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https://www.readbyqxmd.com/read/28749424/drug-discovery-by-molecular-imaging-and-monitoring-therapy-response-in-lymphoma
#1
REVIEW
Senthilkumar Kalimuthu, Ju Hye Jeong, Ji Min Oh, Byeong-Cheol Ahn
Molecular imaging allows a noninvasive assessment of biochemical and biological processes in living subjects. Treatment strategies for malignant lymphoma depend on histology and tumor stage. For the last two decades, molecular imaging has been the mainstay diagnostic test for the staging of malignant lymphoma and the assessment of response to treatment. This technology enhances our understanding of disease and drug activity during preclinical and clinical drug development. Here, we review molecular imaging applications in drug development, with an emphasis on oncology...
July 27, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/28749411/advances-in-testing-techniques-for-digital-microfluidic-biochips
#2
REVIEW
Vineeta Shukla, Fawnizu Azmadi Hussin, Nor Hisham Hamid, Noohul Basheer Zain Ali
With the advancement of digital microfluidics technology, applications such as on-chip DNA analysis, point of care diagnosis and automated drug discovery are common nowadays. The use of Digital Microfluidics Biochips (DMFBs) in disease assessment and recognition of target molecules had become popular during the past few years. The reliability of these DMFBs is crucial when they are used in various medical applications. Errors found in these biochips are mainly due to the defects developed during droplet manipulation, chip degradation and inaccuracies in the bio-assay experiments...
July 27, 2017: Sensors
https://www.readbyqxmd.com/read/28749393/adverse-effects-drug-load-of-antiepileptic-drugs-in-patients-with-epilepsy-monotherapy-versus-polytherapy
#3
Rupa Joshi, Manjari Tripathi, Pooja Gupta, Sheffali Gulati, Yogendra Kumar Gupta
BACKGROUND & OBJECTIVES: Although the need for a combination of antiepileptic drugs (AEDs) in the treatment of epilepsy is well justified, but an associated increase in adverse effects (AEs) lends a restriction to polytherapy. The aim of this study was to evaluate AEs and drug load (prescribed daily dose/defined daily doses) of AEDs in patients with epilepsy (PWE). METHODS: Consecutive PWEs attending Epilepsy clinic in a tertiary care hospital in New Delhi, India, were enrolled in the study...
March 2017: Indian Journal of Medical Research
https://www.readbyqxmd.com/read/28749251/identification-of-spirocyclic-or-phosphate-substituted-quinolizine-derivatives-as-novel-hiv-1-integrase-inhibitors-a-patent-evaluation-of-wo2016094197a1-wo2016094198a1-and-wo2016154527a1
#4
Xiqiang Cheng, Ping Gao, Lin Sun, Ye Tian, Peng Zhan, Xinyong Liu
Highly active antiretroviral therapy (HAART) has been widely adopted to control the HIV-1 infection successfully. HIV-1 integrase (IN) inhibitors are primary drugs in HAART regimens targeting integration step in the HIV-1 life cycle. However, due to the emergence of viral resistance and cross-resistance amongst drugs, there is a pressing need for new and potent IN inhibitors. This review covers the three patents describing spirocyclic and phosphate substituted quinolizine derivatives as novel HIV-1 IN inhibitors for the discovery of new anti-HIV-1 drug candidates...
July 27, 2017: Expert Opinion on Therapeutic Patents
https://www.readbyqxmd.com/read/28749102/an-exploration-of-phytochemicals-from-simaroubaceae
#5
Biba Vikas, B S Akhil, P S R Suja, K Sujathan
Natural products such as plants, animals and minerals have been the basis of treatment of human diseases. Herbal remedies have been used for the treatment of many ailments. Many compounds have been derived from the plant species mentioned in the ancient texts of Indian system of medicine for the treatment of a number of ailments. The R and D thrust in the pharmaceutical sector is focused on development of new drugs, innovative/indigenous processes for known drugs and development of plant based drugs through investigation of leads from the traditional systems of medicine...
July 27, 2017: Asian Pacific Journal of Cancer Prevention: APJCP
https://www.readbyqxmd.com/read/28748912/a-novel-allosteric-site-in-casein-kinase-2%C3%AE-discovered-using-combining-bioinformatics-and-biochemistry-methods
#6
Hai-Ming Jiang, Jiang-Kai Dong, Kun Song, Tong-Dan Wang, Wen-Kang Huang, Jing-Miao Zhang, Xiu-Yan Yang, Ying Shen, Jian Zhang
Casein kinase 2 (CK2) is a highly pleiotropic serine-threonine kinase, which catalyzed phosphorylation of more than 300 proteins that are implicated in regulation of many cellular functions, such as signal transduction, transcriptional control, apoptosis and the cell cycle. On the other hand, CK2 is abnormally elevated in a variety of tumors, and is considered as a promising therapeutic target. The currently available ATP-competitive CK2 inhibitors, however, lack selectivity, which has impeded their development in cancer therapy...
July 27, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28748781/a-versatile-liquid-chromatographic-method-for-the-simultaneous-determination-of-metformin-sitagliptin-simvastatin-and-ezetimibe-in-different-dosage-forms
#7
Asmaa A El-Zaher, Ehab F Elkady, Hanan M Elwy, Mahmoud Abo El Makarim Saleh
A new LC method is introduced with the concept of its versatile application to widely used drugs from different pharmacological classes. Metformin hydrochloride (MTF), sitagliptin phosphate (SIT), simvastatin (SIM) and ezetimibe (EZB) were simultaneously determined with a simple reversed-phase LC method in which a SIT–SIM binary mixture, present in a dosage form brand, was considered central for its development. Chromatographic separation was achieved with a mobile phase of acetonitrile and 0.02 M potassium dihydrogen phosphate (pH 5...
July 27, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/28748755/biotin-and-glutathione-targeting-of-solid-nanoparticles-to-cross-human-brain-endothelial-cells
#8
Szilvia Veszelka, Mária Mészáros, Lóránd Kiss, Zoltán Kóta, Tibor Páli, Zsófia Hoyk, Zsolt Bozsó, Lívia Fülöp, András Tóth, Gábor Rákhely, Mária A Deli
Background The blood-brain barrier restricts drug penetration to the central nervous system. Targeted nanocarriers are new potential tools to increase the brain entry of drugs. Ligands of endogenous transporters of the blood-brain barrier can be used as targeting vectors for brain delivery of nanoparticles. Objective We tested biotin-labeled solid nanoparticles for the first time and compared to biotinylated glutathione-labeled nanoparticles in brain endothelial cells. Method Neutravidin coated fluorescent polystyrene nanoparticles were derivatized with biotin and biotinylated glutathione...
July 27, 2017: Current Pharmaceutical Design
https://www.readbyqxmd.com/read/28748726/natural-products-for-human-health-an-historical-overview-of-the-drug-discovery-approaches
#9
S Bernardini, A Tiezzi, V Laghezza Masci, E Ovidi
Natural products (NPs) are secondary metabolites produced and used by organisms for defending or adapting purposes. These molecules were naturally selected during thousands of years to improve the specificity and cover a very wide range of functions, depending on the origin, the habitat and the specific activity carried out in the organism of origin. Due to these intrinsic features, NPs have been used as healing agents since thousands of years and still today continue to be the most important source of new potential therapeutic preparations...
July 27, 2017: Natural Product Research
https://www.readbyqxmd.com/read/28748555/digitalis-use-and-lung-cancer-risk-by-histological-type-in-men
#10
Wentao Li, Shao-Hua Xie, Lap-Ah Tse, Jesper Lagergren
Lung cancer risk and tumor characteristics differ between sexes. Estrogen has been suggested to counteract lung cancer development. We aimed to test the hypothesis that digitalis use decreases lung cancer risk due to its estrogenic and other anticancer properties in men. This was a nationwide Swedish population-based cohort study between July 1, 2005 and December 31, 2013. Data on the use of digitalis and organic nitrates in all male individuals were derived from the Swedish Prescribed Drug Registry. New lung cancer diagnoses among cohort participants were identified from the Swedish Cancer Registry...
July 27, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28748397/activity-of-the-novel-siderophore-cephalosporin-cefiderocol-against-multidrug-resistant-gram-negative-pathogens
#11
J Dobias, V Dénervaud-Tendon, L Poirel, P Nordmann
The novel siderophore cephalosporin cefiderocol (S-649266) with potent activity against Gram-negative pathogens was recently developed (Shionogi & Co., Ltd.). Here, we evaluated the activity of this new molecule and comparators against a collection of previously characterized Gram-negative isolates using broth microdilution panels. A total of 753 clinical multidrug-resistant Gram-negative isolates collected from hospitals worldwide were tested against cefiderocol and antibiotic comparators (ceftolozane-tazobactam [CT], meropenem [MEM], ceftazidime [CAZ], ceftazidime-avibactam [CZA], colistin [CST], aztreonam [ATM], amikacin [AMK], ciprofloxacin [CIP], cefepime [FEP], and tigecycline [TGC]) for their susceptibility...
July 26, 2017: European Journal of Clinical Microbiology & Infectious Diseases
https://www.readbyqxmd.com/read/28748194/recurrent-metatarsal-fractures-in-postmenopausal-woman-with-low-serum-alkaline-phosphatase-a-rare-diagnosis-not-to-miss
#12
Umair Iqbal, Hafsa Anwar, Ahmad Chaudhary, Madiha Alvi, Amy Freeth
Hypophosphatasia (HPP) is a rare inborn error of metabolism due to a loss-of-function mutation in the gene for tissue nonspecific isoenzyme of alkaline phosphatase (ALP) that results in low levels of ALP. The clinical presentation of HPP is variable and in adults can easily be misdiagnosed as other forms of osteomalacia. We present a case of a 53-year-old Caucasian female who was evaluated for recurrent metatarsal fractures. She reported her first metatarsal fracture at age 21, and since then had at least 8 more metatarsal fractures over her lifetime, most without injury other than weight bearing...
July 2017: Journal of Investigative Medicine High Impact Case Reports
https://www.readbyqxmd.com/read/28748116/gout-an-old-disease-in-new-perspective-a-review
#13
REVIEW
Gaafar Ragab, Mohsen Elshahaly, Thomas Bardin
Gout is a picturesque presentation of uric acid disturbance. It is the most well understood and described type of arthritis. Its epidemiology is studied. New insights into the pathophysiology of hyperuricemia and gouty arthritis; acute and chronic allow for an even better understanding of the disease. The role of genetic predisposition is becoming more evident. The clinical picture of gout is divided into asymptomatic hyperuricemia, acute gouty arthritis, intercritical period, and chronic tophaceous gout. Diagnosis is based on laboratory and radiological features...
September 2017: Journal of Advanced Research
https://www.readbyqxmd.com/read/28747977/use-of-c57bl-6n-mice-on-the-variety-of-immunological-researches
#14
REVIEW
Hyun Keun Song, Dae Youn Hwang
Inbred mice are an essential animal strain for research as they can improve the reproducibility and reliability of study results. The establishment of new inbred lines is continuing, and new inbred lines are being used in many research fields. C57BL/6 is a mouse laboratory animal that has been developed and used as an inbred strain since early stage of mouse strain development, and, in the 1950s, C57BL/6 was separated into substrains by the Jackson Laboratory (C57BL/6J) and the National Institutes of Health (C57BL/6N)...
June 2017: Laboratory Animal Research
https://www.readbyqxmd.com/read/28747773/deciphering-mechanisms-of-acquired-t790m-mutation-after-egfr-inhibitors-for-nsclc-by-computational-simulations
#15
Bin Zou, Victor H F Lee, Lijiang Chen, Lichun Ma, Debby D Wang, Hong Yan
Metastatic non-small-cell lung cancer (NSCLC) with activating EGFR mutations responds very well to first and second generation tyrosine-kinase inhibitors (TKI) including gefitinib, erlotinib and afatinib. Unfortunately, drug resistance will eventually develop and about half of the cases are secondary to the emergence of acquired T790M somatic mutation. In this work, we prospectively recruited 68 patients with metastatic EGFR-mutated NSCLC who have developed progressive disease after first-line TKI with or without subsequent TKI and/or other systemic therapy...
July 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28747725/echinomycin-inhibits-adipogenesis-in-3t3-l1-cells-in-a-hif-independent-manner
#16
Junna Yamaguchi, Tetsuhiro Tanaka, Hisako Saito, Seitaro Nomura, Hiroyuki Aburatani, Hironori Waki, Takashi Kadowaki, Masaomi Nangaku
Obesity is a risk factor for many diseases including diabetes, cancer, cardiovascular disease, and chronic kidney disease. Obesity is characterized by the expansion of white adipose tissue (WAT). Hypertrophy and hyperplasia of adipocytes cause tissue hypoxia followed by inflammation and fibrosis. Its trigger, preadipocyte differentiation into mature adipocytes, is finely regulated by transcription factors, signal molecules, and cofactors. We found that echinomycin, a potent HIF-1 inhibitor, completely inhibited adipogenesis in 3T3-L1 WAT preadipocytes by affecting the early phase of mitotic clonal expansion...
July 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28747710/a-high-content-image-analysis-approach-for-quantitative-measurements-of-chemosensitivity-in-patient-derived-tumor-microtissues
#17
Ilmari Ahonen, Malin Åkerfelt, Mervi Toriseva, Eva Oswald, Julia Schüler, Matthias Nees
Organotypic, three-dimensional (3D) cancer models have enabled investigations of complex microtissues in increasingly realistic conditions. However, a drawback of these advanced models remains the poor biological relevance of cancer cell lines, while higher clinical significance would be obtainable with patient-derived cell cultures. Here, we describe the generation and data analysis of 3D microtissue models from patient-derived xenografts (PDX) of non-small cell lung carcinoma (NSCLC). Standard of care anti-cancer drugs were applied and the altered multicellular morphologies were captured by confocal microscopy, followed by automated image analyses to quantitatively measure phenotypic features for high-content chemosensitivity tests...
July 26, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28747360/cannabinoids-and-the-kidney-effects-in-health-and-disease
#18
Frank Park, Praveen K Potukuchi, Hamid Moradi, Csaba P Kovesdy
Consumption of cannabis and various related products (cannabinoids) for both medicinal and recreational use is gaining popularity. Furthermore, regulatory changes are fostering a cultural shift towards increasing liberalization of cannabis use, thereby increasing the likelihood of even larger numbers of individuals being exposed in the future. The two different types of receptors (CB1 and CB2) that are activated by the pharmacologically active ingredients of cannabis are found in numerous tissues, including the kidneys...
July 26, 2017: American Journal of Physiology. Renal Physiology
https://www.readbyqxmd.com/read/28747120/a-perspective-on-the-contribution-of-animal-models-to-the-pharmacological-treatment-of-posttraumatic-stress-disorder
#19
Valerie Bertaina-Anglade, Susan M O'Connor, Emile Andriambeloson
OBJECTIVES: Posttraumatic stress disorder (PTSD) is a prevalent, chronic, disabling disorder that may develop following exposure to a traumatic event. This review summarizes currently used animal models of PTSD and their potential role in the development of better therapeutics. Heterogeneity is one of the main characteristics of PTSD with the consequence that many pharmacological approaches are used to relieve symptoms of PTSD. To address the translational properties of the animal models, we discuss the types of stressors used, the rodent correlates of human PTSD (DSM-5) symptoms, and the efficacy of approved, recommended and off-label drugs used to treat PTSD in 'PTSD-animals'...
August 2017: Australasian Psychiatry: Bulletin of Royal Australian and New Zealand College of Psychiatrists
https://www.readbyqxmd.com/read/28747103/a-deliberative-framework-to-identify-the-need-for-real-life-evidence-building-of-new-cancer-drugs-after-interim-funding-decision
#20
Leanne Leung, Mário L de Lemos, Laurel Kovacic
Background With the rising cost of new oncology treatments, it is no longer sustainable to base initial drug funding decisions primarily on prospective clinical trials as their performance in real-life populations are often difficult to determine. In British Columbia, an approach in evidence building is to retrospectively analyse patient outcomes using observational research on an ad hoc basis. Methods The deliberative framework was constructed in three stages: framework design, framework validation and treatment programme characterization, and key informant interview...
January 1, 2017: Journal of Oncology Pharmacy Practice
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