Macrocycles are ideal in efforts to tackle “difficult” targets, but our understanding of what
makes them cell permeable and orally bioavailable is limited. Analysis of approximately 100 …

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 …

Oral bioavailability measurements in rats for over 1100 drug candidates studied at
SmithKline Beecham Pharmaceuticals (now GlaxoSmithKline) have allowed us to analyze …

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 …

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

Cyclic cell-penetrating peptides are relatively a newer class of peptides that have a huge
potential for the intracellular delivery of therapeutic agents aimed at treating challenging …

Chemical biologists commonly seek out correlations between the physicochemical
properties of molecules and their behavior in biological systems. However, a new paradigm …

Recent literature shows that intramolecular hydrogen bond (IMHB) formation can positively
impact upon the triad of permeability, solubility, and potency of drugs and candidates. IMHB …

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