Arrive early to attend Protein Kinase Targets (June 23-25)

Don’t Miss

Pre-Conference Short Course: June 25th
Designing Kinase Inhibitors

Structure Based Drug Design of HIV-1 Reverse Transcriptase Inhibitors
Christopher Phillips, Ph.D., Senior Principal Scientist, Exploratory Medicinal Sciences, Pfizer Global Research and Development

From Virtual Screening to Clinic: Discovery of Cevoglitazar
T. R. Vedananda, Ph.D., Program Head, Diabetes & Metabolism, Novartis

The Discovery of OSI-906: A Novel, Potent, Orally Bioavailable Imidazopyrazine-Derived Insulin-like Growth Factor-I Receptor (IGF-1R) Inhibitor with Anti-Tumor Activity
Mark Mulvihill, Ph.D., Associate Director of Chemistry, Oncology, OSI Pharmaceuticals

Fragment based lead generation: An integrated approach applying NMR and BIAcore technology for fragment identification and evaluation
Stefan Geschwindner, Ph.D., Principal Scientist, GSC, AstraZeneca R&D Mölndal

Use of Mass Spectrometry to Help Drive the Design of a Drug Candidate from Inception to Development
Jennifer Nemeth, Ph.D., Principal Research Scientist, Protein Engineering, Centocor Research and Development

The Significance of Unconventional Hydrogen Bonds in Structure-Based Drug Design
Gergely Toth, Ph.D., Scientist, Computational Chemistry and Biology, Chemistry, Elan Pharmaceuticals

Structure-Based Drug Design (SBD) has been in use within the pharmaceutical industry for over twenty-five years. Given the multi-disciplinary nature of drug discovery and development, SBD can hardly be the unique success factor. However, SBD is playing an increasingly important role. SBD of compound properties are still developing and growing in acceptance. In this program, we wish to highlight some recent breakthroughs and successes using SBD, including the accompanying interest in ligand-based.

Recent breakthroughs and "unpublished work" will be discussed at CHI’s Eighth Annual Structure-Based Drug Design conference:

• Discoveries "leading to development candidates" that can be shown

• The "Med Chem" perspective- property optimization in parallel to SBD

  • Considerations of physicochemical compound properties

  • Considerations of in vitro versus in vivo pharmacological compound properties

• The computational or structural viewpoint

• Computational or structural methodology

• Ligand-Based Design

  • The diverse roles of water in ligand binding to targets

  • Ligand design including solvents

• Biophysical approaches

  • MS

  • SPR

  • X-ray Crystallography

  • NMR

  • Homology Models

  • Virtual Screening

  • QSAR

• Combination of the above

• How to cope with structural flexibility of the target

• How to cope with selectivity issues (e.g. kinases, GPCR’s ...)

• Novel targets and the validations of the targets

The program is still in development and final details will be posted soon. Your feedback, suggestions for new session topics, and referrals to new case studies, speakers, technologies and approaches are welcome and appreciated.

We look forward to seeing you on June 25-27, 2008 in Boston!

Sincerely,

Micah Lieberman
Conference Director
Cambridge Healthtech Institute