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Conformationally constrained peptide ligands offer an attractive format for the development of therapeutics. They can bind with high affinity and selectivity to protein targets, they are small enough to diffuse into tissues, they can be synthesized chemica ...
The detection of molecules that can bind to active sites of protein targets and the measurement of their affinities is a promising application of NMR. Nowadays, the screening of drug candidates is routinely done by NMR in pharmaceutical industry. We have p ...
This article reviews important presentations from the 7th Screening Europe Conference, and extracts general trends and developments. Technological advances, as well as novel applications are discussed, thus providing an overview on state-of-the-art high-th ...
Ligands that have an affinity for protein targets can be screened very effectively by exploiting favorable properties of long-lived states (LLS) in NMR spectroscopy. In this work, we describe the use of LLS for competitive binding experiments to measure ac ...
The identification of the targets of therapeutic drugs is one of the major challenges for pharmaceutical companies. The main target responsible for drug action is often known, but most drugs also bind other targets, either causing deleterious side effects ...
The peculiar chemical properties of metal-based drugs impart innovative pharmacological profiles to this class of therapeutic and diagnostic agents, most likely in relation to novel molecular mechanisms still poorly understood. However, inorganic drugs hav ...
The genetic encoding of polypeptides with biological display systems enables the facile generation and screening of very large combinatorial libraries of molecules. By post-translationally modifying the encoded polypeptides, chemically and structurally mor ...
Effective analyte delivery is essential to achieve rapid and sensitive biodetection systems. In this article, we present an actively controlled fluidic system integrated with a suspended plasmonic nanohole sensor to achieve superior analyte delivery effici ...
Bicyclic peptides generated through directed evolution by using phage display offer an attractive ligand format for the development of therapeutics. Being nearly 100-fold smaller than antibodies, they promise advantages such as access to chemical synthesis ...
The identification of all protein targets of a small molecule drug, i.e. target deconvolution, provides the basis for understanding its beneficial or deleterious actions. Target deconvolution remains a major and often problematic task within the biotechnol ...
