In Vitro Permeability Assay Articles & Analysis
20 articles found
ELANE, or neutrophil elastase (NE), is a serine protease stored in the azurophilic granules of neutrophils and is encoded by the ELANE gene on chromosome 19. It plays a pivotal role in the host defense system by degrading bacterial proteins, remodeling extracellular matrices, and shaping inflammatory responses. However, the same proteolytic activity that protects against pathogens can, when ...
The world of drug development has long been marked by the rigorous assessment of cardiac safety. Recognizing the need for a more accurate and efficient evaluation system, the Comprehensive in vitro Proarrhythmia Assay (CiPA) initiative emerged. At the heart of this initiative are CiPA Translational Assays, designed to improve the prediction of drug-induced cardiac arrhythmias. Understanding the ...
In vitro permeability assay kits play a crucial role in the field of pharmaceutical development, particularly when evaluating the absorption characteristics of drugs. ...
Hepatocytes are the chief functional cells of the liver, responsible for the selective uptake, metabolism and excretion of most drugs. Cells for use in plate cultures or suspension assays represent a key tool for predicting properties such as hepatotoxicity, metabolism, and potential drug-drug interactions. Since these cells mimic the properties of the liver, researchers can evaluate the ...
The Clinical CRISPR Successes Are Stacking Up. But Where’s the Emphasis on Quality Control? In mid-September, Intellia released some promising data on two of their CRISPR-based therapeutics. These results are a significant milestone for genome editing and validation of its effectiveness in the clinic. However, the safety of CRISPR-based therapeutics has been a major concern and part of a ...
On February 16, 2022, the data on Paxlovid previously published by Pfizer and submitted to the FDA were published in the New England Journal of Medicine (NEJM). This NEJM article published viral load data that Paxlovid reduced viral load by 0.868 log10 compared to controls for 5 days of treatment, which equates to a remarkable 7.38-fold reduction in viral load. This pivotal study (NCT04960202) ...
Treatment options for COVID-19 remain limited. Researchers at the University of Helsinki and the University of Eastern Finland first searched for appropriate drug targets and reusable drugs and finally discovered six candidates with antiviral effects against SARS-CoV-2. Understanding viral pathogenesis at the molecular level is key to the development of effective therapies for COVID-19. The ...
Overview Confirm Cas9 mRNA expression With our ready-to-use Cas9 RT-PCR primer set, you can quickly and easily confirm Cas9 expression in cells or in vitro transcription assays. The amplicon for Game 1 is 219 bp and the amplicon for Game 2 2 is 122 bp. These primer sets allow the detection of nuclease Cas9, Nickase Cas9 and double mutant Cas9 at the messenger level. The primer sets are compatible ...
For a long time, electrophilic groups have been a minefield in drug development. Therefore, in the classic medicinal chemistry textbooks of the past, it is always recommended to avoid introducing functional groups such as epoxide, acridine and Michael receptor into the structure of drug molecules, because these functional groups are highly reactive and may interact with a wide range of biological ...
Abstract Lactobacillusspecies are the predominant vaginal microbiota found in healthy women of reproductive age and help to prevent pathogen infection by producing lactic acid, H2O2 and anti-microbial compounds. Identification of novel vaginalLactobacillus isolates that exhibit efficient colonisation and secrete anti-Candida factors is a promising strategy to prevent vulvovaginal candidiasis. ...
Abstract Protease proprotein convertase subtilisin-like kexin type 9 (PCSK9) is an important target for the treatment of hypercholesterolemia. Several pharmaceutical companies have focused on the development of mAbs. Yet, our approach has focused on developing orally bioavailable small molecule antagonists. PCSK9 is a serine protease that is synthesized as a zymogen that undergoes autocatalytic ...
The US Environmental Protection Agency has responsibility for assessing endocrine activity of more than 10 000 chemicals, a task that cannot reasonably be achieved solely through use of available mammalian and nonmammalian in vivo screening assays. Hence, it has been proposed that chemicals be prioritized for in vivo testing using data from in vitro high‐throughput assays for specific ...
Coumarin derivative anticoagulant rodenticides used for rodent control are posing a serious risk to wild bird populations. For warfarin (WF) a classic coumarin derivative, chicken have a high LD50 while mammalian species generally have much lower LD50. Large interspecies differences in sensitivity to WF are to be expected. We previously reported substantial differences in WF metabolism among ...
Changes in the endocrine potency of municipal wastewater at 3 wastewater treatment plants (WWTPs) in Australia were investigated using a panel of in vitro receptor‐driven transactivation assays. The assays were based on human estrogen receptor α, androgen receptor, progesterone receptor, glucocorticoid receptor, and peroxisome proliferator‐activated receptor γ2. Total removal efficiencies for ...
In vitro biotransformation assays are currently being explored to improve estimates of bioconcentration factors of potentially bioaccumulative organic chemicals in fish. This study compares thin‐film and solvent‐delivery dosing techniques, as well as single vs. multiple chemical dosing for measuring biotransformation rates of selected polycyclic aromatic hydrocarbons in rainbow trout ...
The incorporation of brominated flame retardants into industrial and household appliances has increased their occurrence in the environment resulting in deleterious effects on wildlife. With the increasing restraints on available compounds there has been a shift to using BFRs that has seen the production of alternative BFRs such as 1,2‐dibromo‐4‐(1,2 dibromoethyl) cyclohexane (TBECH). TBECH ...
Perfluorooctane sulfonate (PFOS) is a widespread and persistent chemical in the environment. We investigated the endocrine‐disrupting effects of PFOS using a combination of in vitro and in vivo assays. Reporter gene assays were used to detect receptor‐mediated (anti‐)estrogenic, (anti‐)androgenic, and (anti‐)thyroid hormone activities. The effect of PFOS on steroidogenesis was assessed both at ...
Previous studies have shown inexplicable declines in breeding waterbirds within western New York/New Jersey Harbor between 1996 and 2002 and elevated polychlorinated dibenzo‐p‐dioxins and polychlorinated biphenyls (PCBs) in double‐crested cormorant (Phalacrocorax auritus) eggs. The present study assessed associations between immune function, prefledgling survival, and selected organ chlorine ...
octreotate has been used for cancer diagnosis and therapy because of its high affinity to somatostatin subtype receptors sstr2 and sstr5. The aim of this study was to evaluate the cytogenetic effect of radio-labelled octreotate in blood cells in vitro, using the cytokinesis-block micronucleus assay. Blood samples of healthy donors were exposed to different activities of octreotate labelled with ...
As indicated by a few recent reports, exposures to low doses of ionising radiation can trigger the activity of natural anti-tumour defence mechanisms and impede the development of transplantable tumours in rodents. In our experimental system, BALB/c mice were irradiated with a single dose of 0.1, 0.2, 0.5, or 1.0 Gy X-rays and then i.v. injected with L1 sarcoma cells. As shown by the results of ...