PEPTIDES & PROTEINS F3C N N H2N N HN
VertexPharmaceuticals PLK1 Ki=<3nM
neutral, antagonist or agonist properties.
Removing downstream bottlenecks Many process chemists and contracted CROs tasked with scaling up development candidates for their customers struggle to modify and adapt synthetic routes that have previously only been used to provide small amounts of material for early studies. This includes installing fundamental properties such as chirality. For example, HPLC may have been used to provide grams of material for early studies, but this technology may not be economically scaleable. With Enzacore structures, scale-up is significantly less
N
N H
N O
Fig 4. A recent example of a highly potent compound with peripheral Enzacore structure.
onerous, the biocatalytic steps necessary for ensuring the correct chirality having already been developed. It is well proven now that enzyme-based chemistry often provides the most cost-efficient and expedient synthesis of molecules from milligram to tonne manufacture, and Enzagen is very well versed in all aspects of the biocatalyst supply chain.
In conclusion
Drug discovery continues to ride the winds of change, but as new leads and drug candidates come through the different pipelines it is certainly consistent that complexity of the molecules is on the rise. Chirality will continue to feature strongly and different technologies are rising to the challenge and maturing to enable delivery of these compounds. The marriage of biocatalysis and molecular modelling has the ability to expedite the passage of molecules emerging from computational design and hasten time to actual scaleable reality. It is this paradigm shift to the acceptance of different
and perhaps unusual marriages of technology that will reap rewards for the end users into the foreseeable future.
Further information
Dr Bill Hamilton Prosarix Ltd Newton Hall Town Street Newton Cambridge CB22 7ZE United Kingdom Tel: +44 1223 870400
Internet links: Email:
bill.hamilton@prosarix.com Web:
www.prosarix.com
Dr Steve Taylor Enzagen Ltd Newton Hall Town Street Newton Cambridge CB22 7ZE United Kingdom Tel: +44 1638 780251
Internet links: Email:
sjctaylor@enzagen.com
Web:
www.enzagen.com
The Peptide Conference 2012 Cambridge, UK, April 17-18, 2012
Attendee registration is now open for The Peptide Conference 2012 organised by avakado media and taking place from April 17-18, 2012 at Chilford Hall Conference Centre, Cambridge, UK.
Presentations cover the use of peptides as analytical tools and diagnostics; therapeutic peptides; synthesis and manufacturing technologies; and peptide drug delivery.
Delegates who will benefit from attending the conference are senior R&D scientists, managers and decision makers from pharmaceutical and biotechnology companies looking to develop new peptide analytics, therapeutics and diagnostics and efficiently and economically manufacture new peptide products.
The conference also features a tabletop exhibition of companies offering peptide R&D and manufacturing technologies and services.
For further information contact: Tom Mulligan
Conference Director avakado media Tel: +44 (0)1403 220755 Email:
tom@avakado.eu Web:
www.avakado.eu
34 sp2 November/December 2011
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