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 kinase C (PKC) has been a tantalizing target for drug discovery ever since it was first
identified as the receptor for the tumour promoter phorbol ester in 1982. Although initial …

Small molecule modulators of biological function can be discovered by the screening of
compound libraries. However, it became apparent that some human disease related targets …

Cancer immunotherapy has made great strides in the recent decade, especially in the area
of immune checkpoint blockade. The outstanding efficacy, prolonged durability of effect, and …

EZH2, the catalytic subunit of PRC2, catalyzes histone H3 lysine 27 (H3K27) trimethylation
to induce the agglutination of chromosomes and in turn represses the transcription of the …

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 …

The Hippo pathway is a critical transcriptional signaling pathway that regulates cell growth,
proliferation and organ development. The transcriptional enhanced associate domain …

ABSTRACT Background Protein-protein interactions (PPIs) are intriguing targets for
designing novel small-molecule inhibitors. The role of PPIs in various infectious and …

Highlights•Cyclic peptides are ideal inhibitors of protein–protein interactions (PPIs), due to
low immunogenicity and large surface area.•Peptide libraries are excellent tools to screen …