Accelerating drug discovery

A newly developed ‘nanocalorimeter’ will enable researchers to measure the level and nature of chemical activity of pharmaceutical prototypes with unparalleled accuracy and speed.

The Scripps-PARC Institute for Advanced Biomedical Sciences, a joint venture of the Palo Alto Research Center (PARC) and The Scripps Research Institute (TSRI), have announced a technology they claim is capable of significantly improving drug discovery.

The newly developed ‘nanocalorimeter’ will enable researchers to measure the level and nature of chemical activity of pharmaceutical prototypes with unparalleled accuracy and speed. This improved clarity will have substantial impact on the cost of drug development by drastically reducing the level of effort required in new drug design.

These advancements will allow pharmaceutical companies to reduce the time to market of drug treatments while reducing research and development investments that can inhibit wide-scale consumer access.

‘The enthalpy array technology developed by the scientists of the Scripps-PARC Institute has the potential to materially alter the course of drug discovery by addressing the principal hindrance to this empirical process: a comprehensive understanding of the drug candidate reactivity,’ said Scripps Research President Richard A. Lerner, MD.

‘This technology allows for the high-volume production of disposable arrays that will drive wide-scale adoption in many applications,’ he added.

Molecular thermodynamics is a key of drug discovery, as it is the best way to understand the way drug candidates bind with drug targets and can provide key indications of a compound’s effectiveness.

However, devising low-cost methods to quickly and accurately characterize these reactions has proven difficult. Traditional calorimetric methods have throughput levels that limit their use to only highly special cases in drug and proteomic research. Researchers have developed alternate assays that offer the rapid analysis of molecular interactions but these rely upon labeling or immobilisation, methods which are time consuming to develop, can compromise test results and provide only a limited picture of the chemical activity. Some of these available measurement technologies also require large quantities of costly compound samples.

The Scripps-PARC Institute’s enthalpy array technology is a low-cost solution that offers requisite levels of precision and throughput. The calorimetric approach precludes the use of binding agents that can degrade the quality of test results and delay discovery.

Current calorimetric tools use up to 1000 times the quantity of sample compounds required by the enthalpy array. Using 250 nanolitre droplets of a test compound on 96-detector arrays, the nanocalorimeter enables researchers to characterise larger numbers of unique samples in a shorter amount of time than traditional methods while reducing material costs.

By enabling more complete characterization of prototype compound interactions with drug targets, the technology will improve researchers’ ability to hone the most effective treatments.

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