, 2016: European Annals of Otorhinolaryngology, Head and Neck Diseases
https://www.readbyqxmd.com/read/27914812/protective-effects-of-gomisin-n-against-hepatic-steatosis-through-ampk-activation
#7
Ye-Rang Yun, Ji-Hyun Kim, Ji Ha Kim, Myeong Ho Jung
Gomisin N (GN) is a phytochemical derived from Schisandra chinensis. It has been reported to exert a protective effect against hepatic steatosis by attenuating endoplasmic recticulum (ER) stress. However, the detailed mechanism by which GN inhibits hepatic steatosis remains to be elucidated. In this study, we examined whether GN activates AMP-activated protein kinase (AMPK) and exerts therapeutic effects on liver X receptor (LXR)- or palmitic acid (PA)-induced triglyceride (TG) accumulation in HepG2 cells. Furthermore, in vivo protective effects of GN against hepatic steatosis were assessed in high-fat diet (HFD)-induced obese mice...
November 30, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27914743/sequential-immunization-with-consensus-influenza-hemagglutinins-raises-cross-reactive-neutralizing-antibodies-against-various-heterologous-ha-strains
#8
Hui Zhou, Yang Huang, Songhua Yuan, Yuanyuan Li, Shuyan Wu, Jianqing Xu, Rui Huang
Seasonal and emerging epidemics caused by influenza virus remain as a public health concern and an economic burden. The weak immunogenicity of conserved epitopes on hemagglutinin that induces broad protective immune responses is the main obstacle to the development of universal vaccines. In the present report, we designed the cross-subtypic sequential vaccination strategy and evaluated its neutralizing antibody (nAb) activity by pseudovirus-based neutralization assays. The results clearly indicated that compared with traditional vaccines strategy, the cross-subtypic sequential immunization could significantly induce a broad serum cross-reactive nAb response in mice as well as against homologous strains, and provide protection from heterologous virus PR8 (H1N1) challenge...
November 30, 2016: Vaccine
https://www.readbyqxmd.com/read/27914742/influenza-virus-specific-antibody-dependent-cellular-cytoxicity-induced-by-vaccination-or-natural-infection
#9
Rory D de Vries, Nella J Nieuwkoop, Mark Pronk, Erwin de Bruin, Geert Leroux-Roels, Elisabeth G W Huijskens, Rob S van Binnendijk, Florian Krammer, Marion P G Koopmans, Guus F Rimmelzwaan
Influenza viruses are responsible for substantial morbidity and mortality during seasonal epidemics. Vaccination is the most effective method to prevent infection, however due to antigenic drift of the viral surface protein hemagglutinin (HA), annual influenza virus vaccination is required. In addition to seasonal viruses, certain (avian) influenza A viruses of other subtypes, like H5N1 or H7N9, cause sporadic zoonotic infections. Therefore, the availability of game-changing novel vaccines that induce "universal" immune responses to a wide variety of influenza A virus subtypes is highly desirable...
November 30, 2016: Vaccine
https://www.readbyqxmd.com/read/27914712/a-6-year-old-presenting-with-headache-and-post-auricular-pain
#10
Naomi Will, Matthew T Whitehead, Holly J Meany, Brian K Reilly
No abstract text is available yet for this article.
November 25, 2016: American Journal of Otolaryngology
https://www.readbyqxmd.com/read/27914592/hyperuricemia-in-systemic-lupus-erythematosus-is-it-associated-with-the-neuropsychiatric-manifestations-of-the-disease
#11
Mahdi Sheikh, Shafieh Movassaghi, Mohammad Khaledi, Maryam Moghaddassi
OBJECTIVES: To assess the association between hyperuricemia and different neuropsychiatric manifestations and stroke risk factors in systematic lupus erythematosus (SLE) patients. METHODS: This study was conducted on 204 SLE patients who were admitted to a tertiary referral center. A standardized questionnaire was completed for all the participants and the medical records were reviewed regarding the occurrence of arterial or venous thrombotic events, stroke, seizure, depression, headache, psychosis, and peripheral neuropathy...
November 2016: Revista Brasileira de Reumatologia
https://www.readbyqxmd.com/read/27914541/two-new-fatty-acids-esters-were-detected-in-ginseng-stems-by-the-application-of-azoxystrobin-and-the-increasing-of-antioxidant-enzyme-activity-and-ginsenosides-content
#12
Shuang Liang, Xuan-Wei Xu, Xiao-Feng Zhao, Zhi-Guang Hou, Xin-Hong Wang, Zhong-Bin Lu
Panax ginseng C.A. Meyer is a valuable herb in China that has also gained popularity in the West because of its pharmacological properties. The constituents isolated and characterized in ginseng stems include ginsenosides, fatty acids, amino acids, volatile oils, and polysaccharides. In this study, the effects of fungicide azoxystrobin applied on antioxidant enzyme activity and ginsenosides content in ginseng stems was studied by using Panax ginseng C. A. Mey. cv. (the cultivar of Ermaya) under natural environmental conditions...
November 2016: Pesticide Biochemistry and Physiology
https://www.readbyqxmd.com/read/27914235/hyaluronan-as-a-promising-excipient-for-ocular-drug-delivery
#13
REVIEW
Michaela Guter, Miriam Breunig
Hyaluronan (HA) is a naturally occurring polysaccharide and well known for its exceptional properties such as high biocompatibility and biodegradability, along with a low immunogenicity. Besides its use for various biomedical applications it recently came into focus as a favorable excipient for the formulation of various ocular therapeutics. This review article summarizes the ocular distribution of HA and its most heavily investigated binding protein "cluster of differentiation 44" (CD44) which is the rationale for the clinical use of HA, primarily as an additive in ocular applications ranging from eye drops to contact lenses...
November 30, 2016: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/27914146/pregnancy-and-delivery-in-a-generalized-dystonia-patient-treated-with-internal-globus-pallidal-deep-brain-stimulation-a-case-report
#14
Hye Ran Park, Jae Meen Lee, Hyeyoung Park, Chae Won Shin, Han Joon Kim, Hee Pyoung Park, Dong Gyu Kim, Beom Seok Jeon, Sun Ha Paek
Internal globus pallidus (GPi) deep brain stimulation (DBS) has been widely accepted as an effective treatment modality of medically refractory dystonia. However, there have been few studies regarding the safety issue of pregnancy and childbirth related with DBS. This report describes a female patient who was pregnant and delivered a baby after GPi DBS surgery. A 33-year-old female patient with acquired generalized dystonia underwent bilateral GPi DBS implantation. She obtained considerable improvement in both movement and disability after DBS implantation...
January 2017: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/27914145/differential-cell-count-and-crp-level-in-blood-as-predictors-for-middle-east-respiratory-syndrome-coronavirus-infection-in-acute-febrile-patients-during-nosocomial-outbreak
#15
Ga Eun Park, Cheol In Kang, Jae Hoon Ko, Sun Young Cho, Young Eun Ha, Yae Jean Kim, Kyong Ran Peck, Jae Hoon Song, Doo Ryeon Chung
A case-control study was performed to identify clinical predictors for Middle East respiratory syndrome coronavirus (MERS-CoV) infection among patients with acute febrile illness during the nosocomial outbreak. Patients with MERS-CoV were more likely to have monocytosis with normal white blood cell (WBC) count and lower C-reactive protein (CRP) level. Simple laboratory data such as complete blood counts (CBC) with differential count could be a useful marker for the prediction of MERS and triage at the initial presentation of acute febrile patients in outbreak setting...
January 2017: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/27914144/outdoor-air-pollution-and-pterygium-in-korea
#16
Ki Woong Lee, Yoon Hyeong Choi, Sung Ha Hwang, Hae Jung Paik, Mee Kum Kim, Won Ryang Wee, Dong Hyun Kim
We investigated relationships between outdoor air pollution and pterygium in Korean adults. This study includes 23,276 adults in population-based cross-sectional data using the Korea National Health and Nutrition Examination Survey 2008-2011. Pterygium was assessed using slit lamp biomicroscopy. Air pollution data (humidity, particulate matter with aerodynamic diameter less than 10 μm [PM₁₀], ozone [O₃], nitrogen dioxide [NO₂], and sulfur dioxide levels [SO₂]) for 2 years preceding the ocular examinations were acquired...
January 2017: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/27914138/therapeutic-response-for-functional-abdominal-pain-in-children-with-occult-constipation-laxatives-versus-prokinetic-drugs
#17
Eun Kyo Ha, Homin Jang, Su Jin Jeong
The relationship between functional abdominal pain (FAP) and occult constipation (OC) in children who did not meet the Rome III criteria for constipation has rarely been reported. This study aimed to estimate the prevalence of OC in patients with FAP and to compare the effectiveness of prokinetic drugs and laxatives for FAP and OC. Pediatric outpatients (n = 212; aged 4-15 years) who satisfied the Rome III criteria for childhood FAP were divided into 2 groups based on Leech scores: group 1 < 8; group 2 ≥ 8...
January 2017: Journal of Korean Medical Science
https://www.readbyqxmd.com/read/27914093/lsmo-nanoparticles-coated-by-hyaluronic-acid-for-magnetic-hyperthermia
#18
Yuanwei Chen, Ying Wang, Xi Liu, Mai Lu, Jiangwei Cao, Tao Wang
Magnetic hyperthermia with the treating temperature range of 41-46 °C is an alternative therapy for cancer treatment. In this article, lanthanum strontium manganates (La1-x Sr x MnO3, 0.25 ≤ × ≤ 0.35) magnetic nanoparticles coated by hyaluronic acid (HA) which possesses the ability of targeting tumor cells were prepared by a simple hydrothermal method combined with a high-energy ball milling technique. The crystal structure, morphology, magnetic properties of the HA-coated magnetic nanoparticles (MNPs), and their heating ability under alternating magnetic field were investigated...
December 2016: Nanoscale Research Letters
https://www.readbyqxmd.com/read/27913910/a-randomized-trial-of-displaying-paid-price-information-on-imaging-study-and-procedure-ordering-rates
#19
Alyna T Chien, Lisa Soleymani Lehmann, Laura A Hatfield, Kate E Koplan, Carter R Petty, Anna D Sinaiko, Meredith B Rosenthal, Thomas D Sequist
BACKGROUND: Prior studies have demonstrated how price transparency lowers the test-ordering rates of trainees in hospitals, and physician-targeted price transparency efforts have been viewed as a promising cost-controlling strategy. OBJECTIVE: To examine the effect of displaying paid-price information on test-ordering rates for common imaging studies and procedures within an accountable care organization (ACO). DESIGN: Block randomized controlled trial for 1 year...
December 2, 2016: Journal of General Internal Medicine
https://www.readbyqxmd.com/read/27913871/n2o-emission-characteristics-and-its-affecting-factors-in-rain-fed-potato-fields-in-wuchuan-county-china
#20
Liwei Wang, Cheng Wang, Zhihua Pan, Hui Xu, Lin Gao, Peiyi Zhao, Zhiqiang Dong, Jingting Zhang, Guohui Cui, Sen Wang, Guolin Han, Hui Zhao
Representing an important greenhouse gas, nitrous oxide (N2O) emission from cultivated land is a hot topic in current climate change research. This study examined the influences of nitrogen fertilisation, temperature and soil moisture on the ammonia monooxygenase subunit A (amoA) gene copy numbers and N2O emission characteristics. The experimental observation of N2O fluxes was based on the static chamber-gas chromatographic method. The ammonia-oxidising bacteria (AOB) and ammonia-oxidising archaea (AOA) gene copy numbers in different periods were measured by real-time polymerase chain reaction (PCR)...
December 3, 2016: International Journal of Biometeorology
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