Rebecca C. Furze

TL;DR: It is shown that broadly neutralizing antibodies (bNAbs) can interfere with establishment of a silent reservoir by Fc-FcR-mediated mechanisms, and combinations of inducers and bNAbs constitute a therapeutic strategy that impacts the establishment and maintenance of the HIV-1 reservoir in humanized mice.

TL;DR: This article describes the structure-based optimization of a series of naphthyridones from micromolar leads with no selectivity over the BET bromodomains to inhibitors with sub-100 nM ATAD2 potency and 100-fold BET selectivity.

TL;DR: The discovery of a hit from a fragment-based targeted array is described, which produced the first known micromolar inhibitors of the ATAD2 bromodomain.

TL;DR: This work reports the first reported low-nanomolar, selective and cell permeable chemical probe for ATAD2, a cancer-associated protein whose bromodomain has been described as among the least druggable of that target class.

TL;DR: The design and synthesis of a dual active histone deacetylase (HDAC)/bromodomain and extra terminal (BET) small molecule tool inhibitor, DUAL946 is described, which was confirmed by in vitro biochemical and biophysical testing and through chemoproteomic competition experiments in cell lysates.