New 3-D Control Offers Innovative Drug Discovery Route
A collaborative team of scientists at Yale University has demonstrated a new and highly versatile approach for quickly assembling drug-like compounds.
Reported in the latest publication of Science (the journal of the American Association for the Advancement of Science) their work has essentially identified a broad new pathway to drug discovery and medical treatment.
Lead researcher Jonathan Ellman, a professor of pharmacology at Yale University, explains that drug molecules interact with their targets, such as proteins or enzymes, by attaching to them in a way that neutralises the target's undesirable effects in the body. The focus of this particular research effort has been on piperidines, an organic compound class widely used in the pharma industry, which is a key synthetic target for drug discovery and development.
These compounds form the scaffold or core structure that supports molecular fragments and bind to a drug's targets. By applying regiochemistry the investigators were able to identify options for creating highly substituted piperidine derivatives. Consequently they have been able to highlight a way that different piperidine derivatives can be generated by varying the strength of acid.
As a direct result of confirming this novel approach, scientists now have far more power over the three-dimensional structure of a key class of molecular compounds. Ellman says that this means it will be easier for their manipulation, ultimately allowing the drug molecules which fit their targets in the right way to be developed: "Now we've got a lot more control over the shape and orientation of this class of drug compounds, and this essentially gives us greater flexibility in creating effective drugs”.
Funding support from the National Institutes of Health, the US Department of Energy and the Swiss National Science Foundation has allowed the researchers to easily make new piperidines. This has much importance for the pharma industry because the process that is used for the development of many drugs has subsequently been sped up and made simpler.
Drug developers are allowed to use the outcomes from this study straightaway because the research is being published without any patent constraints making the findings highly relevant to anyone involved in this sector. From Ellman’s perspective allowing open access to this new knowledge means that potentially important drugs can be identified and developed: "I believe that this is the most effective approach for rapidly translating this work into new drugs”.
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