Chip Based Method For Drug Development

The drug development often relies on high throughput cell basing screening of large compound libraries. In spite of increasing demand, the number of newly developed drugs decreased continuously in the past decades.

However, the lack of miniaturized and parallelized methodologies for high-throughput chemical synthesis in the liquid phase and incompatibility of synthesis of bioactive compounds and screening for their biological effect have led to a strict separation of these steps so far. The search for new active substances, their production, characterization, and screening for biological effectiveness are very complex and costly.

Screening on a single chip

One of the reasons is that all three steps have been carrying out separately so far; This makes the process expensive and inefficient. For this reason, we have developed a platform that combines synthesis of compound libraries with biological high throughput screening on a single chip.

This so called chemBIOS platform is compatible with both organic solvents for synthesis and aqueous solutions for biological screenings. “We use the chemBIOS platform to perform 75 parallel three-component reactions for synthesis of a library of lipids, i.e. fats, followed by characterization using mass spectroscopy, on chip formation of lipoplexes, and biological cell screening.

Cell screening

The entire process from library synthesis to cell screening takes only three days and about 1 ml of total solution, demonstrating the potential of the chemBIOS technology to increase efficiency and accelerate screenings and drug development.

All compounds are producing, isolating, and characterizing separately. Then, biologists analyze the molecule library for biological activity. Highly active compounds, so-called hits, are returned to chemistry. Based on this pre-selection, chemists synthesize further variations of these compounds. These secondary molecule libraries then contain optimized compounds.

This process is time consuming and requires a large range of materials and solvents. This makes development more expensive and slower and also limits the number of substances screened to a feasible number.