Combinatorial Chemistry & High Throughput Screening - Volume 11, Issue 1, 2008

A high throughput screening assay for the identification of ligands to pharmacologically significant receptors was developed based on magnetic particles containing immobilized receptors followed by liquid chromatography-mass spectrometry (LC-MS). This assay is suitable for the screening of complex mixtures such as botanical extracts. For proofof- principle, estrogen receptor-α (ER-α) and ER-β were immobilized on magnet Read More

The cure rates in cancer chemotherapy are affected by the development of drug resistance and severe side effects. Due to these limitations, there is an urgent need for improved therapeutics. Bioactive compounds from medicinal plants represent a valuable resource for novel anticancer drugs. To gain a systematic approach, we established a library of 531 cytotoxic natural products derived from traditional Chinese medicine. Cell Read More

African trypanosomes are the causative agent of sleeping sickness. The therapeutics used to control and treat the disease are very ineffective and thus, the development of improved drugs is urgently needed. Recently, new strategies for the design of novel trypanocidals have been put forward. Among them are techniques that rely on parasite-specific RNA aptamers. One approach involves the aptamer-directed transport of lytic Read More

We have developed a miniaturized and multiplexed solution assay for the measurement of protease activity in complex samples. This technology can accelerate research in functional proteomics and enable biologists to carry out multiplexed protease inhibitor screens on a large scale. The assay readout is based on Illumina's universal Sentrix® BeadArrays. The peptide sequences that serve as protease substrates are conju Read More

The primary literature concerning the combinatorial synthesis of organophosphorus compounds is reviewed and discussed. The subject matter is divided into three main sections describing the solid phase, solution phase and solvent- free synthesis of phosphorus containing organic molecules. The review covers the synthesis of compounds in which the final products contain phosphorus-carbon bonds, primarily phosphonates, p Read More

Recently, significant progress has been made towards understanding the pathogenesis of cancer from the molecular standpoint. To this end, a growing number of approaches are being exploited for the identification and validation of new therapeutic targets suitable for potent and specific intervention. The type 1 insulin-like growth factor receptor (IGF-1R) system has recently become the focus of major attention in the aren Read More

Cell replacement therapy of severe degenerative diseases such as diabetes, myocardial infarction and Parkinson's disease through transplantation of somatic cells generated from embryonic stem (ES) cells is currently receiving considerable attention for the therapeutic applications. ES cells harvested from the inner cell mass (ICM) of the early embryo, can proliferate indefinitely in vitro while retaining the ability to differentiat Read More