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6 Innovations in Drug Discovery Biomolecule Research

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Discover a smartphone app that improves column selection, plus a new method for the quantification of bradykinin in plasma

22 Sept 2015
Sarah Thomas
Associate Editor

Editorial article

Learn more about high-tech column selection, natural product characterization and quantitation, and transferring workflows from ELISA to FLISA

Column Genie – Improved Column Selection at Your Fingertips

The Column Genie app from Thermo Fisher Scientific is a unique tool that helps you choose the most suitable LC column for your application. Filter the catalogue of more than 100 columns by chromatographic mode or application area, and refine results based on parameters such as particle size and column dimensions. Watch this video to learn how to navigate the Column Genie app on a tablet, taking you step by step through the app's functionality. The app is available for iOS and Android devices. Read more.

Fluorescence Polarization-Based Assay for Screening for H-Prostaglandin D Synthase Inhibitors

Prostaglandins are a group of lipid compounds that are involved in diverse effects in animal physiology. Prostaglandin D2 (PGD2) has been characterized for its role in asthma, where its concentration has been shown to be 10 times higher in asthma patients, leading to bronchial airway contraction after exposure to an allergen. For this and other reasons, inhibitors are sought for the hematopoietic prostaglandin D synthase (H-PGDS) which catalyzes the final PGD2 biosynthesis step. This application note evaluates the performance of Cayman Chemicals’ green FP-based inhibitor assay screening kit. The kit was tested with both the CLARIOstar and PHERAstar FS from BMG Labtech. Settings more suitable for high throughput screening (HTS) were also tested. Download method.

An Improved SPE-LC-MS/MS Method for the Quantification of Bradykinin in Human Plasma Using the ionKey/MS

This study utilizes specifically designed blood collection techniques to inhibit bradykinin formation ex vivo, taking advantage of mixed mode solid-phase extraction (SPE) and use of the novel and highly efficient ionKey/MS System from Waters for selective, sensitive, and robust chromatographic separation, and quantification of the nonopeptide. Accurate quantification of bradykinin in plasma is particularly challenging because it is present in low pg/mL levels, is rapidly metabolized, and is also artificially produced during blood sampling and sample preparation via proteolytic processes. Peptides in general are often difficult to analyze by LC-MS/MS, as mass spectrometer (MS) sensitivity can be low due to the formation of multiple precursors and poor or overly extensive fragmentation. Download method.

Determination of Drug-Kinase Residence Time with the Transcreener® ADP2 FP Assay

This application note provides a protocol and experimental example for the use of the Transcreener® ADP2 FP Assay from BellBrook Labs, to determine the residence time of a drug (or drug candidate) during its interaction with a kinase. The duration of residence time may be highly relevant for assessing the durable pharmacologic effects of a drug candidate. In general, longer residence time results in improved efficacy, as the extended contact between drug and enzyme results in extended inhibition of enzyme activity, which in turn allows longer pharmacological effects at lower doses, reducing off-target effects. Download method.

Multiplexed FLISA Assays on mirrorball®

Enzyme-linked immunosorbant assays (ELISA) can be used in multiple stages of the drug discovery process to help identify and measure the cellular responses to therapeutic or toxic molecules. Although ELISAs are very sensitive, they are time-consuming, require multiple separate wash steps and incubation steps, and are not amenable to multiplexing. This application note from TTP Labtech demonstrates the transfer of standard commercially available colorimetric IL-8 and IL-6 ELISA kits onto a no-wash bead-based assay format on the mirrorball, FLISA (fluorescence-linked immunosorbant assay). Download method.

Webinar Highlights: Strategies for the Separation and Characterization of Protein Biopharmaceuticals

Protein biopharmaceuticals are being developed at an explosive rate and have attracted great interest from both smaller biotech firms and large pharmaceutical companies. Developing protein biopharmaceuticals and their follow-on versions is highly demanding in many ways. From an analytical perspective, handling biomolecules presents new challenges for chromatographers, and the field of bio-chromatography is advancing rapidly as new and higher resolution techniques for characterizing proteins, including monoclonal antibodies, are evaluated and better understood. Read the highlights or watch the webinar on-demand.

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You can also learn more about biomolecules in drug discovery on our biopharmaceuticals page.

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LC-MSLC-MS (liquid chromatography-mass spectrometry) systems and equipment are used for separation and quantitative analysis of complex mixtures, combining liquid chromatography and mass spectrometry. Quantify proteins, contaminants, pesticides or screen for drug metabolites with a high level of sensitivity. LC-MS systems and equipment include reverse phase, normal phase and specialized columns integrated with various MS detectors such as time-of-flight (TOF), quadrupole, orbitrap or ion trap mass analyzers. LC-MS/MS instruments equipped with a qTOF or triple quadrupole analyzer give greater sensitivity and resolving power to your analysis. Find the best LC-MS equipment in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.Mass SpectrometryMass spectrometry (MS) is a powerful analytical technique used to identify and quantify molecules based on the mass-to-charge ratio of gas-phase ions. It provides detailed information about the structure, composition, and properties of compounds and is widely used across fields such as environmental monitoring, materials science, drug discovery and development, food and beverage testing, and wider chemical research. Key MS techniques include tandem mass spectrometry (MS/MS), liquid chromatography–mass spectrometry (LS-MS) and inductively coupled plasma (ICP-MS). Choosing from these wide range of techniques and technologies can be a daunting task, so keep up to date with scientific applications, performance expectations, and customer reviews here all in one place. Visit our product directory to receive quotes direct from the manufacturer. ELISAEnzyme-linked immunosorbent assays (ELISA), also known as enzyme immunoassays (EIA), are used for the detection and quantification of proteins, peptides and antibodies in a sample. ELISA often comes in kit format, with pre-selected antibody pairs to detect specific proteins or biomarkers of diseases such as diabetes and obesity, or cardiovascular and neurological disorders. Detection is made possible with chemiluminescent, fluorescent or colorimetric substrates and detection instruments such as microplate / ELISA readers. Other kits available include: Enzyme-linked immunospot (ELISPOT) assays for the quantification of protein-producing cells and chemiluminescent immunoassays (CLIA) kits. Find the best ELISA kits and products in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.High-Throughput ScreeningHigh-throughput screening (HTS) is an automated drug discovery technique for identification of active compounds against a compound library. Use HTS readers and integrated assay preparation / analysis workstations to screen your compounds. Identify active compounds against various HTS libraries, including membranes, proteins and peptides and HTS cell lines. Find the best high-throughput screening products in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.Microplate Readers / DetectorsMicroplate readers are used to automate the detection and analysis of labeled or label-free components in microplates during assays or live-cell monitoring. Microplate readers are generally distinguished by their mode of detection. Types include absorbance, luminescence, fluorescence intensity, fluorescence polarization, TRF / FRET and multimode microplate readers. Microplate readers deliver a high throughput of samples by reading multiple wells simultaneously, with the 96-well format the most commonly used. As a result, microplate readers are often used in the drug discovery, bioassays, research and pharmaceutical industries for screening applications. Microplate loading can also be automated, with robotic microplate stackers to increase throughput. Find the best microplate readers in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.ADME-ToxicologyADME-toxicology (ADME-Tox) studies are used in pharmacology and pharmacokinetics to assess the activity/toxicity of drugs <i>in vivo</i> or <i>in vitro</i>. Find bioassays for absorption, distribution, metabolism, and excretion of drug molecules including cytotoxicity, transporter/permeability, metabolism and activity assays as well as hepatocytes and cell lines for ADME. Find the best ADME-toxicology products in our peer-reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.Cell-Based AssaysCell-based assays are used to monitor the presence, quantity and activities of a desired cellular analyte including drug molecules or biomarkers. This can reveal information on cell health (apoptosis, cytotoxicity, viability and proliferation assays), cell metabolism, cell migration and cell signaling mechanisms. Find the best cell-based assay products, kits and equipment with our peer reviewed product directory: compare products, check customer reviews and receiving pricing direct from manufacturers.Compound AnalysisCompound analysis is used to discover specific compounds that could be promising candidates for pharmaceutical use. This potential is identified when compounds have the desired effect, such as interaction with a target protein, during high throughput screening.Toxicology / Drugs of Abuse TestingToxicology and Drugs of Abuse Testing is the investigation into toxic and illegal substances found at the scene of a crime or from a suspect and / or victim associated with a scene of a crime. Analyzers, immunoassays and drugs of abuse test kits and presumptive test kits are an essential aspect of toxicology investigation.AutomationAutomation in laboratories and manufacturing processes enhances efficiency, precision, and scalability by reducing the need for manual intervention. It plays a critical role in improving productivity, minimizing human error, and accelerating workflows in fields like diagnostics, drug development, and industrial testing. Automation technologies include robotic systems, automated liquid handlers, and process control systems that streamline complex tasks and ensure consistent, reproducible results. Explore our peer-reviewed product directory to discover the best automation solutions, compare options, read user reviews, and get prices directly from manufacturers.Fluorescence Based AssayFluorescence based assays are widely used in life science research and high-throughput screening to measure a broad range of cellular activities.Drug TestingIt is essential to test the efficacy and toxicity of drugs at every stage of their development to ensure that a pharmaceutical product is fit for purpose and safe for use before reaching the stage of mass production and distribution.High ThroughputHigh throughput experiments allow the simultaneous processing of several samples. This parallelization reduces the cost per experiment and increases reproducibility and output volume of data.PharmacokineticsBiopharmaceuticalsBiopharmaceuticals are proteins and other compounds (such as nucleic acids) produced by living organisms that have uses as therapeutics or for in vivo diagnostics. The most well known example of a biopharmaceutical product, and the first to be approved for therapeutic use, was recombinant human insulin.

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