6 Innovations in Drug Discovery Biomolecule Research

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.