Eric M Gordon

TL;DR: A strategy to discover low molecular weight ligands that bind weakly to targeted sites on proteins through an intermediary disulfide tether is reported, which allows one to nucleate drug design from a spatially targeted lead fragment.

TL;DR: Targeted, broad-spectrum metabolomics of plasma showed that chronic fatigue syndrome is a highly concerted hypometabolic response to environmental stress that traces to mitochondria and was similar to the classically studied developmental state of dauer, opening a fresh path for the rational development of new therapeutics.

TL;DR: Using a dynamic combinatorial technology, 'extended tethering', unique nonpeptidic inhibitors for caspase-3 are identified using reversible, tight-binding molecules that are druglike and distinct from known inhibitors.

TL;DR: The design, synthesis, and in vitro activities of a series of potent and selective small-molecule inhibitors of caspase-3 are described and a high-resolution X-ray cocrystal structure of 4 and 66b supports the predicted binding modes of the authors' compounds with caspases.

TL;DR: The AE isostere class represents a promising advance in the development of BACE-1 inhibitors, and possesses enzymatic and cell assay IC(50)s of 26 nM and 180 nM, respectively.