We discovered a highly potent bicyclic cage-like conformationally restricted, and proteolytically stable cyclopeptide, termed sunflower derived trypsin inhibitor, SFTI-1. We designed and synthesized a number of SFTI-1 analogs to improve its inhibitory specificity and serum stability. Some of the conformationally constrained cage-like bicyclic peptides and peptidomimetics demonstrate much better selectivity (more than 20-fold improvement) and stability. Our current goals are to develop more selective inhibitory analogs to SFTI-1, and to evaluate them in in vivo systems.

Agency
National Institute of Health (NIH)
Institute
Division of Basic Sciences - NCI (NCI)
Type
Intramural Research (Z01)
Project #
1Z01BC010703-01
Application #
7338833
Study Section
(LMC)
Project Start
Project End
Budget Start
Budget End
Support Year
1
Fiscal Year
2006
Total Cost
Indirect Cost
Name
Basic Sciences
Department
Type
DUNS #
City
State
Country
United States
Zip Code