Bartholomew J. Votta

TL;DR: Major improvements to the proteolysis targeting chimeras (PROTACs) method are described, a chemical knockdown strategy in which a heterobifunctional molecule recruits a specific protein target to an E3 ubiquitin ligase, resulting in the target's ubiquitination and degradation.

TL;DR: A novel profile of activity strongly suggests that cytokine inhibitors could provide significant benefit in the therapy of chronic inflammatory disease.

TL;DR: X-ray crystallographic studies of the target enzyme complexed with inhibitor reinforce the observations made from site-directed mutagenesis studies, thereby providing a molecular basis for understanding the kinase selectivity of these inhibitors.

TL;DR: Overall TRPV4 plays an important role in urinary bladder function that includes an ability to contract the bladder as a result of the expression of TRPv4 in the UBSM, and 4α-PDD demonstrated a weak ability tocontract bladder strips compared with GSK1016790A.