Adrian Whitty

TL;DR: The prevalence and pharmacological advantages of covalent drugs are surveyed, how potential risks and challenges may be addressed through innovative design, and the broad opportunities provided by targeted covalENT inhibitors are presented.

TL;DR: A small-molecule inhibitor of tumor necrosis factor α (TNF-α) that promotes subunit disassembly of this trimeric cytokine family member and forms a complex with a dimer of TNF- α subunits is identified.

TL;DR: The isolation and characterization of rat and human cDNAs for a novel cell-surface associated accessory protein, RETL2, that shares 49% identity with RETL1 are reported, raising the possibility that RETL 1 andRETL2 have distinctive roles during development and in the nervous system of the adult.

TL;DR: Results suggest that the greater biological activity of IFN-β-la is due to a stabilizing effect of the carbohydrate on structure, similar to that of other recombinant IFN products approved for the treatment of multiple sclerosis.

TL;DR: Analysis of the binding modes of a representative set of macrocycle-protein complexes provides evidence that large, natural product derived macrocycles can bind to targets that are not druggable by conventional, drug-like compounds, supporting the notion that natural product inspired synthetic macro cycles can expand the number of proteins that are druggability by synthetic small molecules.