The 5th Annual Modern Drug Discovery & Development summit was held in San Diego the 14th to the 16th of October, 2009. It was a good place to meet important project leaders involved in modern medicinal chemistry. More than 140 talks were organized into seven tracks to cover all the strategies for drug discovery and development.

“Biological Therapeutics” presented new achievements in antibody-based therapies, vaccine developments, protein applications and biologics delivery. “Advances in Stem Cell Discoveries” covered the status and future of stem cell research while the US government changed this year its policy concerning human embryonic stem cells. “Partnering, Licensing & Outsourcing” gave precious information about the ways to select the best partners for a good collaboration. “Toxicity & Drug Safety” was dedicated to PK / PD / TD markers and new techniques to assess toxicity. “Translational Medicine” was a diverse program to discover a selection of all the themes of the summit.

Among others, in the “Drug Desing & Lead Discovery” track, new dopamine transporter inhibitors identified using pharmacophore based design were presented by Istvan J. Enyedy from Biogen Idec. Andreas Kuglstatter, from Roche Palo Alto, described five strategies based on fragments to design new kinase inhibitors. Dramane Lainé discussed the COPD program of GlaxoSmithKline where quinuclidine series were identified as new long acting muscarinic antagonists. George Keresu from Gedeon Richter introduced the concept of “lead obesity” and the way to improve optimization using ligand efficacy and lipophylic efficacy. Finally a very chemical talk from Jie Jack Li described the generation of new potent MMP-13 inhibitors for the treatment of osteoarthritis at Bristol Myers Squibb.

Metalloproteases have also applications in cancer therapy like the MMP-14 new inhibitor series presented by Lili Huang from Dyax during the “Cancer Targets & Therapeutics” track. A first session was dedicated to novel oncology biomarkers. In session II, interesting chemical series were described like the new aminopyrrolidines Akt inhibitors from Pfizer discussed by Kevin Freeman-Cook and the thiazole urea AZD7762 from Astra Zeneca, presented by Susan Ashwell, an inhibitor of checkpoint kinase which is now in phase I clinical trials. The last session explored the possibilities to use RNA technologies for cancer therapy.