Combinatorial Chemistry & High Throughput Screening - Volume 14, Issue 8, 2011

A fundamental challenge in bioscience research is to quantify changes in the concentration of key signaling molecules within the context of biologically relevant cellular model systems. Cell-based assays represent a useful midpoint between whole animals and purified molecules for understanding complex biological processes in a statistically valid way. In particular, they enable a reductionist approach to understandi Read More

The luminescent reporter gene assay (LRGA) is arguably the most prominent type of reporter gene assay used in biomolecular and pharmaceutical development laboratories. Part of this popularity is due to the high signal associated with luciferases, the foundation of this technology. This feature makes them ideally suited for high throughput screening applications where potentially millions of chemical compounds can be analyzed Read More

ADME-Tox testing examines the effects of an organism, tissue or cell on a compound, as well as the effects that the compound has on an organism, tissue or cell, and has gained in importance in the overall drug discovery process over the past twenty years. This is due to the rising percentage of drug candidate attrition in the 1990s and early 2000s due to adverse ADME/Tox profiles. The increased importance placed upon ADME/T Read More

Several assay technologies have been successfully adapted and used in HTS to screen for protein kinase inhibitors; however, emerging comparative analysis studies report very low hit overlap between the different technologies, which challenges the working assumption that hit identification is not dependent on the assay method of choice. To help address this issue, we performed two screens on the cancer targ Read More

Whole-animal studies have been the mainstay of toxicity testing for decades. These approaches are too expensive and laborious to effectively characterize all of the chemicals currently in commercial use. In addition, there are social and ethical pressures to reduce, refine and replace animal testing in toxicology. The National Research Council (NRC) has outlined a new strategy to transition from animal-based tests to hi Read More

Angiogenesis is a promising area of research that targets key therapeutic areas like cancer; wound healing, inflammatory diseases, etc. There is an increasing demand for screening of potential angiogenic and anti-angiogenic agents using sensitive, robust cell-based assays. We have developed a reporter vector containing cis-acting elements that respond to growth factors/angiogenic ligands for use in a cell-based luciferase report Read More

Dr. Watson has a B.S. in Genetics and Cell Biology from the University of Minnesota, an M.S. in Bacteriology; and a Ph.D. in Biomolecular Chemistry from the University of Wisconsin. After a clinical postdoctoral fellowship in Clinical Chemistry and Molecular Diagnostics he became Director of Molecular Diagnostics at Epicentre Technologies where he led R&D and Marketing efforts for their clinical research products. Subsequent Read More

Cell surfaces, especially mammalian cell surfaces, are heavily coated with complex poly- and oligosaccharides, and these glycans have been implicated in many functions, such as cell-to-cell communication, host-pathogen interactions and cell matrix interactions. Not surprisingly then, the aberrations of glycosylation are usually indicative of the onset of specific diseases, such as cancer. Therefore, glycans are expected to s Read More

The application of Isodon species in Chinese folk medicine has a long histroy, especially the ones called ‘Xihuangcao’ in Chinese. ‘Xihuangcao’ has been successfully applied to treat acute hepatitis, cholecystitis, enteritis, dysentery and trauma. The original species of ‘Xihuangcao’ is Isodon lophanthoides (Buch.-Ham.ex D.Don). However, there are five sources of Chinese medicinal herb ‘Xihuangcao’ due to their similar morp Read More

β-Fructofuranosidases can divert their hydrolytic activity towards transglycosylation for the synthesis of high value-added products, including prebiotic fructooligosaccharides (FOS). A directed evolution strategy has been employed to enhance the transferase rate of the β-fructofuranosidase (SoINV) from the Schwanniomyces occidentalis yeast for the production of β-(2→6)-linked FOS. To screen for transfer Read More

The section on patent review will be focused in the areas of interest to the readers of CCHTS. The search was conducted using the following key words: combinatorial chemistry, high throughput screening, drug repurposing, chemical library, high content screening, drug discovery and natural products. All patents highlighted here are identified by the patent number issued either by the World Intellectual Property Organization o Read More