in vitro assay Articles
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hspCas9-RT-PCR Primer Set
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 ...
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Inhibition of the development of pulmonary tumour nodules and stimulation of the activity of NK cells and macrophages in mice by single low doses of low-LET radiation
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 ...
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CYP‐mediated warfarin metabolic ability is not a critical determinant of warfarin sensitivity in avian species; in vitro assays in several birds and in vivo assays in chicken
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 ...
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Paxlovid: Spring of Caronic Anhydrides
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) ...
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TBECH‐mediated steroid hormone receptor activation and gene regulation in chicken LMH cells
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 ...
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121 - Development of Protease Proprotein Convertase Subtilisin-Like Kexin Type 9 Antagonists
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 ...
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Abstract 4842: A comparative preclinical study of PARP inhibitors demonstrates superb properties for IDX-1197
Abstract Background PARP inhibitors have demonstrated clinically meaningful increase in progression-free survival as a single agent in women with recurrent ovarian cancer following a response to platinum-based chemotherapy. We aimed to develop a novel PARP inhibitor that may have potent antitumor efficacy. IDX-1197 is a novel, potent, selective, and orally bioavailable poly (ADP-ribose) ...
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Abstract A106: Development of IDX-1197, a novel, selective, and highly potent PARP inhibitor
Abstract Background: PARP inhibitors have demonstrated clinically meaningful increase in progression-free survival as a single agent in women with recurrent ovarian cancer following a response to platinum-based chemotherapy. However, there still needs more improvement in efficacy because PARP inhibitors have comparatively low efficacy in non-germline BRCA-mutated patients. We aimed to develop ...
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Perfluorooctane sulfonate (PFOS) affects hormone receptor activity, steroidogenesis, and expression of endocrine‐related genes in vitro and in vivo
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 ...
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Pooled Human Cryopreserved Hepatocytes
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 ...
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Evaluation of the scientific underpinnings for identifying estrogenic chemicals in nonmammalian taxa using mammalian test systems
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 ...
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Assessment of multiple hormonal activities in wastewater at different stages of treatment
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 ...
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GST-Pull Down Technology
Introduction to protein interactions The functioning of biological systems is inextricably linked to protein-protein interactions, and important biological processes such as DNA synthesis, gene transcriptional activation, protein translation, modification and localization, and information transfer all involve the role of protein complexes. Therefore, it is particularly important to discover and ...
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Comprehensive protein interaction network helps discover candidate drugs for the treatment of COVID-19
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 ...
By Profacgen
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Design and R&D of Covalent Drugs
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 ...
By BOC Sciences
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Vaginal lactobacilli inhibit growth and hyphae formation of Candida albicans
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. ...
By KoBioLabs
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Clinical CRISPR Success Demonstrates Need for Quality Control
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 ...
By CRISPR QC
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Evaluating Microbiome Therapies with Intestinal Cell Models
The microbiome has been shown to play roles in many different disease processes and is implicated in many more, from infectious and gastrointestinal diseases to autoimmune and neurological disorders. Advanced models of the gut leveraging intestinal and colonic stem cells are enabling the development of more reliable and robust systems for evaluating the impact of changes in the microbiome on gut ...
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