HIGH THROUGHPUT SCREENING HELPING THE DRUG DISCOVERY

by Selleckchem | Oct 14 2012

HIGH THROUGHPUT SCREENING: INTRODUCTION:

In pharmaceutical industries different techniques are important and used for the novel drug discovery. Among these techniques the most effective one in this area is high throughput chemical screening. It is also named as HTS assays or high throughput assays which are being used for the biological, pharmacological assessment or the assessment of biochemical activities of a large number of drugs by the help of the latest automatic technology [1]. Such technology is not only helpful in discovery of appropriate receptors, enzymes, ligands for different ion channels and the other pharmacologically important targets but also used in the extensive studies of various desired biochemical or cellular pathways by the aid of unknown and novel chemical agents. Regarding this an important example is of the screening of kinase inhibitor library for screening that is much easier than various other traditional methodologies [2]. Reviews of high throughput screening are an efficient source of acknowledging the importance of HTS. These reviews reveal the speed and accuracy of high throughput screening in the pharmaceutical industries in improving the scientific approaches and business structures [3].

HIGH THROUGHPUT SCREENING: IMPORTANCE
For the best and effective results of high throughput screening a better way is the use of this technique with its application of counter screens for a better and an immensely developed system. The properly handled high throughput assays can remarkably decrease the ambiguity and uncertainty of the obtained results. It is also good and efficient in strategic detection of false positive and false negative results [4]. The vast expanding market of HTS is now proving itself to be effective and efficient in handling the obscurities of the drug’s pharmacokinetics and the drug’s metabolism as compared to the previously used methods. High throughput screening assay is actually the most initial and the most critical step in the discovery of a novel drug which determines the potency of particular chemical agent against the particular disease [5]. Now by the help of genomic HTS assays, the researchers aim to screen a large number of different small chemical molecules and compounds to identify the possible hits by a accurate and speedy method.

PROGRESS IN HIGH THROUGHPUT ASSAYS:
With the help of high throughput screening assays, now it is possible to determine the potency of any chemical compound and also to observe the absorption potential of a particular chemical agent along with its chemical properties to cross the blood brain barrier. An efficient way to analyze its pharmacodynamics and pharmacokinetics in more details is the Computer modeling. However, by the help of latest instruments the researchers are now able to make a much faster HTS assay which is better than before and also better in comparison to traditional methods [6]. Now a very good number of scientists are emphasizing on implementation of the statistical methodology by robust replicates analysis in the primary screening steps and this technique can hit the targets in a much better way [7]. Furthermore, the accuracy of HTS assays can also be increased by its application of computational virtual high-throughput screening of commercial compound libraries in order to target the hits by the agreement acquired by both high-throughput screening and virtual high-throughput screening [8].

REFERENCES:
1. Hertzberga RP, P.A., High-throughput screening: new technology for the 21st century. Current Opinion in Chemical Biology, 2000.
2. Slon-Usakiewicz, J., Global Kinase Screening. Applications of Frontal Affinity Chromatography Coupled to Mass Spectrometry in Drug Discovery. Anal. Chem., 2005.
3. Sundberg SA, e.a., High-throughput and ultra-high-throughput screening: solution- and cell-based approaches. Current Opinion in Biotechnology, 2000.
4. White, R., High-Throughput Screening in Drug Metabolism and Pharmacokinetic Support of Drug Discovery. Annual Review of Pharmacology and Toxicology, 2000.
5. Broach JR, T.J., High-throughput screening for drug discovery. Nature Biotechnology, 1996.
6. Parker GJ, e.a., Development of High Throughput Screening Assays Using Fluorescence Polarization: Nuclear Receptor-Ligand-Binding and Kinase/Phosphatase Assays. J Biomol Screen, 2000
7. Malo N, e.a., Statistical practice in high-throughput screening data analysis. Nature Biotechnology, 2006.
8. Jenkins JL, e.a., Virtual screening to enrich hit lists from high-throughput screening: A case study on small-molecule inhibitors of angiogenin. Proteins: Structure, Function, and Bioinformatics, 2003.