2013 Archived Content

Fourth Annual


Small Molecule Approaches

April 16-17, 2013

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7:45 am Continental Breakfast Breakout Discussions

In this interactive session, several topics will be offered for discussions and delegates are invited to choose a topic of interest and join the moderated discussion at hand. In this informal setting, participants are encouraged to share examples from their work, vet ideas with peers and be part of a group problem-solving endeavor. We emphasize that this is an informal exchange amongst scientists and is not meant to be, in any way, a product promoting session.


Topic: Kinase Inhibitor Design

Moderator: William Pitts, Ph.D., Group Leader, Medicinal Chemistry, Bristol Myers Squibb and Co.

  • Allosteric Approaches
  • Structural Approaches
  • Selectivity/toxicity Issues

Topic: GPCRs in Inflammation

  • Which GPCRs are showing the most promise
  • Screening and assay considerations
  • Selectivity issues

Topic: Covalent Drug Design

Moderator: C. Eric Schwartz, Ph.D., Senior Director, Chemistry, Celgene Avilomics Research

  • What’s the difference between a targeted covalent inhibitor and a reactive metabolite?
  • Why aren’t covalent modifiers infinitely potent?
  • Approaches to achieve selectivity?

Topic: Macrocyclics as Inflammation Drug Candidates

Moderator: Jan Hoflack, Ph.D., Head, Drug Discovery, ONCODESIGN Biotechnology


New Targets and Approaches for Inflammation 

8:55 Chairperson’s Opening Remarks

Suvit Thaisrivongs, Ph.D., Executive Director, Chemistry, Pfizer

9:00 Anti-Chemokine Neutraligands as Potential Anti-inflammatory Drugs: From in vitro to in vivo Studies

Jean-Luc Galzi, Ph.D., Professor, Biotechnology and Cellular Signaling, University of Strasbourg

The discovery and use of small chemical compounds targeting chemokines -or neutraligands- will be described within the scope of anti-inflammatory therapeutic research. The potency of these chemokine neutralizing compounds in airway inflammation will be presented, illustrating new concepts in allergic disease treatment. The generality of the concept will be discussed.

9:30 Restoration of Phagocytic Function in Gaucher Macrophages by Non-Inhibitory Small Molecule Chaperones

Samarjit Patnaik, Ph.D., Research Scientist, National Center for Advancing Translational Sciences, NIH

Gaucher disease is a rare genetic disorder caused by lack of glucocerebrosidase enzymatic activity. This leads to pronounced lysosomal substrate storage and impaired function in macrophages, the crucial sentinel cells that initiate acute inflammation. We demonstrate effective reversal of disease phenotypes in advanced cellular models with non-inhibitory small molecule chaperones.

10:00 Coffee Break in the Exhibit Hall with Poster Viewing

10:45 Discovery of Lesinurad, a URAT1 Inhibitor in Clinical Development for the Treatment of Gout

Jean-Luc Girardet, Ph.D., Vice President, Chemistry & Development Support, Ardea Biosciences, Inc.

Lesinurad is currently being developed for the treatment of hyperuricemia in gout patients. This molecule acts by inhibiting the reabsorption of uric acid in the kidney. It is being studied in phase 3 as combination therapy with xanthine oxidase inhibitors which reduce the production of serum uric acid.

LipoScience11:15 GlycA and GlycB: Unique New Serum Markers of Systemic Inflammation Accessed by NMR Spectroscopy

James Otvos, Ph.D., CSO, LipoScience, Inc.

Efficiently-quantifiable NMR signals from the N-acetylglucosamine/galactosamine (GlycA) and sialic acid (GlycB) moieties of glycosylated serum proteins can serve as unique new measures of systemic inflammation. Prospective clinical data indicate GlycA is more strongly associated with CHD, diabetes, CKD and other outcomes than traditional inflammation markers such as hs-CRP and fibrinogen. 

11:30 Targeted Peptide Nanomedicine for Rheumatoid ArthritisHayat Onyuksel, Ph.D., Professor, Biopharmaceutical Sciences, University of Illinois at ChicagoVasoactive intestinal peptide (VIP) is an endogenous neuropeptide with demonstrated anti-inflammatory activity. However, its intravenous use is limited due to its very short half life. We have developed a targeted, stable and safe nanomedicine of VIP using phospholipid micelles, and showed its high activity with no side effects on an animal model of RA.

12:00 End of Conference

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