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https://www.readbyqxmd.com/read/28092860/design-synthesis-and-biological-evaluation-of-quinazoline-phosphoramidate-mustard-conjugates-as-anticancer-drugs
#1
Songwen Lin, Yingbo Li, Yufen Zheng, Laichun Luo, Qi Sun, Zemei Ge, Tieming Cheng, Runtao Li
A series of novel compounds with phosphoramide mustard functionality incorporated into the quinazoline scaffold of EGFR/HER2 inhibitors were designed and synthesized as multi-target-directed ligands against tumor cells. In vitro assays showed that tumor cell lines with high HER2 level were more sensitive to the compounds than tumor cells with low HER2 level. Compound 10d (EMB-3) was one of the most potent inhibitors with IC50 of 7.4 nM and 82 nM against EGFR and HER2, respectively. The mechanism studies were also supported by the effect of 10d-induced DNA damage in MDA-MB-468 cells...
January 3, 2017: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28092841/phytochemical-study-and-protective-effect-of-trigonella-foenum-graecum-fenugreek-seeds-against-carbon-tetrachloride-induced-toxicity-in-liver-and-kidney-of-male-rat
#2
Sakhria Mbarki, Hichem Alimi, Hafsia Bouzenna, Abdelfettah Elfeki, Najla Hfaiedh
Liver and kidney diseases are a global concern, therefore considerable efforts to obtain fine herbs useful as drugs from medicinal plants are currently in progress. The aim of this work was to study the antioxidant effects of previous supplementation with fenugreek seeds (FS) against carbon tetrachloride (CCl4) toxicity in the liver and kidney. CCl4 toxicity was induced by one dose (i.g. 5ml CCl4/kg of body weight, 50% CCl4 in olive oil) after 7 weeks of normal diet or diet rich in 10% of grinded fenugreek seeds (20g of pellet rat food/rat/day)...
January 13, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28092772/the-expression-of-endothelin-1-in-chronic-lymphocytic-leukemia-is-controlled-by-epigenetic-mechanisms-and-extracellular-stimuli
#3
Silvia Martinelli, Rossana Maffei, Stefania Fiorcari, Chiara Quadrelli, Patrizia Zucchini, Stefania Benatti, Leonardo Potenza, Mario Luppi, Roberto Marasca
Endothelin-1 (ET-1) is a hormone peptide widely expressed and is involved in several biological processes, important not only for normal cell function but also for tumor development, including cell proliferation, invasion, metastasis, angiogenesis and osteogenesis. In accordance, ET-1 was already shown to contribute to the growth and progression of many different solid cancers. We recently demonstrated that ET-1 has a role in the pathogenesis of chronic lymphocytic leukemia (CLL) where it is abnormally expressed...
December 30, 2016: Leukemia Research
https://www.readbyqxmd.com/read/28092694/proton-pump-inhibitors-risks-of-long-term-use
#4
REVIEW
Leonardo Henry Eusebi, Stefano Rabitti, Maria Laura Artesiani, Dania Gelli, Marco Montagnani, Rocco Maurizio Zagari, Franco Bazzoli
Proton pump inhibitors are among the most commonly prescribed classes of drugs and their use is increasing, in particular for long term treatment, often being over-prescribed and used for inappropriate conditions. In recent years, considerable attention has been directed towards a wide range of adverse effects, and even when a potential underlying biological mechanism is plausible, the clinical evidence of the adverse effect is often weak. Several long term side effects have been investigated ranging from interaction with other drugs, increased risk of infection, reduced intestinal absorption of vitamins and minerals, and more recently kidney damage and dementia...
January 16, 2017: Journal of Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28092388/exploration-and-analysis-of-drug-modes-of-action-through-feature-integration
#5
Mingyuan Xin, Jun Fan, Mingyao Liu, Zhenran Jiang
Identifying drug modes of action (MoA) is of paramount importance for having a good grasp of drug indications in clinical tests. Anticipating MoA can help to discover new uses for approved drugs. Here we first used a drug-set enrichment analysis method to discover significant biological activities in every mode of action category. Then, we proposed a new computational model, a probability ensemble approach based on Bayesian network theory, which integrated chemical, therapeutic, genomic and phenotypic properties of over a thousand of FDA approved drugs to assist with the prediction of MoA...
January 16, 2017: Molecular BioSystems
https://www.readbyqxmd.com/read/28091916/new-experimental-model-of-rat-risk-behavior-effects-of-nicotine-and-phenazepam
#6
S K Sudakov, G A Nazarova, E V Alekseeva
We described a new model of risk behavior in rats that allows selection of animals predisposed to risk behavior in the absence of other biological motivations. Phenazepam administration did not change the intensity of risk behavior in "risky" animals, but stimulated risk behavior in rats that were not predisposed to it. Nicotine inhibited risk behavior in "risky" animals and strengthened it in "cautious" rats. In the intermediate group, the drugs did not induce significant changes. A similar effect of the drugs was observed in the previous models...
January 14, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28091567/quantifying-the-relative-contributions-of-different-solute-carriers-to-aggregate-substrate-transport
#7
Mehdi Taslimifar, Lalita Oparija, Francois Verrey, Vartan Kurtcuoglu, Ufuk Olgac, Victoria Makrides
Determining the contributions of different transporter species to overall cellular transport is fundamental for understanding the physiological regulation of solutes. We calculated the relative activities of Solute Carrier (SLC) transporters using the Michaelis-Menten equation and global fitting to estimate the normalized maximum transport rate for each transporter (Vmax). Data input were the normalized measured uptake of the essential neutral amino acid (AA) L-leucine (Leu) from concentration-dependence assays performed using Xenopus laevis oocytes...
January 16, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28090657/toward-greater-insights-on-pharmacokinetics-and-exposure-response-relationships-for-therapeutic-biologics-in-oncology-drug-development
#8
Yaning Wang, Brian Booth, Atiqur Rahman, Geoffrey Kim, Shiew Mei Huang, Issam Zineh
There has been increased interest in optimizing dosing regimens for oncology products over the past decade. Investigations to refine dosing regimens often occur after new drug approval.(1) There is growing focus on the use of exposure-response (ER) approaches to identify optimal dosing regimens for therapeutic biologics. Herein, we describe several recent observations that have informed our thinking on the use of ER analyses in the dose regimen optimization of therapeutic biologics developed to treat cancer...
January 16, 2017: Clinical Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/28090647/the-multifaceted-role-of-extracellular-vesicles-in-metastasis-priming-the-soil-for-seeding
#9
REVIEW
Brunna Dos Anjos Pultz, Felipe Andrés Cordero da Luz, Sara Socorro Faria, Leandro Peixoto Ferreira de Souza, Paula Cristina Brígido Tavares, Vivian Alonso Goulart, Wagner Fontes, Luiz Ricardo Goulart, Marcelo José Barbosa Silva
Extracellular vesicles (EVs), including exosomes, play a key role in inter and intracellular communication, promoting the proliferation and invasion of recipient cells to support tumor growth and metastasis. Metastasis comprises multiple steps that first include the detachment of tumor cells through epithelial to mesenchymal transition (EMT), allowing the physical dissemination to distant organs. Thereafter, cancer-derived exosomes are still critical components for preparing the tumor microenvironment by (i) enabling tumor cells to escape from the immunological surveillance and (ii) arranging the pre-metastatic site for the engraftment of detached cancer cells...
January 16, 2017: International Journal of Cancer. Journal International du Cancer
https://www.readbyqxmd.com/read/28089965/increasing-patient-safety-by-closing-the-sterile-production-gap-part-2-implementation
#10
James Agalloco
Terminal sterilization is considered the preferred means for the production of sterile drug products as it affords enhanced safety for the patient as the formulation is filled into its final container, sealed and sterilized. Despite the obvious patient benefits, the use of terminal sterilization is artificially constrained by unreasonable expectations for the minimum time-temperature process to be used. The core misunderstanding with terminal sterilization is a fixation that destruction of a high population of a resistant biological indicator is required...
January 15, 2017: PDA Journal of Pharmaceutical Science and Technology
https://www.readbyqxmd.com/read/28089964/increasing-patient-safety-by-closing-the-sterile-production-part-1-introduction
#11
James Agalloco
Terminal sterilization is considered the preferred means for the production of sterile drug products as it affords enhanced safety for the patient as the formulation is filled into its final container, sealed and sterilized. Despite the obvious patient benefits, the use of terminal sterilization is artificially constrained by unreasonable expectations for the minimum time-temperature process to be used. The core misunderstanding with terminal sterilization is a fixation that destruction of a high population of a resistant biological indicator is required...
January 15, 2017: PDA Journal of Pharmaceutical Science and Technology
https://www.readbyqxmd.com/read/28089942/targeting-egfr-t790m-mutation-in-nsclc-from-biology-to-evaluation-and-treatment
#12
Antonio Passaro, Elena Guerini-Rocco, Alessia Pochesci, Davide Vacirca, Gianluca Spitaleri, Chiara Matilde Catania, Alessandra Rappa, Massimo Barberis, Filippo de Marinis
The identification of EGFR mutations and their respectively tyrosine kinase inhibitors (TKIs), changed dramatically treatment and survival of patients with EGFR-positive lung cancer. Nowadays, different EGFR TKIs as afatinib, erlotinib and gefitinib are approved worldwide for the treatment of NSCLC harbouring EGFR mutations, in particular exon 19 deletions or exon 21 (Leu858Arg) substitution EGFR mutations. In first-line setting, when comparing with platinum-based chemotherapy, these target drugs improves progression-free survival, response rate and quality of life...
January 12, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28089842/curbing-tumorigenesis-and-malignant-progression-through-the-pharmacological-control-of-the-wound-healing-process
#13
REVIEW
Melania Dovizio, Angela Sacco, Paola Patrignani
The prevention of cancer development and its progression is an urgent unmet medical need. Novel knowledge on the biology of cancer has evidenced that genetic changes occurring within cancer cells contribute, but are not sufficient, for tumor promotion and progression. The results of clinical studies and experimental animal models have suggested pursuing new avenues for the prevention of cancer development in the early stages, by using drugs that modulate platelet responses and those interfering with the synthesis and action of the mediators of inflammation...
January 12, 2017: Vascular Pharmacology
https://www.readbyqxmd.com/read/28089786/3-carboxyphenylboronic-acid-modified-carboxymethyl-chitosan-nanoparticles-for-improved-tumor-targeting-and-inhibitory
#14
Xin Wang, Bing Wei, Xu Cheng, Jun Wang, Rupei Tang
Carboxymethyl chitosan-based nanoparticles (CM NPs) were prepared, and were further modified with a tumor-homing ligand (3-carboxyphenylboronic acid, 3-CPBA) to give tumor-targeting nanoparticles (CB NPs). Particle sizes were measured by dynamic light scattering, while the morphology was observed via transmission electron microscopy and scanning electronic microscope. The results show that CM and CB NPs are spherical-like, and kinetically stable in various conditions. Doxorubicin (DOX) as a model drug was successfully encapsulated to give CM-DOX and CB-DOX NPs...
January 12, 2017: European Journal of Pharmaceutics and Biopharmaceutics
https://www.readbyqxmd.com/read/28089770/structural-pierce-into-molecular-mechanism-underlying-clostridium-perfringens-epsilon-toxin-function
#15
Saeed Khalili, Abolfazl Jahangiri, Zahra Sadat Hashemi, Bahman Khalesi, Meysam Mardsoltani, Jafar Amani
Epsilon toxin of the Clostridium perfringens garnered a lot of attention due to its potential for toxicity in humans, extreme potency for cytotoxicity in mice and lack of any approved therapeutics prescribed for human. However, the intricacies of the Epsilon toxin action mechanism are yet to be understood. In this regard, various in silico tools have been exploited to model and refine the 3D structure of the toxin and its two receptors. The receptor proteins were embedded into designed lipid membranes within an aqueous and ionized environment...
January 12, 2017: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/28089695/the-pharmacology-of-tacrine-at-n-methyl-d-aspartate-receptors
#16
REVIEW
Martin Horak, Kristina Holubova, Eugenie Nepovimova, Jan Krusek, Martina Kaniakova, Jan Korabecny, Ladislav Vyklicky, Kamil Kuca, Ales Stuchlik, Jan Ricny, Karel Vales, Ondrej Soukup
The mechanism of tacrine as a precognitive drug has been considered to be complex and not fully understood. It has been reported to involve a wide spectrum of targets involving cholinergic, gabaergic, nitrinergic and glutamatergic pathways. Here, we review the effect of tacrine and its derivatives on the NMDA receptors (NMDAR) with a focus on the mechanism of action and biological consequences related to the Alzheimer's disease treatment. Our findings indicate that effect of tacrine on glutamatergic neurons is both direct and indirect...
January 13, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28089171/protease-inhibitors-of-parasitic-flukes-emerging-roles-in-parasite-survival-and-immune-defence
#17
REVIEW
Shiwanthi L Ranasinghe, Donald P McManus
Protease inhibitors play crucial roles in parasite development and survival, counteracting the potentially damaging immune responses of their vertebrate hosts. However, limited information is currently available on protease inhibitors from schistosomes and food-borne trematodes. Future characterization of these molecules is important not only to expand knowledge on parasitic fluke biology but also to determine whether they represent novel vaccine and/or drug targets. Moreover, protease inhibitors from flukes may represent lead compounds for the development of a new range of therapeutic agents against inflammatory disorders and cancer...
January 11, 2017: Trends in Parasitology
https://www.readbyqxmd.com/read/28088906/epratuzumab-and-blinatumomab-as-therapeutic-antibodies-for-treatment-of-pediatric-acute-lymphoblastic-leukemia-current-status-and-future-perspectives
#18
Raffaella Franca, Diego Favretto, Marilena Granzotto, Giuliana Decorti, Marco Rabusin, Gabriele Stocco
BACKGROUND: More than 85% of children affected by acute lymphoblastic leukemia (ALL) are successfully treated; however relapse remains a remarkable clinical concern, with 50-60% of relapsing patients facing a fatal outcome. Management of relapsed patients includes standardized intensive risk-adapted regimens based on conventional drugs, and hematopoietic stem cells transplantation for patients with unfavourable features. Biological drugs, in particular the monoclonal antibody epratuzumab and the bi-functional recombinant single chain peptide blinatumomab, have been recently recognized as novel potential agents to be integrated in salvage ALL therapy to further improve rescue outcome...
January 12, 2017: Current Medicinal Chemistry
https://www.readbyqxmd.com/read/28088864/an-integrated-high-throughput-multi-omics-platform-enables-data-driven-construction-of-cellular-responses-and-reveals-global-drug-mechanisms-of-action
#19
Jeremy L Norris, Melissa A Farrow, Danielle B Gutierrez, Lauren D Palmer, Nicole Muszynski, Stacy D Sherrod, James C Pino, Jamie L Allen, Jeffrey M Spraggins, Alex L R Lubbock, Ashley T Jordan, William Burns, James C Poland, Carrie E Romer, M Lisa Manier, Yuan-Wei Nei, Boone M Prentice, Kristie L Rose, Salisha Hill, Raf Van de Plas, Tina Tsui, Nathaniel M Braman, M Ray Keller, Stacey A Rutherford, Nichole A Lobdell, Carlos F Lopez, D Borden Lacy, John A McLean, John Peter Wikswo, Eric P Skaar, Richard M Caprioli
An understanding of how cells respond to perturbation is essential for biological applications; however, most approaches for profiling cellular response are limited in scope to pre-established targets. Global analysis of molecular mechanism will advance our understanding of the complex networks constituting cellular perturbation and lead to advancements in areas, such as infectious disease pathogenesis, developmental biology, pathophysiology, pharmacology, and toxicology. We have developed a high-throughput multi-omics platform for comprehensive, de novo characterization of cellular mechanisms of action...
January 14, 2017: Journal of Proteome Research
https://www.readbyqxmd.com/read/28088690/electrochemical-studies-of-dna-interaction-and-antimicrobial-activities-of-mn-ii-fe-iii-co-ii-and-ni-ii-schiff-base-tetraazamacrocyclic-complexes
#20
Anuj Kumar, Vinod Kumar Vashistha, Prashant Tevatia, Randhir Singh
Tetraazamacrocyclic complexes of Mn(II), Fe(III), Co(II) and Ni(II) have been synthesized by template method. These tetraazamacrocycles have been analyzed with various techniques like molar conductance, IR, UV-vis, mass spectral and cyclic voltammetric studies. On the basis of all these studies, octahedral geometry has been assigned to these tetraazamacrocyclic complexes. The DNA binding properties of these macrocyclic complexes have been investigated by electronic absorption spectra, fluorescence spectra, cyclic voltammetric and differential pulse voltammetric studies...
January 6, 2017: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
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