Drugs, usually long acting and metabolically stable molecules, might be the source of adverse effects triggered by complex drug interactions, anaphylaxis and drug-induced coagulopathy. To circumvent this growing drug safety issue, we herein investigate the opportunity offered by bio-orthogonal chemistry for in vivo drug neutralization. We design a small-molecule anticoagulant drug (Warfarin) co...

Small-molecule fluorescent probes have been widely used in target identification, but this method has many disadvantages. For example, the identified proteins are usually complex, and additional biochemical studies are needed to distinguish real targets from interference results. To address this problem, we propose a series of strategies for improving the efficiency of target identification. Fi...

The highly controversial force-induced cycloreversion of 1,2,3-triazole, its well-known retro-click reaction, is shown to be possible only for 1,5-substituted triazoles, but competes with rupture of an adjacent singlebond. We draw this conclusion from both static and dynamic calculations under external mechanical forces applied to unsubstituted and 1,4and 1,5-substituted triazoles. The JEDI (Ju...

Multi-functional supramolecular hydrogels have emerged as smart biomaterials for diverse biomedical applications. Here we report a multi-functional supramolecular hydrogel formed by the conjugate of the bioactive GRGDS peptide with biaryltetrazole that is the substrate of photo-click reaction. The hydrogel was used as a biocompatible matrix to encapsulate live cells for 3D culture. The presence...

The enzyme-directed synthesis is an emerging fragment-based lead discovery approach in which the biological target is able to assemble its own multidentate ligands from a pool of building blocks. Here, we report for the first time the use of the human acetylcholinesterase (AChE) as an enzyme for the design and synthesis of new potent heterodimeric huprine-based inhibitors. Both the specific cli...

Polysaccharides are complex but essential compounds utilized in many areas such as biomaterials, drug delivery, cosmetics, food chemistry or renewable energy. Modifications and functionalizations of such polymers are often necessary to achieve molecular structures of interest. In this area, the emergence of the “click” chemistry concept, and particularly the copper-catalyzed version of the Huis...

The memory load of assembling (Specifier)-Head-Complement(s) phrases in mono-clausal Subject-VerbObject sentences was assessed by employing the click-detection paradigm –a technique that has been shown to be sensitive to different cognitive loads within and between clauses in complex sentences. 60 pairs of Spanish sentences, containing a longer phrase in either the Subject or Object position we...

The use of flow chemistry techniques has flourished over the past decade, with the field expanding to include the use of copper flow reactors in bench-top organic synthesis in recent years. These reactors are available in a variety of forms and possess a number of advantages over their batch reaction counterparts, in terms of both safety and yield. This review will highlight the current researc...

Presently, the majority of reports deal with combining chemical reactions, in a stepwise fashion, to obtain well-defined polymers. In the future, chemists need to address new challenges such as increase in the range of available efficient reactions, developing libraries of compatible one-pot reactions, and the application of obtained materials in key industries. Indeed, the rising importance of...

We describe the use of iterative in situ click chemistry to design an Akt-specific branched peptide triligand that is a drop-in replacement for monoclonal antibodies in multiple biochemical assays. Each peptide module in the branched structure makes unique contributions to affinity and/or specificity resulting in a 200 nM affinity ligand that efficiently immunoprecipitates Akt from cancer cell ...