The following nonconfidential brief project summaries are presented below to
demonstrate just a few of the various types of projects that our scientists have
successfully completed.

 

 

Leukotriene B4 (LTB4) Antagonist

Developed a novel series of LTB4 receptor antagonists for an academic client using a structure based approach. Developed fluorescent-labeled ligand. NIH SBIR funded. One paper published1.

  1. D. Kiel et al. Adv. Prostaglandin Thromboxane Leukot. 1991 21A:403

 

Cannabinoid CB2 antagonist

Developed a novel series of CB2 antagonists with an academic collaborator using a structure-based approach.

 

Glucosyl-Ceramide Synthase Inhibitor

Carried out SAR studies on lead compound with an academic collaborator. New potent analog developed.

Project was NIH SBIR funded.  One paper published1. One patent issued2. Resulted in Pharma company licensing deal.

  1. A. Abe et al. J. Lipid Res. 1995 36:611
  2. US 5,916,911 (1999)

 

 

Sirt1 Activator

Discovered a natural product Sirt1 activator (resveratrol) as potential lifespan extension agent employing a natural products-based screening approach.  Carried out SAR studies on lead compound.  Two papers published1,2. Patents issued3. Resulted in Pharma company licensing deal.

  1. KT Howitz et al. Nature 2003 425:191
  2. H Yang et al. Aging Cell 2007 6:35
  3. US 7,544,497 (2009)

 

Discovery of Novel Endogenous Lipid Mediators

Synthesized new lipids related to anandamide to confirm structure of endogenous mediators and ligands with academic collaborator. Discovered new target for anti-inflammatory analgesic drug development. Three papers published1-3. One patent issued4.

  1. SM Huang et al. J. Biol. Chem. 2001 276:42639
  2. CJ Chu et al. J. Biol. Chem. 2003 278:13633
  3. SH Burstein et al. Bioorg. Med. Chem. 2007 15:3345
  4. US 7,544,714 (2009)

 

Sphingosine Kinase-1 Inhibitor

Designed and synthesized novel series of Sphingosine Kinase-1 inhibitors as potential anticancer agents using structure-based approach with academic collaborator. Two papers published1,2. One patent issued3.  Resulted in Pharma company licensing deal.

  1. SW Paugh et al. Blood 2008 112:1382
  2. D Kapitonov et al. Cancer Res. 2009 69:6915
  3. US 8,314,151 (2012)

 

GPR55 Receptor Deorphaning

Designed and synthesized potential endogenous ligands for GPR55 with academic collaborator. Project is on-going.