Peptides have the potential to be potent pharmaceutical agents for the treatment of many
central nervous system derived maladies. Unfortunately peptides are generally water …

One of the major hurdles in developing therapeutic agents is the difficulty in delivering drugs
through the intestinal mucosa and blood-brain barriers (BBB). The goal here is to describe …

Backbone N-methylation is common among peptide natural products and has a substantial
impact on both the physical properties and the conformational states of cyclic peptides …

We report an atomistic physical model for the passive membrane permeability of cyclic
peptides. The computational modeling was performed in advance of the experiments and …

Delivery of proteins/peptides to the gastrointestinal (GI) tract via peroral/oral route involves
tremendous challenges due to unfavorable environmental conditions like harsh pH …

Despite the vast number of techniques developed for the cyclization of small peptides,
cyclization efficiency remains problematic in peptides that lack turn-promoting structures …

DNA-templated organic synthesis enables the translation, selection, and amplification of
DNA sequences encoding synthetic small-molecule libraries. Previously we described the …

The intent of this paper is to update the reader on various strategies which have been
utilized to increase the paracellular permeability of protein and polypeptide drugs across the …

Cyclization and selected backbone N-methylations are found to be often necessary but not
sufficient conditions for peptidic drugs to have a good bioavailability. Thus, the design of …

Cyclic peptides are of considerable interest as potential protein ligands. It has been
postulated that cyclic molecules might be more cell permeable than their linear counterparts …