Matthew T. Dimare

TL;DR: EnPlex, an efficient, high-throughput method for simultaneously assessing inhibitor potency and specificity, is reported and followed-up of a series of dipeptidyl peptidase 4 (DPP4) inhibitors showed that EnPlex indeed predicted efficacy and safety in animal models, and suggest such profiling can be incorporated into the earliest stages of drug discovery.

TL;DR: The results show that the potency of simple dipeptide boronic acid-based inhibitors can be combined with selectivity against DPP8/9 in vivo to produce agents with a relatively wide therapeutic index (>500) in rodents.

TL;DR: It is demonstrated that purified FAP cleaves human FGF-21 at this site in vitro, and that an FAP-specific inhibitor, ARI-3099, blocks the activity in mouse, monkey and human plasma and prolongs the half-life of circulating human F GF-21 in mice.

TL;DR: It is reported that incorporation of specially designed amino acid analogues at the P1' position, directly C-terminal of the enzyme cleavage site, renders peptides, including glucagon-like peptide-1 (7-36) amide and six other examples, highly resistant to serine protease degradation without significant alteration of their biological activity.