In one of my earlier blog, Dec., 28th 2008, ( FBDD- A New Approach Of Drug Discovery) I did mention about the use of a number of biophysical techniques as screening tools including high-throughput x-ray crystallography (the advantage of giving the best picture of how the fragment sits in the target) and when paired with NMR allows you to create a structure-based lead.
With different companies approaching this new route in different ways like :
- high-throughput x-ray crystallography
- NMR-fragment screening
- fluorescence polarization assay and many other interesting ways like Protien-Protein interactions etc., this field I think have important role to play.
While reading Science Daily (Online issue, Sept 21, 2009), I found this interesting (article ) and really innovative finding , which I want to share...
Preliminary studies by the researchers (Dr. Ken & Dr.Rakesh )have shown that the new mass spectrometry tool—known as MALDI-QqQMS (matrix-assisted laser desorption ionization-triple quadruple mass spectrometer)—provides a superior means of measuring the enzyme reactions critical to drug discovery at speeds comparable to currently available high-throughput screening systems at significantly lower costs. As per the claim by the researchers, Dr. Ken Greis, "If introduced broadly, the new generation mass spectrometry-based method the researchers are proposing could significantly reduce the cost of running drug compound screening assays while also saving drug development teams substantial time by improving the accuracy of data collected. As per the claim by these researchers the above mentioned methods are costly.
Dr. Ken Greis and Dr. Rakesh Rathore have developed a custom high-throughput screening method using a generalized platform. Unlike the commercially available systems that analyze byproducts and coupled reactions, their system directly measures and quantifies the substrate and the end product of the reaction. They say using mass spectrometry to measure the mass and quantity of the product gives researchers a direct measure of the assay and more reliable compounds to explore, eliminating the chances for molecular interference common with chemiluminescence and fluorescence-based systems. Its a remarkable achievement and hope in the near future we will have an automated system for commercial use with least expense. Best of luck. For More....
Dr. Ken Greis and Dr. Rakesh Rathore have developed a custom high-throughput screening method using a generalized platform. Unlike the commercially available systems that analyze byproducts and coupled reactions, their system directly measures and quantifies the substrate and the end product of the reaction. They say using mass spectrometry to measure the mass and quantity of the product gives researchers a direct measure of the assay and more reliable compounds to explore, eliminating the chances for molecular interference common with chemiluminescence and fluorescence-based systems. Its a remarkable achievement and hope in the near future we will have an automated system for commercial use with least expense. Best of luck. For More....
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