Structure Based Design of Novel Il5 Receptor Antagonists

Period of Performance: 09/01/1999 - 08/31/2000


Phase 1 SBIR

Recipient Firm

Cengent Therapeutics, Inc.
San Diego, CA 92127
Principal Investigator


DESCRIPTION: (Adapted from the applicant's abstract) IL-5 is a T cell derived cytokine involved in the pathogenesis of atopic diseases. It specifically controls the production, activation and localization of eosinophils. Eosinophils are the major cause of tissue damage resulting in the symptoms of asthma and related allergic disorders. Thus, the design of orally bioavailable IL-5 receptor antagonists is an important area of therapeutic research for allergic asthma. Phase 1 of this project includes the following objectives: 1) generation of a 3-D dynamic model of a solvated IL-5; 2) identification of a surface aminoacyl sidechains which participate in ligand-receptor binding to generated pharmacophoric templates; 3) identification of non-peptide chemical that match the template for the described chemical properties; and 4) evaluation of biochemical and pharmacological activities of the selected small molecule IL-5 receptor antagonist candidates. Algorithms and computational tools necessary to derive these compounds have been established and implemented at Structural Bioinformatics inc. the goal of phase 2 activities aimed at refinement of the initial leads into qualified pre-clinical candidates for IL-5 antagonism PROPOSED COMMERCIAL APPLICATION: NOT AVAILABLE