Leanne Cutler

TL;DR: This work has yielded a potent, selective compound I-BET762 that is now under evaluation in a phase I/II clinical trial for nuclear protein in testis (NUT) midline carcinoma and other cancers.

TL;DR: A novel series of quinoline isoxazole BET family bromodomain inhibitors shows good oral bioavailability in both the rat and minipig as well as demonstrating efficient suppression of bacterial induced inflammation and sepsis in a murine in vivo endotoxaemia model.

TL;DR: A selective non‐peptidic BACE‐1 inhibitor is designed, GSK188909, that potently inhibits β‐cleavage of APP and reduces levels of secreted and intracellular Aβ in SHSY5Y cells expressing APP and can effectively lower brain Aβin vivo.

TL;DR: Preclinical studies show that I-BET762 has a favorable pharmacologic profile as an oral agent and that it inhibits myeloma cell proliferation, resulting in survival advantage in a systemicMyeloma xenograft model.

TL;DR: The present results demonstrate that compounds often considered to be Pgp substrates in rodents with poor passive permeability may still exhibit reasonable CNS penetration in vivo; i.e., where the unbound fractions and nonspecific tissue binding act as a compensating force.