… Another predicted outcome of ‘omics’ studies in humans is a greater emphasis in the
future on personalized medicines based on identification of an individual’s genetic make-up. …

… Hepworth and S. Liras of Pfizer) in chemical space that become increasingly sparse with
increasing molecular mass. We postulate that many of these islands are populated with …

By utilizing structure-based drug design (SBDD) knowledge, a novel class of phosphodiesterase
(PDE) 10A inhibitors was identified. The structure-based drug design efforts identified a …

Diazo decomposition of allylic and homoallylic diazoacetates lOa-p and 22a-j catalyzed by
chiral dirhodium (II) tetrakis [methyl 2-pyrrolidone-5 (S)-carboxylate], Rh2 (5S-MEPY) 4 (7), …

Enhancing the oral bioavailability of peptide drug leads is a major challenge in drug design.
As such, methods to address this challenge are highly sought after by the pharmaceutical …

Helix‐constrained polypeptides have attracted great interest for modulating protein–protein
interactions (PPI). It is not known which are the most effective helix‐inducing strategies for …

Cyclic peptide natural products contain a variety of conserved, nonproteinogenic structural
elements such as d-amino acids and amide N-methylation. In addition, many cyclic peptides …

The use of peptides in medicine is limited by low membrane permeability, metabolic instability,
high clearance, and negligible oral bioavailability. The prediction of oral bioavailability of …

… Given the liver’s key role in metabolic regulation and the fact that it is the principal tissue
affected by diseases such as hepatitis B and C viruses as well as hepatocellular carcinoma, …

… We report the design and in vitro evaluation of S. pyogenes Cas9 proteins harboring
asialoglycoprotein receptor ligands (ASGPrL). In particular, we demonstrate that the resulting …