Brandon P. Schuff

TL;DR: It is shown that within a Bruton’s tyrosine kinase/cereblon PROTAC system, potent knockdown correlates with alleviation of steric clashes in the absence of thermodynamic cooperativity, which broadens the scope of PROTAC applications and affects fundamental design criteria across the field.

TL;DR: Methods for measuring the reactivity of covalent reactive groups (CRGs) with a biologically relevant nucleophile, glutathione (GSH), along with kinetic data for a broad array of electrophiles are described.

TL;DR: Evidence is provided for a number of analogues suggesting that the siderophore receptors PiuA and PirA play a role in drug uptake in P. aeruginosa strain PAO1.

TL;DR: A novel series of monocarbam compounds exhibiting promising antibacterial activity against multidrug resistant Gram-negative microorganisms is reported, along with the synthesis of one such molecule MC-1 and structure-activity relationships associated with the in vitro and in vivo efficacy of 1 and related analogues.

TL;DR: In this article, a series of electrophiles (acrylamides, nitriles, cyanamides, sulfones, and sulfonamides) using Nα-acetyl-L-lysine as a model amine-based nucleophile was compared with results using glutathione (GSH).