Wei Jin

TL;DR: In an effort to identify small molecules that would disrupt the interaction between the light-chain metalloprotease of BoNT serotype A and its cognate substrate, a multifaceted screening effort was undertaken and validate the use of high-throughput screening protocols to define previously unrecognized chemical scaffolds for the development of therapeutic agents to treat BoNT exposure.

TL;DR: High throughput screening of synthetic combinatorial small molecule libraries is used to identify inhibitors of arenavirus infection using pseudotyped virion particles bearing the glycoproteins of highly pathogenic arenaviruses, resulting in the discovery of a series of novel small molecule inhibitors of viral entry.

TL;DR: Characterization of a representative O-(acylamino) prodrug in vivo indicates that they approach the potency and exceed the efficacy of thefree drug itself (CBI-indole2), indicating that not only is the free drug effectively released from the inactive prodrug but also that they offer additional advantages related to a controlled or targeted release in vivo.

TL;DR: The screening of a >9000 compound library of synthetic DNA binding molecules for selective binding to the consensus sequence of the transcription factor LEF-1 followed by assessment of the candidate compounds in a series of assays that characterized functional activity assures that activity in the final functional assay may be directly related to the inhibition of gene transcription and DNA binding properties of the identified molecules.

TL;DR: One compound was identified that inhibits wild-type protease, as well as a drug-resistant protease with six mutations that suggests an allosteric non-competitive mechanism of inhibition and may represent a starting point for an additional strategy for anti-retroviral therapy.