Stephanie Guillet, Tomi Lazarov ... Frédéric Geissmann
Loss-of-function variants of human ACK1 and BRK kinase underlie systemic lupus erythematosus in young patients from multiplex families and disrupt the anti-inflammatory response of macrophages to apoptotic cells.
Confronting different models of chromatin accessibility with temporally resolved transcription profiles favors a scenario where transcription factors actively, rather than passively, drive chromatin from the inaccessible to the accessible state.
Ganesh V Raj, Gangadhara Reddy Sareddy ... Ratna K Vadlamudi
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.
CBP/p300 acetylation of histone H3 at promoters and enhancers stimulates transcriptional elongation through recruitment of the super-elongation complex and BRD4.
Rebecca EK Mandt, Madeline R Luth ... Amanda K Lukens
The mutational flexibility of the antimalarial target dihydroorotate dehydrogenase thwarts the use of collateral sensitivity as a strategy to suppress the evolution of resistance.
Cancer cells driven by mutations in KRAS or EGFR are dependent on DUSP6 to prevent ERK-induced cell death, creating a novel vulnerability for targeted therapy.
James D Joseph, Beatrice Darimont ... Jeffrey H Hager
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.
