NOVEL DRUGS AND HIGH THROUGHPUT SCREENING

by Selleckchem | Apr 09 2012

INTRODUCTION:
High throughput screening assay is well known technique in pharmaceutical industries and having fame due to its role in novel drug discoveries. This is also abbreviated as high throughput screening assay, by the help of this technique or assay a good number of compounds like drugs are assessed with reference to their biochemical, biological or pharmacological activities by the aid of new automatic technologies [1]. High throughput screening has not only proven to be effective in the field of new therapeutic agents like ligands for different receptors, enzyme proteins, ion channels and many other pharmaceutical targets, But this screening technique is also being used for profiling a cellular or biochemical pathway of interest for therapeutic targeting of this pathway by unknown compounds. The one of best example is screening libraries of kinases which are now much easier way as compared to old methods [2]. In order to understand the value of high throughput screening one should look at reviews of this technique where accuracy and speed are the main tools which have brought the improvement in scientific research and also in the business of pharmaceutical world [3].

SIGNIFICANCE OF HIGH THROUGHPUT SCREENING:
Selection and implementation is better criteria in high throughput screen along with the application of counter screens aids significantly in developing a better system. The uncertainty and ambiguity is decreased significantly by high throughput sequencing when handled properly as this technique is also very helpful with suitable strategy to analyze false negative and positive [4]. In past the newly discovered drug faced obscurities in its metabolism and pharmacokinetic screening which has been over come efficiently by high throughput screening. High throughput screening is always very critical during drug discovery as it is amongst initial hierarchy of the discovery when finding an appropriate molecule for a particular disease [5]. Researchers hope for screening a wide range of the chemical compounds from a chemical library in order to hit an accurate point at a very high rate by high throughput genomics.

NEW HIGH THROUGHPUT SCREENING APPROACHES:
With the help of high throughput screening many compounds are having now detailed descriptions because of which it is now possible to evaluate the ability of a particular chemical compound by its absorption potential along with the understanding of blood-brain barrier passing ability. The pharmacokinetics and pharmacodynamics are studied now in much greater details due to computer modeling. Aside from all old methods, scientists are now developing more advance high throughput assays with the help of latest instrumentations than ever [6] done in the past. It has been noted that many of the researchers are now interested in the statistical analysis in the process of high throughput screening as it uses many replicates in primary screening, hence it will help to specify the conditions [7]. High throughput screening accuracy can also be enhanced by applying computational based theoretical high throughput screening of compound libraries parallel to identify the exact hits by comparing theoretical high throughput screening with 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.