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Discovery of Inositol(1,4,5)trisphosphate Receptor Inhibitors

Award Information

Agency:
Department of Health and Human Services
Branch:
N/A
Award ID:
89384
Program Year/Program:
2008 / SBIR
Agency Tracking Number:
NS049920
Solicitation Year:
N/A
Solicitation Topic Code:
N/A
Solicitation Number:
N/A
Small Business Information
ECHELON BIOSCIENCES, INC.
675 ARAPEEN DRIVE, SUITE 302 SALT LAKE CITY, UT 84108-
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Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No
 
Phase 1
Fiscal Year: 2008
Title: Discovery of Inositol(1,4,5)trisphosphate Receptor Inhibitors
Agency: HHS
Contract: 1R43NS049920-01A2
Award Amount: $93,749.00
 

Abstract:

DESCRIPTION (provided by applicant): Stroke has become a significant cause of mortality and morbidity among elderly people in industrialized countries. To address the growing burden of health care costs and the immeasurable emotional toll on families as we ll as affected individuals, new pharmacological agents for prevention and treatment are desperately needed. Oxygen deprivation and oxidative stress lead to release of cytochrome c, which is related in turn to the activation of Ins(1,4,5)P3 receptors (IP3R) controlling calcium release from intracellular stores. Therefore, small molecule antagonists of IP3R would be attractive therapeutic candidates to restore proper calcium signaling pathways and prevent apoptosis. To establish the feasibility of this approa ch, Echelon Biosciences proposes to synthesize and identify potential IP3 antagonists. Specifically, we will use in silico modeling in combination with chemical library synthesis to prepare phosphate-free IP3 mimetics that dock in the ligand binding site, as well as a series of xestospongin (a potent natural IP3R inhibitor) analogs. Candidate compounds will be screened using a medium throughput in-cell fluorescence-based assay in which the time course for calcium release by IP3 in appropriately stimulated c ells is monitored in Fluo-3 plus drug-treated fibroblasts. Activity will be optimized by iterative cycles of modeling and synthesis based on biological activities observed.

Principal Investigator:

Business Contact:


ksauder@echelon-inc.com
Small Business Information at Submission:

ECHELON BIOSCIENCES, INC.
675 ARAPEEN DRIVE, SUITE 302 SALT LAKE CITY, UT 84108

EIN/Tax ID: 841417180
DUNS: N/A
Number of Employees: N/A
Woman-Owned: No
Minority-Owned: No
HUBZone-Owned: No