GDC-0810 is a novel, orally bioavailable SERD that exhibits robust pre-clinical activity in models of ER+ breast cancer, including models of tamoxifen resistance, and those that express the ERα mutations, ER.Y537S and ER.D538G.

Cryogenic electron microscopy enables real-time structure-based drug design to advance the discovery of novel classes of small molecule inhibitors.

Single-molecule tracking at scale, analyzing millions of cells and thousands of compounds per day, demonstrates that measuring protein motion provides mechanistic insights relevant to drug discovery.

A novel first-in-class small molecule (ERX-11) that interacts with and disrupts the interactome of the estrogen receptor (ER), blocks the growth of ER-positive breast cancers, including those that are resistant to currently approved hormonal agents.

The first-in-class kinase inhibitor, Ibrutinib, destabilizes its autoinhibited Bruton’s tyrosine kinase (BTK) target, and a remote resistance mutation causes global structural changes that activate BTK catalytic activity.

Human genomic DNA contains uracil in the late replicating, constitutive heterochromatic regions, while treatment with drugs perturbing thymidylate biosynthesis shifts the uracil distribution pattern towards the euchromatin in UNG-inhibited cells.

Effective antiestrogens engage a new structural interaction to improve therapeutic antagonism in hormone-resistant breast cancer cells expressing Y537S estrogen receptor alpha.

Formation of a giant unilocular vacuole through a macropinocytosis-like process in cells with disrupted actin cytoskeleton promotes resistance to anoikis.