In the last century, small-molecule natural products were the main inspiration for most drug
discovery programs based either on high-throughput screening (HTS) or rational design …

Since Hedin's characterization of trypsin and antitrypsin in 1906,(1) arguably the first
account of a regulatory protein–protein interaction (PPI), contemporary understanding of …

Protein–protein interactions (PPIs) have emerged as important and challenging targets in
chemical biology and medicinal chemistry. The main difficulty encountered in the discovery …

PCSK9 (proprotein convertase subtilisin/kexin type 9) is a negative regulator of the hepatic
LDL receptor, and clinical studies with PCSK9-inhibiting antibodies have demonstrated …

Naturally occurring antimicrobial peptides (AMPs) present several drawbacks that strongly
limit their development into therapeutically valuable antibiotics. These include susceptibility …

Proprotein convertase subtilisin/kexin type 9 (PCSK9) has been recently identified as a new
useful target for hypercholesterolemia treatment. This work demonstrates that natural …

Motivation Protein glycation is a familiar post-translational modification (PTM) which is a two-
step non-enzymatic reaction. Glycation not only impairs the function but also changes the …

The conventional anticancer therapeutics usually lack cancer specificity, leading to damage
of normal tissues that patients find hard to tolerate. Ideally, anticancer therapeutics carrying …

Peptide‐based therapeutics have grown in importance over the last few decades.
Furthermore, peptides have been extensively used as lead compounds in the drug …

Post-translational lysine methylation and acetylation are two major modifications of lysine
residues. They play critical roles in various biological processes, especially in gene …