Dr Stephen K Burley, CSO and SVP of Research at SGX Pharmaceuticals, Inc to give Keynote presentation at 3rd Modern Drug Discovery and Development Summit

Released on: October 17, 2007, 9:14 am

Press Release Author: GTCbio

Industry: Pharmaceuticals

Press Release Summary: Dr. Stephen K. Burley, CSO and SVP of Research at SGX
Pharmaceuticals will give the Keynote presentation at GTCbio's Drug Design & Lead
Discovery conference - one of six tracks at the 3rd Modern Drug Discovery &
Development Summit on November 28-30, 2007 in San Francisco.

Press Release Body: MONROVIA, CA - Dr. Stephen K. Burley, Chief Scientific Officer
and Senior Vice-President Research at SGX Pharmaceuticals, Inc. located in San
Diego, CA will give the Keynote presentation at GTCbio's Drug Design & Lead
Discovery conference - one of six tracks at the 3rd Modern Drug Discovery &
Development Summit on November 28-30, 2007 at the Hyatt Regency San Francisco
Airport.

Dr. Burley's presentation will cover fragment-based discovery of selective, orally
bioavailable tyrosine kinase inhibitors for targeted treatment of human cancers with
examples from SGX's FASTT (Fragments of Active Structures) platform.

The fragment-based drug discovery platform utilizes high-throughput X-ray
crystallography for lead identification/optimization. The process exploits
crystallographic screening to detect, visualize and identify small ligands (MW
150-200) that are bound to the target protein. Each member of the FASTT
fragment/scaffold library was selected to be amenable to rapid chemical elaboration
at two or three points of chemical diversity using parallel organic synthesis.
Initial lead optimization involves using SGX's knowledge of the co-crystal structure
of the target-fragment complex and advanced computational chemistry tools to guide
synthesis of small focused linear (one-dimensional) libraries. These linearly
elaborated fragments/scaffolds are then evaluated with in vitro biochemical and
cellular assays and co-crystal structure determinations. Thereafter, optimal
variations at each point of chemical diversity are combined to synthesize focused
combinatorial (two- or three-dimensional) libraries that are again examined with
assays and crystallography. (The potential chemical diversity of the fully
elaborated FASTT fragment/scaffold library far exceeds 160 million compounds.)
Active compound series are prioritized for further medicinal chemistry and compound
development efforts using the results of in vitro and in vivo ADME and in vitro
toxicology studies. Successful applications of the FASTT fragment-based lead
discovery/optimization process will be presented for a portfolio of well validated
oncology targets.

The 3rd Modern Drug Discovery & Development Summit features over 150 speakers
participating in 6 concurrent conferences, 6 study sessions and 3 pre-conference
workshops. Tracks include Biological Therapeutics, Drug Delivery Technology,
Translational Medicine, Drug Design and Lead Optimization, Emerging Targets, and
Pharmaco - Kinetics, Dynamics, Genomics and Genetics. For more information, visit
www.gtcbio.com.


ABOUT GTCbio

GTCbio organizes conferences specifically for the biomedical and biopharmaceutical
industries. Our goal is to facilitate the exchange of biopharmaceutical and
biomedical intelligence between industry leaders, academic and government
organizations, and the financial community.

GTCbio is a subsidiary of Global Technology Community, LLC, a privately held company
founded in 2002.

Contact: GTCBIO (626) 256-6405, (626) 256-6460 fax, raniah@gtcbio.com


Web Site: http://www.gtcbio.com

Contact Details: GTCbio
434 W Foothill Blvd.
Monrovia, CA 91016
626)256-6405
raniah@gtcbio.com

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