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Structure-Guided Drug Discovery: Fragment-Based Lead Identification and Optimization

Speaker:
Stephen K. Burley, MD, DPhil, FRSC
Chief Scientific Officer
and Senior Vice President, Research
Structural GenomiX, Inc.

Moderator
John Munroe, Ph.D.
Director, Discovery Chemistry Research & Technologies.
Eli Lilly & Co.

Registration for the live event is now closed. However, if you are interested in viewing an online recording which contains the entire presentation, including audio, you may purchase this for $169 USD. Please click the button below and you will be emailed information on how to access the recorded event. MAC USERS: Unfortunately at this time the recordings cannot be viewed on the MAC OS.

This live webcast addressed real-time access to structural information for kinase and protease targets can shorten the timeline to produce potent, selective drug candidates.

Real-time access to structural information at the atomic level and advanced computational tools can enable significant advances toward the discovery of novel small molecule inhibitors of pharmaceutical targets that are not encumbered by existing drug patents. One approach that exploits real-time access to structural information applies integrated processes that combine high-throughput x-ray crystallography with fragment-based methods, for parallel lead identification and lead optimization.

This strategy utilizes crystallographic screening of synthetically-enabled fragment libraries to provide useful starting points for fragment lead optimization, via design and synthesis of affinity-enhancing chemical variations of the fragment hit with the aid of high-throughput organic chemistry and advanced computational chemistry tools. This integrated approach will be discussed using examples drawn from two pharmaceutically important target classes: kinases and proteases.

The 1½–hour presentation addressed:

  • Crystallographic screening methods to identify synthesis-amenable complexes of target and lead compounds (latter, MS 150-200)
  • Computational-chemistry applications to guide high-throughput organic synthesis
  • Evaluation of focused, one-dimensional libraries through biochemical assays and co-crystallography<
  • Methods to optimize variations at points of chemical diversity, to access significantly higher chemical-shape diversity than with conventional HTS
  • Examination of 2-D and 3-D libraries through crystallography, cellular assays, and ADMET

An extensive Q&A session followed the presentation, with worldwide participation

Be Sure to Participate in this Virtual Seminar on Structure-Guided Drug Discovery: Fragment-Based Lead Identification and Optimization. You will be able to attend this real-time tutorial from anywhere that you have an Internet connection…from your office or from your conference room.

One Low Registration Fee of $149 entitled you to a “site” registration, which enables you to invite your colleagues and members of your staff to participate, whether gathered around a computer or in a conference room with speakerphone and screen.

It Couldn’t Be Easier! You’ll view the presentation over your Web browser. On a separate telephone line (which you can put on speakerphone), you will hear the audio and be able to ask questions of the presenter. You can also submit questions from your keyboard. Collateral material will be sent to you electronically after the seminar.

Time Well Spent! No travel, no time away. From your office or conference room, this hour-and-a-half seminar will provide you with an authoritative presentation that includes ample time for your questions and discussion. Registrations will be limited to ensure interactive participation

Presented byGenetic Engineering News