High Throughput Screening in Drug Discovery for Cancer Research Peptides Using High Resolution LCMS

11 Jul 2013

Lead discovery groups are constantly developing new methodologies to screen large chemical libraries against a specific target. The majority of these methods utilize plate reader devices, ELISA, and other analytical techniques that are amenable to high throughput analysis. Existing analytical methodology used for screening can be less than ideal due to sample prep considerations, limit of detection, and specificity of analyte detection. In this application note read high resolution LCMS can provide a high quality alternative while maintaining a sampling rate that is suitable for HTS requirements.

Thermo Scientific Exactive Plus Orbitrap LC-MS

Thermo Fisher Scientific

The Exactive Plus Orbitrap LC-MS is a benchtop full scan mass spectrometer designed for compound identification and high-throughput, high-performance screening. The Exactive Plus delivers high resolution accurate mass (HRAM) data and fast, reproducible results for qualitative and quantitative analysis. The availability of HRAM and full scan capability gives you all the data, all the time. It allows retrospective data analysis and eliminates MS method development leading to improved and simplified analytical throughput.Exactive Plus is easy-to-use, cost effective to operate and coupled with workflow-driven software, makes an ideal instrument for new users in routine analytical laboratories.Selected benefits of the Exactive Plus are specified below: High Resolving Power (up to 140,000) - Eliminates isobaric interferences to increase confidence for analysis or complex samples Mass accuracy - Better than 1ppm in full scan and AIF scan using fully automated AGC and mass calibration procedures offers confident identification U-HPLC Scan Speed - The 12Hz scanning frequency of Exactive Plus is fully compatible with U-HPLC and ensures exact mass measurement for fast chromatography applications Fast Polarity Switching - A full cycle of 1 positive and 1 negative scan is performed within 1 second at a resolution setting of 35,000 without sacrificing mass accuracy All-Ion-Fragmentation (AIF) - With multiple dissociation techniques; in source collisional induced dissociation (CID) and high energy collisional dissociation (HCD), provides MS and MS/MS data Full MS scan, AIF scan, data dependent AIF, alternating Full MS and AIF scan Intuitive software interface The Exactive Plus Orbitrap LC-MS is ideal for the following applications: Environmental and Food Safety Clinical Research Forensic Toxicology Drug discovery, metabolism and pharmacokinetics (DMPK) Metabolomics Pharmaceutical BioPharma – Intact Protein analysis Laboratories analyzing food, pharmaceuticals, neutraceuticals, and other complex samples can now purchase Exactive Plus LC-MS system equipped from the factory with IonSense ID-CUBE™ ion sources. This configuration is designed to minimize the need for sample preparation to simplify and speed analyses.

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UHPLC and HPLCHigh performance liquid chromatography (HPLC) and ultra high performance liquid chromatography (UHPLC), also known as UPLC, are analytical techniques used to separate, identify and quantitate components of complex mixtures including biological samples such as proteins and lipids as well as chemical mixtures of pesticides, drugs and oils. Both techniques are liquid chromatographic methods but differ by operating pressures (HPLC < 6000 psi < UHPLC ). Components of HPLC and UHPLC systems include columns, detectors, pumps, autosamplers and column heaters. Explore a range of UHPLC and HPLC columns for your specific sample needs including reverse phase, normal phase, ion exchange, HILIC, ion exclusion and size exclusion columns. For more specialized HPLC, explore FPLC, countercurrent LC and simulated moving bed systems. Find the best UHPLC and HPLC equipment in our peer reviewed product directory: compare products, check customer reviews and receive pricing direct from manufacturers.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. 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.BiomarkersBiomarkers are biological markers which can be measured and evaluated to indicate a biological state. The use of biomarkers in research and diagnosis can indicate a normal or disease state or drug response of cells / tissues. Biomarkers include genetic markers, cell surface markers such as antigens, antibodies or receptors and secreted molecules such as cytokines. An assay system is required for identification of biomarkers. :Cancer ResearchAlthough cancer is often referred to as a single condition, it actually consists of more than 100 different diseases. Microscopy, mass spectrometry, high throughput sequencing and flow cytometry are some of the most common techniques employed in cancer research labs.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.PeptidesPeptides are short chains of amino acids that play key roles in biological processes, including signaling, immune responses, and enzyme regulation. Peptide research is critical in drug discovery, diagnostics, and vaccine development. Browse our peer-reviewed product directory to find the best peptides and peptide-related products, compare options, check reviews, and get pricing directly from manufacturers.