Sonia Lobo Planey

TL;DR: A current review of the literature reveals a continued reliance on the synthesis of novel structures with increased potency, rather than a focus on maintaining optimal physicochemical properties associated with ADMET throughout drug optimization, which may contribute significantly to the overall quality of candidate drugs at different stages of discovery.

TL;DR: The mechanisms of SERM tissue specificity are discussed and the therapeutic application of well-known and emergent SERMs are highlighted, including thromboembolic events, that have proven to be obstacles in their clinical utility.

TL;DR: The data establish trodusquemine as an effective central and peripheral PTP1B inhibitor with the potential to elicit noncachectic fat‐specific weight loss and improve insulin and leptin levels.

TL;DR: This review will focus on how glucocorticoid-induced apoptosisin lymphocytes is mediated by the glucoc Corticoid receptor, including a discussion of GR structure, function, and recent data implicating its role in the apoptotic process.

TL;DR: This work presents a method called palmitoyl-cysteine isolation capture and analysis (or PICA) to identify PAT-substrate relationships in a living vertebrate system and demonstrates its effectiveness by identifying CKAP4/p63 as a substrate of DHHC2, a putative tumor suppressor.