Applied Peptidomimetics: Creating a functional model for Alzheimer's disease research and catalytic activity of small peptides" (2009). University of Tennessee Honors Thesis Projects.

A microfluidic technique for combinatorial chemical synthesis of peptidomimetics has been developed. The new 32step method is fast, automated and includes an integrated magnetic separation of inorganic catalysts from reaction products. This proof-of-concept study should lead to methods for generating libraries of compounds suitable for screening for bioactivity.

autophagy is a cellular process mediating degradation of bulk cytoplasm, long-lived proteins and entire organelles. in this process, double-membrane vesicles, the autophagosomes, wrap around portions of cytosol and transport them to the lysosome for degradation. several molecules participate in autophagosome nucleation and elongation, including various components of the class iii pi3k complex, ...

Introduction Phosphorus-based peptidomimetics have been attractive target compounds during research and development of metalloproteinase inhibitors [1]. Their inhibiting activities are thought to be associated with mimicry of the metal-mediated transition state or tetrahedral-intermediate of the amide hydrolysis [2]. Because of the important roles of metal ions in the structures and functions o...

A series of beta-diketone derivatives of RGD peptidomimetics that selectively bind to alphavbeta3 and alphavbeta5 integrins were synthesized and covalently docked to the reactive lysine residues of monoclonal aldolase antibody 38C2. The resulting targeting devices strongly and selectively bound to human cancer cells expressing integrins alphavbeta3 and alphavbeta5 as analyzed by flow cytometry....

Trifluoromethyl propargylamines react with various azide derivatives to afford 1,4-disubstituted 1,2,3-triazoles through a Huisgen 1,3-dipolar cycloaddition. The reaction is catalyzed by a Cu(I) species in acetonitrile, and the corresponding products are obtained in good yields. This process thus offers an entry to new trifluoromethyl peptidomimetics as interesting scaffolds.