Xu Ran

TL;DR: The use of the Huisgen 1,3-dipolar cycloaddition reaction to generate triazole-stapled BCL9 α-helical peptides is reported, which show a marked increase in helical character and an improvement in binding affinity and metabolic stability relative to wild-type and linear BCL 9 peptides.

TL;DR: A survey of the last three years of literature on PPI inhibitors suggests a (more nuanced) conclusion to the question of whether PPIs are good drug targets; namely, that some PPI are readily 'druggable' given the right choice of scaffold, while others still seem to deserve the 'undruggability' moniker.

TL;DR: The design, synthesis, and evaluation of γ-carboline-containing compounds as a new class of small-molecule BET inhibitors and a cocrystal structure of 18 in complex with BRD4 BD2 at 1.4 Å resolution is determined, which provides a solid structural basis for the compound's high binding affinity and for its further structure-based optimization.

TL;DR: The design, synthesis, and evaluation of macrocyclic peptidomimetics that bind to WD repeat domain 5 (WDR5) and block the WDR5-mixed lineage leukemia (MLL) protein-protein interaction are reported.

TL;DR: Findings demonstrate broader, p53-independent roles for MDM2 and HUWE1 in apoptosis and specifically suggest the potential for therapy directed againstMDM2 to overcome lapatinib resistance.