Maite de los Frailes

TL;DR: Using purified recombinant HDAC proteins, several novel HDAC inhibitors that preferentially inhibit HDAC1 or HDAC8 are identified and displayed distinct properties in inducing histone acetylation and reporter gene expression.

TL;DR: A series of 3-aryl-4-isoxazolecarboxamides identified from a high-throughput screening campaign as novel, potent small molecule agonists of the human TGR5 G-protein coupled receptor demonstrated improved GLP-1 secretion in vivo via an intracolonic dose coadministered with glucose challenge in a canine model.

TL;DR: The optimisation of an HTS hit series leading to the identification of structurally novel, selective, orally bioavailable mGluR2 positive modulators GSK1331258 and GSK 1331268 is described.

TL;DR: This work endeavored to screen the GSK compound collection for MIF inhibitors using a miniaturized, activity-based kinetic assay, finding 17 chemotypes prioritized and progressed to further stages of validation and characterization to better assess their therapeutic potential.

TL;DR: A novel series of indolines showing potent in vitro ghrelin receptor agonist activity and acceleration of gastric emptying in rats is discovered.