AstraZeneca, Pfizer, Astex Pharmaceuticals discuss identification of lead inhibitors and structural optimisation of protein ligands with therapeutic efficacy

LONDON, UNITED KINGDOM, November 20, 2015 /EINPresswire.com/ -- SMi Group Reports: AstraZeneca,Pfizer,Astex Pharmaceuticals will discuss identification of lead inhibitors and structural optimisation of protein ligands with therapeutic efficacy

“Activity-based protein profiling (ABPP) has emerged as a powerful chemoproteomic tool
to characterize the selectivity of enzyme inhibitors on a global scale”. (Source: ACS Med. Chem. Lett. 2011, 43,61,62)

With successful examples of covalent inhibition of the fatty acid amide hydrolase (FAAH) presenting a promising strategy in the treatment of pain and inflammatory disorders, Doug Johnson, Pfizer et al have previously reported a class of piperidine urea FAAH inhibitors and gone on to develop their clinical candidate PF-04457845. (Source: ACS Med. Chem. Lett. 2011, 2, 91–96)

Doug Johnson, Research Fellow at Pfizer will be giving a keynote address at the Advances and Progress in Drug Design conference: Reviving covalent drug design: Discovery of PF-04457845, an irreversible FAAH inhibitor with exquisite selectivity. He will take a closer look at the unique benefits of small molecule covalent drug candidates and activity-based protein profiling, as well as clickable probes to evaluate selectivity of covalent binding.

Furthermore, Gianni Chessari, Director at Astex Pharmaceuticals will give an exclusive session on small molecules in drug design, answering the hot questions – are all protein-fragment interactions favourable? Is the bound conformation a low energy geometry?

Tove Tjogren, Associate Director at AstraZeneca will will take the stage with discovering structure-based drug design within the lipid bilayer. This will take a look at the role of solvent within the protein-lipid interface and ligand efficiency metrics in the context of membrane embedded binding sites.

Other speakers include: Gregg Seigal, Chief Executive Officer, ZoBio; Howard Feldman, Principal Scientist, Chemical Computing Group; Herman van Vlijmen, Senior Director, Janssen; Manuel Francisco Molina-Martin, Research Scientist, Eli Lilly; Jordi Munoz Muriedas, Investigator, GSK and many more.

The Advances and Progress in Drug Design conference program will deliver interactive presentations, case studies and keynote addresses that will enable attendees to understand key developments in protein-based drug design, optimise biophysical tools for compound validation and high resolution screening ad learn unique benefits of small molecule covalent drug design.

Confirmed Sponsors for 2016: Chemical Computing Group, Openeye Scientific Software, NanoTemper Technologies

Those who are interested in attending are advised to register before 30th November to secure the place at the conference and save £200.

For the full event agenda/ to register please visit: www.drug-design.co.uk/ein

For sponsorship opportunities please contact Alia Malick on +44 (0) 20 7827 6168 or email: amalick@smi-online.co.uk

For media enquiries please contact Anna Serazetdinova on +44 (0) 20 7827 6180 or email aserazetdinova@smi-online.co.uk

To register for Advances and Progress in Drug Design please contact Matthew Apps on +44 (0) 207 827 6093 or email mapps@smi-online.co.uk

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About SMi Group:
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Matthew Apps
SMi Group Ltd
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