Combinatorial Chemistry & High Throughput Screening - Volume 9, Issue 8, 2006

Oligosaccharide processing enzymes such as glycosidases and glycosyltransferases are important classes of biocatalysts involved in synthesising specific oligosaccharide structures on proteins and lipids. These enzymes are known to be involved in a wide range of important biological processes, such as intestinal digestion, post-translational processing of glycoproteins, lysosomal catabolism of glycoconjugates and inter Read More

Combinatorial chemistry was shown to be an efficient tool for the preparation of new aroma-impact compounds. In this case, polyfunctional thiols were synthesized quickly using halide reagents or Bunte salt intermediates. They were separated by gas chromatography and then characterized using low resolution EI and CI mass spectrometry. The individual sensorial properties of the thiol products (i.e. odor and perception thres Read More

We report a robust method for the detection of hybridization events using a microarray-based assay on a nanoporous membrane platform. The technique is characterized by a hybridization time of only 1 hour and uses Cy5- labeled, 7-mer oligodeoxynucleotide probes modified with locked nucleic acid (LNA) nucleotides. We show that the volume of the DNA spotted onto a nanomembrane can be reduced to ∼4 nL with detec Read More

Gelatinase B/MMP-9 fulfills crucial regulator or effector functions in disease states and may be pharmacologically targeted by specific inhibitors. The characteristics of cleavages of a natural gelatinase B substrate were simulated and amino acids with zinc-ion chelating side-groups were employed to design a library of peptide-based inhibitors. Here, we extend previous findings of combinatorial chemical synthesis and subsequent lib Read More

In light of emerging interest in the relevance of c-Jun NH2-terminal protein kinase 3 (JNK3) as a promising drug target, we describe here an advanced non-radioactive immunosorbent JNK3 activity assay that is applicable for routine screening of small molecule ATP-competitive enzyme inhibitors. We modified and established a JNK3/ATF-2 protocol based on our previously described p38 MAPK method [1] for a substrateb Read More

The systematic evolution of ligands by exponential enrichment (SELEX) is a combinatorial oligonucleotide library- based in vitro selection approach in which DNA or RNA molecules are selected by their ability to bind their targets with high affinity and specificity, comparable to those of antibodies. Nucleic acids with high affinity for their targets have been selected against a wide variety of compounds, from small molecules, such as Read More

Cyclic ADP-ribose (cADPR) is an intracellular messenger that triggers the release of calcium ions from intracellular stores in a variety of cell types. The fluorometric cycling assay has become the preferred method for measuring cADPR due to its high level of sensitivity (in the sub-nanomolar range) and its use of commercially available reagents. Additionally, the assay is performed in multiwell plates, making it suitable for high Read More