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https://www.readbyqxmd.com/read/29733878/multi-step-high-throughput-conjugation-platform-for-the-development-of-antibody-drug-conjugates
#1
Sebastian Andris, Michaela Wendeler, Xiangyang Wang, Jürgen Hubbuch
Antibody drug conjugates (ADCs) form a rapidly growing class of biopharmaceuticals which attracts a lot of attention throughout the industry due to its high potential for cancer therapy. They combine the specificity of a monoclonal antibody (mAb) and the cell-killing capacity of highly cytotoxic small molecule drugs. Site-specific conjugation approaches involve a multi-step process for covalent linkage of antibody and drug via a linker. Despite the range of parameters that have to be investigated, high-throughput methods are scarcely used so far in ADC development...
May 4, 2018: Journal of Biotechnology
https://www.readbyqxmd.com/read/29732996/targeting-trypanothione-reductase-of-leishmanial-major-to-fight-against-cutaneous-leishmaniasis
#2
Abdul Aziz A Bin Dukhyil
BACKGROUND: 1.2-2.0 million cases of leishmaniasis occur annually throughout the world. The available drugs like Amphotericin B, antimonials and miltefosine are unable to fulfill the need due less effectiveness, high toxicity, resistance, high cost and complex route of administration. Leishmania survives inside the macrophages through different evasion mechanisms; one of that is activation of its trypanothione reductase enzyme which neutralizes the reactive oxygen species generated inside the macrophages to kill the parasites...
May 2, 2018: Infectious Disorders Drug Targets
https://www.readbyqxmd.com/read/29717260/a-modified-gene-trap-approach-for-improved-high-throughput-cancer-drug-discovery
#3
Shelli M Morris, Andrew J Mhyre, Savanna S Carmack, Carrie H Myers, Connor Burns, Wenjuan Ye, Marc Ferrer, James M Olson, Richard A Klinghoffer
While advances in laboratory automation has dramatically increased throughout of compound screening efforts, development of robust cell-based assays in relevant disease models remain resource-intensive and time-consuming, presenting a bottleneck to drug discovery campaigns. To address this issue, we present a modified gene trap approach to efficiently generate pathway-specific reporters that result in a robust "on" signal when the pathway of interest is inhibited. In this proof-of-concept study, we used vemurafenib and trametinib to identify traps that specifically detect inhibition of the mitogen-activated protein kinase (MAPK) pathway in a model of BRAFV600E driven human malignant melanoma...
May 2, 2018: Oncogene
https://www.readbyqxmd.com/read/29678427/the-psychological-impact-of-adult-traumatic-brachial-plexus-injury
#4
Zoe A Landers, Rishabh Jethanandani, Steve K Lee, Carol A Mancuso, Mavis Seehaus, Scott W Wolfe
PURPOSE: There is a high incidence of posttraumatic stress disorder (PTSD), depression, suicide risk, and psychological distress after orthopedic trauma and hand and upper-extremity injury. Although patients with traumatic adult brachial plexus injury are particularly vulnerable to psychologic distress, minimal clinical data exist about this cohort of patients. In this study, we sought to discover the prevalence of depression, PTSD, suicidal ideation, and substance abuse. METHODS: Between February, 2013 and July, 2014, during scheduled preoperative and/or postoperative appointments, the social worker at a metropolitan brachial plexus center conducted psychosocial assessments and questionnaire assessments of 21 patients evaluating for PTSD, depression, and substance use using 3 validated scales: PTSD Checklist-Specific, Patient Health Questionnaire-8, and National Institute on Drug Abuse Quick Screen...
April 17, 2018: Journal of Hand Surgery
https://www.readbyqxmd.com/read/29642834/-risk-of-travel-associated-tuberculosis
#5
Süheyla Sürücüoğlu
Tuberculosis has spread by human movements throughout history. There have been reports indicating tuberculosis transmission on all travel vehicles, including aircrafts, ground vehicles and vessels until today. However, due to the ever increasing of air transportation and air travelling among countries with low and high tuberculosis incidence, transmission risk especially in aircrafts has become an important issue worldwide. But in many of the studies conducted in this regard, transmission of tuberculosis in aircrafts was found very low...
January 2018: Mikrobiyoloji Bülteni
https://www.readbyqxmd.com/read/29557724/drug-targeted-virtual-screening-and-molecular-dynamics-of-lipu-protein-of-mycobacterium-tuberculosis-and-mycobacterium-leprae
#6
Gurkamaljit Kaur, Bharati Pandey, Arbind Kumar, Naina Garewal, Abhinav Grover, Jagdeep Kaur
The lipolytic protein LipU was conserved in mycobacterium sp. including M. tuberculosis (MTB LipU) and M. leprae (MLP LipU). The MTB LipU was identified in extracellular fraction and was reported to be essential for the survival of mycobacterium. Therefore to address the problem of drug resistance in pathogen, LipU was selected as a drug target and the viability of finding out some FDA approved drugs as LipU inhibitors in both the cases was explored. Three dimensional (3D) model structures of MTB LipU and MLP LipU were generated and stabilized through molecular dynamics (MD)...
March 20, 2018: Journal of Biomolecular Structure & Dynamics
https://www.readbyqxmd.com/read/29556217/molecular-and-conventional-analysis-of-acute-diarrheal-isolates-identifies-epidemiological-trends-antibiotic-resistance-and-virulence-profiles-of-common-enteropathogens-in-shanghai
#7
Feng Yang, Yonggen Jiang, Lihua Yang, Juanxiu Qin, Mingquan Guo, Yuxia Lu, Hongyou Chen, Yuan Zhuang, Jinghao Zhang, Hong Zhang, Zhaoyun Dai, Min Li, Changqing Yang, Min Chen, Yanmei Zhang, Hu Zhao
Objective: To investigate prevalence of acute diarrhea in Shanghai and analyze virulence associated-genes and antibiotic resistance of major enteropathogens using combination of conventional and molecular epidemiology methods. Method: The 412 stool specimens were obtained by systematic sampling from diarrhea patients throughout entire year 2016. Bacterial and viral pathogens were identified and bacterial isolates were cultured and screened for antibiotic resistance profiles. Two most prevalent bacteria, Vibrio parahaemolyticus and Salmonella were further typed by multi-locus sequence typing (MLST) and analyzed for presence of virulence-associated genes...
2018: Frontiers in Microbiology
https://www.readbyqxmd.com/read/29517154/quantification-of-cystine-in-human-renal-proximal-tubule-cells-using-liquid-chromatography-tandem-mass-spectrometry
#8
Amer Jamalpoor, Rolf W Sparidans, Carla Pou Casellas, Johannes J M Rood, Mansi Joshi, Rosalinde Masereeuw, Manoe J Janssen
Nephropathic cystinosis is characterized by abnormal intralysosomal accumulation of cystine throughout the body, causing irreversible damage to various organs, particularly the kidneys. Cysteamine, the currently available treatment, can reduce lysosomal cystine and postpone disease progression. However, cysteamine poses serious side effects and does not address all of the symptoms of cystinosis. To screen for new treatment options, a rapid and reliable high-performance liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed to quantify cystine in conditionally immortalized human proximal tubular epithelial cells (ciPTEC)...
March 8, 2018: Biomedical Chromatography: BMC
https://www.readbyqxmd.com/read/29380379/high-throughput-oxidation-screen-of-antibody-drug-conjugates-by-analytical-protein-a-chromatography-following-ides-digest
#9
Jakob W Buecheler, Matthias Winzer, Christian Weber, Henning Gieseler
OBJECTIVES: Oxidation of protein therapeutics is a major chemical degradation pathway which may impact bioactivity, serum half-life and stability. Therefore, oxidation is a relevant parameter which has to be monitored throughout formulation development. Methods such as HIC, RPLC and LC/MS achieve a separation of oxidized and non-oxidized species by differences in hydrophobicity. Antibody-drug conjugates (ADC) although are highly more complex due to the heterogeneity in linker, drug, drug-to-antibody ratio (DAR) and conjugation site...
May 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29378620/human-infection-with-sub-periodic-brugia-spp-in-gampaha-district-sri-lanka-a-threat-to-filariasis-elimination-status
#10
Chandana H Mallawarachchi, T G A Nilmini Chandrasena, Ranjan Premaratna, S M N S M Mallawarachchi, Nilanthi R de Silva
BACKGROUND: Post-mass drug administration (MDA) surveillance during the lymphatic filariasis (LF) elimination program in Sri Lanka, revealed the re-emergence of brugian filariasis after four decades. This study was done with the objectives of investigating the epidemiology and age-specific vulnerability to infection. Surveillance was done using night blood smears (NBS) and the Brugia rapid test (BRT), to detect microfilaria (MF) and anti-Brugia IgG4 antibodies in blood samples collected from an age-stratified population enrolled from two high-risk study areas (SA)s, Pubudugama and Wedamulla in the Gampaha District...
January 29, 2018: Parasites & Vectors
https://www.readbyqxmd.com/read/29333040/pharmacological-screening-of-trachyspermum-ammi-for-antihyperlipidemic-activity-in-triton-x-100-induced-hyperlipidemia-rat-model
#11
Uzma Saleem, Saba Riaz, Bashir Ahmad, Mohammad Saleem
Background: Mortality rate is increasing due to cardiovascular problems throughout the world. These cardiac problems are directly associated with dyslipidemia. Aim: The aim of this study was to evaluate the antihyperlipidemic effect of aqueous extract and methanol extract of Trachyspermum ammi at 1 g/kg, 3 g/kg, and 5 g/kg dose levels in rats. Materials and Methods: For this purpose, 45 male albino rats were used and randomly divided into nine equal groups ( n = 5)...
December 2017: Pharmacognosy Research
https://www.readbyqxmd.com/read/29297315/utilizing-random-forest-qsar-models-with-optimized-parameters-for-target-identification-and-its-application-to-target-fishing-server
#12
Kyoungyeul Lee, Minho Lee, Dongsup Kim
BACKGROUND: The identification of target molecules is important for understanding the mechanism of "target deconvolution" in phenotypic screening and "polypharmacology" of drugs. Because conventional methods of identifying targets require time and cost, in-silico target identification has been considered an alternative solution. One of the well-known in-silico methods of identifying targets involves structure activity relationships (SARs). SARs have advantages such as low computational cost and high feasibility; however, the data dependency in the SAR approach causes imbalance of active data and ambiguity of inactive data throughout targets...
December 28, 2017: BMC Bioinformatics
https://www.readbyqxmd.com/read/29289377/treatment-of-paraphilic-disorders-in-sexual-offenders-or-men-with-a-risk-of-sexual-offending-with-luteinizing-hormone-releasing-hormone-agonists-an-updated-systematic-review
#13
REVIEW
Daniel Turner, Peer Briken
BACKGROUND: Different pharmacologic agents are used in the treatment of paraphilic disorders in sexual offenders or men with a risk of sexual offending, with luteinizing hormone-releasing hormone (LHRH) agonists being the agents introduced more recently to treatment regimens. AIM: To summarize the relevant literature concerning LHRH agonist treatment of paraphilic disorders in sexual offenders and update the previously published systematic review by Briken et al (J Clin Psychiatry 2003;64:890-897)...
January 2018: Journal of Sexual Medicine
https://www.readbyqxmd.com/read/29249913/new-strategies-to-improve-polypectomy-during-colonoscopy
#14
Michael B Wallace
In the United States, colorectal cancer (CRC) is the second-leading cause of cancer-related deaths. The most effective strategy for prevention of CRC is to screen for and remove precancerous polyps. There are various ways to screen for CRC. In the United States, the most common method is colonoscopy. Polyps are classified primarily through pathology. Size is the primary risk factor for malignancy. In general, the bigger the polyp, the greater the risk for malignancy. There are 3 basic options for removal: standard polypectomy; advanced resection techniques, known as endoscopic mucosal resection (EMR) and endoscopic submucosal dissection (ESD); and surgical removal...
October 2017: Gastroenterology & Hepatology
https://www.readbyqxmd.com/read/29227878/harm-reduction-based-and-peer-supported-hepatitis-c-treatment-for-people-who-inject-drugs-in-georgia
#15
Tamar Kikvidze, Niklas Luhmann, Elisabeth Avril, Maia Butsashvili, Konstantine Labartkava, Aurélie Etienne, Diane Le Pluart, Ina Inaridze, Ana Gamezardashvili, David Kharshiladze, Julie Bouscaillou
No abstract text is available yet for this article.
February 2018: International Journal on Drug Policy
https://www.readbyqxmd.com/read/29215913/high-content-screening-comparison-of-cancer-drug-accumulation-and-distribution-in-two-dimensional-and-three-dimensional-culture-models-of-head-and-neck-cancer
#16
Feng Shan, David A Close, Daniel P Camarco, Paul A Johnston
High cancer drug development attrition rates have provoked considerable debate about whether the two-dimensional tumor growth inhibition high-throughput screening assays used in pre-clinical lead discovery adequately reflect solid tumor complexity. We used automated high-content screening image acquisition and analysis methods to compare fluorescent drug uptake, accumulation, and distribution in Cal33 and FaDu head and neck cancer (HNC) monolayer and multicellular tumor spheroid (MCTS) models. Ellipticine, idarubicin, daunorubicin, and doxorubicin were studied because of their fluorescent properties and broad anti-tumor activities...
January 2018: Assay and Drug Development Technologies
https://www.readbyqxmd.com/read/29201009/-in-vitro-and-in-silico-risk-assessment-in-acquired-long-qt-syndrome-the-devil-is-in-the-details
#17
REVIEW
William Lee, Monique J Windley, Jamie I Vandenberg, Adam P Hill
Acquired long QT syndrome, mostly as a result of drug block of the Kv11. 1 potassium channel in the heart, is characterized by delayed cardiac myocyte repolarization, prolongation of the T interval on the ECG, syncope and sudden cardiac death due to the polymorphic ventricular arrhythmia Torsade de Pointes (TdP). In recent years, efforts are underway through the Comprehensive in vitro proarrhythmic assay (CiPA) initiative, to develop better tests for this drug induced arrhythmia based in part on in silico simulations of pharmacological disruption of repolarization...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/29044549/effects-of-clioquinol-on-the-scuticociliatosis-causing-protozoan-miamiensis-avidus-in-olive-flounder-paralichthys-olivaceus
#18
J-H Lee, J-J Park, J-H Choi, S-Y Kang, Y-J Kang, K H Park
Scuticociliatosis is a devastating and intractable protozoal disease in olive flounder, leading to a significant loss throughout the year. This study aimed to investigate a systemically effective antiscuticociliatosis agent for olive flounder for better absorption into the infected internal organs. The in vitro and in vivo antiscuticociliatosis effects of clioquinol (CQ) were examined after screening 30 biocidal agents against the highly pathogenic scuticociliate Miamiensis avidus. CQ was the most potent in vitro drug of those tested against cultured M...
March 2018: Journal of Fish Diseases
https://www.readbyqxmd.com/read/28979759/mass-spectrometric-directed-system-for-the-continuous-flow-synthesis-and-purification-of-diphenhydramine
#19
Bradley P Loren, Michael Wleklinski, Andy Koswara, Kathryn Yammine, Yanyang Hu, Zoltan K Nagy, David H Thompson, R Graham Cooks
A highly integrated approach to the development of a process for the continuous synthesis and purification of diphenhydramine is reported. Mass spectrometry (MS) is utilized throughout the system for on-line reaction monitoring, off-line yield quantitation, and as a reaction screening module that exploits reaction acceleration in charged microdroplets for high throughput route screening. This effort has enabled the discovery and optimization of multiple routes to diphenhydramine in glass microreactors using MS as a process analytical tool (PAT)...
June 1, 2017: Chemical Science
https://www.readbyqxmd.com/read/28951824/intraocular-in%C3%A2-vivo-imaging-of-pancreatic-islet-cell-physiology-pathology
#20
REVIEW
Ingo B Leibiger, Per-Olof Berggren
BACKGROUND: Diabetes mellitus has reached epidemic proportions and requires new strategies for treatment. Unfortunately, the efficacy of treatment regimens on maintaining/re-gaining functional beta cell mass can, at the present, only be determined indirectly. Direct monitoring of beta cell mass is complicated by the anatomy of the endocrine pancreas, which consists of thousands to a million of discrete micro-organs, i.e. islets of Langerhans, which are scattered throughout the pancreas...
September 2017: Molecular Metabolism
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