A midthroughput screening follow-up program targeting the first bromodomain of the human
BRD4 protein, BRD4(BD1), identified an acetylated-mimic xanthine derivative inhibitor. This …

Cancer cells utilize the main de novo pathway and the alternative salvage pathway for
deoxyribonucleotide biosynthesis to achieve adequate nucleotide pools. Deoxycytidine kinase is …

Over the past few decades, hit identification has been greatly facilitated by advances in high-throughput
and fragment-based screenings. One major hurdle remaining in drug discovery …

Protein–protein interactions (PPIs) mediate nearly every cellular process and represent
attractive targets for modulating disease states but are challenging to target with small molecules…

Protein–protein interactions (PPIs) represent an enormous source of opportunity for
therapeutic intervention. We and others have recently pinpointed key rules that will help in …

Spermatogenesis is a dynamic process that is regulated by adhesive interactions between
germ and Sertoli cells. Germ cells express the Junctional Adhesion Molecule-C (JAM-C, …

The pleiotropic cytokine hormone leptin, by activating its receptor OB-R, plays a major role
in many biological processes, including energy homeostasis, immune function, and cell …

Syntenin stimulates exosome production and its expression is upregulated in many cancers
and implicated in the spread of metastatic tumor. These effects are supported by syntenin …

Neuroplin 1 (NRP1), a transmembrane protein interacting with Vascular Endothelial Growth
Factor VEGF-A 165 (called here VEGF165) and the tyrosine kinase Receptor 2 (VEGFR2) …

Differentially screening the Fr-PPIChem chemical library on the bromodomain and extra-terminal
(BET) BRD4-BDII versus -BDI bromodomains led to the discovery of a BDII-selective …