The characterization of agents that inhibit cell proliferation and division is particularly important for drug discovery research. Both events can be analyzed using HCS approaches by multiplexing cell cycle-specific cellular targets. One technique is EdU staining, which detects the S-phase of the cell cycle through incorporation of the nucleoside analog Uridine into newly synthesized DNA strands. Furthermore, there are well validated protein markers available that are associated with certain cell cycle phases. View PDF

Cytotoxicity is a very complex process affecting multiple pathways and is not manifested by determining one morphological parameter. However, the ability to measure early indicators of toxicity is an essential part of drug discovery. Cell-based High Content Applications are a powerful tool for determining several events in cytotoxicity simultaneously. We describe a rapid and flexible dye-based high content cytotoxicity assay performed with the widely-used HepG2 (human hepatocellular carcinoma) cells. View PDF

One of the most important tasks in anticancer treatment is the inhibition of cell proliferation by interruption of the cell cycle. As the cell cycle is subdivided into the four phases G1-, S-, G2- and M-phase, there are diverse targets for arresting cells either during DNA replication in S-phase or during division in mitosis. Several cytoplasmic proteins like the cyclines have been identified to be proprietary in cell cycle control whereas Cyclin B1 in particular is essential for initiation of mitosis. View PDF

Apoptosis – the genetically coded program leading to the self-destruction of a cell – can be induced via two main pathways, the death receptor-mediated pathway, and the mitochondrial pathway. Induction of either finally results in the activation of caspases, a class of intracellular cytokine proteases which are considered to be the central components of the apoptotic response. By breaking down key cellular components that are required for maintaining normal cellular functions caspases are responsible for executing morphological and biochemical consequences directly or indirectly attributed to apoptosis. View PDF

G-protein coupled receptors (GPCRs) are an attractive drug target for several clinically relevant disorders. This is primarily due to their membrane location, ubiquitous expression and critical involvement in many mammalian physiological systems. While several assays targeted at downstream GPCR signalling events have allowed characterization of this receptor superfamily, there are few non-invasive techniques that allow analysis of the receptor-ligand interaction at the cellular level. View PDF