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Drug Discovery & Development White Papers

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91-105 of 137 results
Analysis of Water-Soluble Polymers Using Linear Size Exclusion HPLC Columns and a Semi-Micro SEC System
| By Tosoh Bioscience
In recent years water-soluble polymers are gaining more and more interest in different applications. The molecular weight distribution of polymers is usually characterized by size exclusion chromatography (SEC) coupled with refractive index, viscometric or laser light scattering detection. Recent advances in SEC comprise semi-micro SEC and the design of linear columns providing wide molecular weight separation ranges and near-linear calibrations.
Drug Research > Drug Discovery & Development > White Papers
CHARACTERIZING BIOTHERAPEUTICS WITH HPLC
| By Tosoh Bioscience
Development and production of biopharmaceuticals is a growing segment of pharmaceutical industry. Therapeutic proteins include blood factors, thrombolytic agents, growth factors, interferons, interleukins, therapeutic enzymes and last but not least monoclonal antibodies.
Drug Research > Drug Discovery & Development > White Papers
Reversed-Phase Analysis of Alkylbenzene Sulfonates
| By Tosoh Bioscience
Linear alkylbenzene sulfonates (LASs) are synthetic surfactants, which are produced by alkylation and sulfonation of benzene. LASs are a mixture of homologues and phenyl positional isomers, each containing an aromatic ring sulfonated at the para position and attached to a linear alkyl chain. The product is used in detergents and cleaning products for domestic and industrial use.
Drug Research > Drug Discovery & Development > White Papers
Characterisation Studies of PEGylated Lysozyme
| By Tosoh Bioscience
PEGylation, the process by which polyethylene glycol (PEG) chains are attached to protein and peptide drugs is a common practice in the development of biopharmaceuticals to prolong serum half-life and improve pharmacokinetics of a drug. There is increasing demand for chromatographic methods to separate the modified isoforms from the native protein.
Drug Research > Drug Discovery & Development > White Papers
Glycosylation analysis by hydrophilic interaction chromatography (HILIC) – N-Glyco mapping of the ZP-domain of murine TGFR-3
| By Tosoh Bioscience
Glycosylation is one of the most common forms of post-translational modification of eukaryotic proteins. Glycosylated proteins (glycoproteins) make up the majority of human proteins. The polysaccharide side chains (Glycans) play critical roles in physiological and pathological reactions ranging from immunity to cell signaling, development and death.
Drug Research > Drug Discovery & Development > White Papers
Alternate Selectivity for Polar Compounds in Hydrophilic Interaction Liquid Chromatography (HILIC) Using a New Amino Type HILIC Column
| By Tosoh Bioscience
Hydrophilic interaction liquid chromatography (HILIC) offers unique advantages for the separation of very polar compounds when compared to reversed-phase chromatography. A new silica based HILIC phase was developed to provide additional selectivity options in HILIC separations. The separation of water soluble vitamins on the new TSKgel NH2-100 HILIC column and on the well known TSKgel Amide-80 HILIC column demonstrates the differences in selectivity.
Drug Research > Drug Discovery & Development > White Papers
Analysis of Melamine and Cyanuric Acid in Milk by LC-MS/MS
| By Tosoh Bioscience
Melamine is an organic base and a trimer of cyanamide, with a 1,3,5-triazine skeleton. Melamine is combined with formaldehyde to produce melamine resin, a very durable thermosetting plastic, and melamine foam, a polymeric cleaning product. The end products include countertops, dry erase boards, fabrics, glues, house wares and flame retardants. Melamine is one of the major components in Pigment Yellow 150, a colorant in inks and plastics.
Drug Research > Drug Discovery & Development > White Papers
HPLC Analysis of lysozyme in different types of wine
| By Tosoh Bioscience
Hen’s egg white lysozyme is used in winemaking to eliminate lactic acid bacteria and to control malolactic fermentation. As eggs and derivatives are regarded as potential allergenics the European Commission issued a directive that wine labels must include information about egg derived ingredients like lysozyme. As a consequence the International Organisation for Wine and Vine (OIV) published a standard method for measurement of lysozyme in wine by HPLC, which is based on a method developed at the University of Bologna.
Drug Research > Drug Discovery & Development > White Papers
Analysis of cationic polymers by Size Exclusion Chromatography with TSK-GEL®
| By Tosoh Bioscience
In recent years water soluble cationic polymers are gaining more and more interest in different applications ranging from hair conditioning to gene transfection and drug delivery. The molecular weight distribution of polymers is usually characterized by SEC coupled with refractive index, viscometric or laser light scattering detection.
Drug Research > Drug Discovery & Development > White Papers
HILIC–MS - High Resolution and Sensitivity for the Analysis of Very Polar Compounds
| By Tosoh Bioscience
Hydrophilic interaction liquid chromatography (HILIC) offers unique advantages for mass spectrometric detection of very polar compounds when compared to reversed phase chromatography. The higher organic content of the eluent in HILIC supports efficient evaporation of the solvent, thus enhancing sensitivity and altering ion suppression.
Drug Research > Drug Discovery & Development > White Papers
Journal of Biomolecular Screening
| By ZoBio
Fragment-based drug discovery (FBDD) has become a widely accepted tool that is complementary to high-throughput screening (HTS) in developing small-molecule inhibitors of pharmaceutical targets. Because a fragment campaign can only be as successful as the hit matter found, it is critical that the first stage of the process be optimized. Here the authors compare the 3 most commonly used methods for hit discovery in FBDD: high concentration screening (HCS), solution ligandobserved nuclear magnetic resonance (NMR), and surface plasmon resonance (SPR). They selected the commonly used saturation transfer difference (STD) NMR spectroscopy and the proprietary target immobilized NMR screening (TINS) as representative of the array of possible NMR methods. Using a target typical of FBDD campaigns, the authors find that HCS and TINS are the most sensitive to weak interactions. They also find a good correlation between TINS and STD for tighter binding ligands, but the ability of STD to detect ligands with affinity weaker than 1 mM KD is limited. Similarly, they find that SPR detection is most suited to ligands that bind with KD better than 1 mM. However, the good correlation between SPR and potency in a bioassay makes this a good method for hit validation and characterization studies.
Drug Research > Drug Discovery & Development > White Papers
Target Immobilization and NMR Screening of Fragments in Early Drug Discovery
| By ZoBio
Using localized NMR spectroscopy on immobilized targets provides us with a method to simultaneously assess binding of small molecules to two different samples. This Target Immobilized NMR Screening (TINS) has a number of advantages, not least is the requirement for minimal quantities of non-isotopically labeled protein and the applicability to insoluble or unstable targets. The technique is sensitive to binding with KD values in the range of 100 nM to 20 mM, while careful selection of the reference protein reduces the number of false positive hits. This combination ensures a maximal number of valid hits from which to select starting points for hit elaboration projects. Hits can be prioritized using biological assays when appropriate, as well as an array of biophysical techniques. So far a variety of soluble proteins, including kinases, GTPases, viral targets and proteases, as well as a membrane protein, have been successfully screened against our fragment library. Here we illustrate our experiences with a number of examples which emphasize the usefulness of the method in selecting and prioritizing fragment hits for elaboration towards leads.
Drug Research > Drug Discovery & Development > White Papers
91-105 of 137 results