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Novasite Pharmaceuticals Awarded $3.4 Million NIH Grant to Screen Receptor Families in Parallel for Allosteric Modulators
Tuesday November 16, 12:45 pm ET
SAN DIEGO--(BUSINESS WIRE)--Nov. 16, 2004--Novasite Pharmaceuticals, Inc. (Novasite), today announced that it has received a Bioengineering grant from the National Institutes of Health (NIH) totaling $3,365,000 for a period of 4 years. The award supports scale-up of Novasite's proprietary Single Cell Screening technology for parallel screening of more than 100 G-Protein Coupled Receptors (GPCRs), an important family of drug targets that is responsible for approximately 40% of drug sales. Novasite's platform is uniquely capable of performing functional screens for allosteric modulators, a subclass of GPCR drugs with a novel and potentially safer mechanism of action.
"This substantial NIH grant will enable Novasite to scale up our parallel screening efforts from thirty to more than one hundred GPCR targets simultaneously. Parallel screening enables us to screen receptor families and control cells at the same time under identical conditions, dramatically reducing the high percentage of false positives typical of standard screening methods. Parallel screening also empowers our Single Cell Structure-Function drug discovery approach by facilitating more efficient screening of hundreds of receptor variants instead of conventional methods which screen against one receptor at a time," said John Ransom, Ph.D., Vice President of Biology and the Principal Investigator of this grant. "Novasite's proprietary platform is uniquely capable of detecting allosteric modulators, because it can reliably measure subtle variations in the signal induced by the natural ligand."
"Allosteric modulators represent a promising, novel class of drugs within the GPCR family, combining a safer mechanism of action with the most significant family of drug targets," commented Juan Ballesteros, Ph.D., Chief Scientific Officer of Novasite. "Our Single Cell Structure-Function platform is uniquely positioned to lead the discovery of this novel class of GPCR drugs."
Allosteric modulators are drugs that modulate the response of the natural ligand by binding at a regulatory site that is different from the normal binding site of the receptor. They represent a safer mechanism of action because instead of directly inducing an effect they modulate the effect of the body's own ligands. Their localized site of action and limited maximal effect may prevent side effects, overdose, tolerance, abuse and dependence.
Novasite Pharmaceuticals
Novasite Pharmaceuticals has developed an integrated "Single Cell Structure-Function" approach to enable the discovery of allosteric modulators and difficult agonist drugs targeting G-Protein Coupled Receptors ("GPCRs"). Allosteric modulation is a novel and safer mechanism of action for GPCR drugs. This novel high-growth market has become a major focus for pharmaceutical companies because it combines the best mechanism of action of a drug with the most important family of drug targets, GPCRs. Novasite's proprietary approach is uniquely capable of solving the key technical challenges in discovering GPCR Allosteric Modulators; Single Cell Screening enables functional detection of these effects, and the Structure-Function approach provides structural information to guide medicinal chemistry. Furthermore, Novasite's breakthrough crystallography approach may enable elucidation of the complete 3D structures of these receptors. For more information, please visit www.Novasite.com.
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Contact:
Novasite Pharmaceuticals
Kathryn Rucker, 858-875-8582
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fun!!, love this sort of stuff |
