High Throughput Screening for High speed Drug Discovery

Automisation of the labaratories is a multi-disciplinary strategy to research, develop, optimize and capitalize on technologies in the laboratory that enable new and improved processes. Due to the advancement in the laboratories techniques the ease of performing researches and experiments augmented day by day. Laboratory robotics is another most widely known application of laboratory automation technology. The field of laboratory automation comprises many different automated laboratory instruments, devices, software algorithms, and methodologies used to enable, expedite and increase the efficiency and effectiveness of scientific research in laboratories.Laboratory automation professionals are

• Academic
• Commercial
• Government researchers
• Scientists
• Engineers

These persons conduct research and develop new technologies to increase productivity, elevate experimental data quality, reduce lab process cycle times, or enable experimentation that otherwise would be impossible.

Today's laboratories require the various applications of technology to achieve timely progress and to be remain competitive. Laboratories devoted to activities such as High-Throughput Screening, Combinatorial Chemistry, Automated clinical and analytical testing, diagnostics, large scale bio-repositories, and many others, would not exist without advancements in laboratory automation.

Fig: Steps involved in Drug Development research 

Discovery of the new Lead compounds for Novel therapeutic targets is a multi-step process involving:

·        Drug design

·        Synthesis

·        Pharmacological screening

As the first step towards the drug development the biological targets needs to be identified.

In the next step the potential compounds are screened against the identified target.

Conventionally this has been slow and tedious manual process requiring huge investment of manpower, time and money. Depending upon the steps involve in the screening protocol, like centrifugation, phase extraction, filtration, precipitation and subsequent signal amplification and detection. The evaluation of the few hundred compounds might take weeks to months. Many more years elapse in trying to understand the molecular mechanism and for evaluating the kinetics and toxicity, before a lead compound is generated for investigation in Clinical Studies consequently; the conventional drug discovery program has been termed a Low Throughput Screening (L.T.S.).

Fig: Screening of Unknown Active Molecule

The last two decades have seen innovations in the technology that have helped to evolve LTS into an  automated, microprocessor controlled robotic process called “High Throughput Screening (H.T.S.)”. This quantitative leap in the drug discovery paradigm has been achieved via a synergy of chemistry, biology, engineering, and informatics. HTS has helped to speed up LTS and now over 50,000-100,000 compounds can be scanned per week, against the validated biological target.Further advancements are making it possible to screen 10,000-100,000 compounds within 24 hrs. time and called as Ultra High Throughput Screening (uHTS).

High Throughput Synthesis of large number of test compounds in a lesser time is also a reality now. This is achieved by combinatorial chemistry using parallel synthesis technology. A similar strategy has also been adopted in studies towards molecular mechanisms of drug action, absorption, metabolism, and toxicity studies to decrease the time spent in preclinical studies in the drug development program. Thus, valuable compounds can now be selected rapidly from a large number of samples with minimal human and cost involvement.

In industry, high-throughput chemical screens typically entail purifying a specific protein target, then testing the company's compound library to identify hits that change that protein's activity. The protein targets themselves are chosen on the basis of biological activity, perceived 'druggability', and the company's existing intellectual property covering particular drugs and targets.

Fig: Screening and Data Processing steps of RNAi documentation

It is strongly believe that high throughput screening (HTS) technology needs to play an increasing and major role in academic research which enables academic researchers to identify biological probes and to provide leads for drug discovery aimed at orphan diseases.

The goal of this work is to get the science back into the hands of the scientists by providing some simplified solutions to some difficult problems in High Throughput Screening (HTS) analysis. Solutions that avoid the added complexity, reduced ease of use and hiding of functionality that can make n-tiered solutions frustrating to work with.

Fig: Steps and the Technology involved in the High Throughput Screening Analysis.