Approximately 75% of all disease-relevant human proteins, including those involved in
intracellular protein–protein interactions (PPIs), are undruggable with the current drug …

Peptides and proteins are not orally bioavailable in mammals, although a few peptides are
intestinally absorbed in small amounts. Polypeptides are generally too large and polar to …

We use computational design coupled with experimental characterization to systematically
investigate the design principles for macrocycle membrane permeability and oral …

In its 33 years, ADDR has published regularly on the po5tential of oral delivery of biologics
especially peptides and proteins. In the intervening period, analysis of the preclinical and …

Develo** macrocyclic peptides that can reach intracellular targets is a significant
challenge. This review discusses the most recent strategies used to develop cell permeable …

Drug discovery for difficult targets that have large and flat binding sites is often better suited
to compounds beyond the “rule of 5”(bRo5). However, such compounds carry higher …

The renaissance of peptides in pharmaceutical industry results from their importance in
many biological functions. However, low metabolic stability and the lack of oral availability of …

For decades, the development of peptides as potential drugs was aimed solely at peptides
with the highest affinity, receptor selectivity, or stability against enzymatic degradation …

Drug design efforts are turning to a new generation of therapeutic targets, such as protein–
protein interactions (PPIs), that had previously been considered “undruggable” by typical …

Peptides have traditionally been perceived as poor drug candidates due to unfavorable
characteristics mainly regarding their pharmacokinetic behavior, including plasma stability …