Peptidomimetic Modulators of BACE1

Rationally Designed Peptidomimetic Modulators of Aβ Toxicity in Alzheimer's Disease

Alzheimer's disease is one of the devastating illnesses mankind is facing in the 21st century. The main pathogenic event in Alzheimer's disease is believed to be the aggregation of the β-amyloid (Aβ) peptides into toxic aggregates. Molecules that interfere with this process may act as therapeutic agents for the treatment of the disease. Use of recognition unit based peptidomimetics as inhibitor...

Peptidomimetic Library

Development of peptidomimetic ligands of Pro-Leu-Gly-NH2 as allosteric modulators of the dopamine D2 receptor

A variety of stable, small-molecule peptidomimetic ligands have been developed to elucidate the mechanism by which the neuropeptide Pro-Leu-Gly-NH(2) (PLG) modulates dopaminergic neurotransmission. Photoaffinity labeling ligands based upon PLG peptidomimetics have been used to establish that PLG binds to the D(2) dopamine receptor at a site that is different from the orthosteric site, thus maki...

Synthetic Approaches towards Peptidomimetic Design

• Modified peptides: these molecules contain relatively small modifications that do not modify the peptide bond, and thus they still possess a chemical structure of peptide nature. • Pseudopeptides: in these compounds partial modifications of either peptide bonds or side-chains are introduced, contributing to the generation of molecules possessing a chemical structure of only partial peptide na...

Peptidomimetic isoform selective nNOS inhibitors

T he discovery of the cyclic nucleotides 3',5'cyclic monophosphate (cAMP, Prod. No. A 9501, A 4137) and guanosine 3',5'-cyclic monophosphate (cGMP, Prod. No. G 7504, G 6129) led to the first formulation of the second messenger concept. These cyclic nucleotides are now known to be ubiquitous intracellular second messengers that mediate the response of cells to a variety of extracellular stimuli ...