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.
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.
Transcription elongation by the elongation factor P-TEFb promotes the epithelial–mesenchymal transition and metastasis of breast cancer cells, implicating inhibition of this factor as a potential treatment for the late stages of this cancer.
3D culture of breast cancer in biologically relevant ECM potentiates the growth-inhibitory effects of unacylated ghrelin and AZP-531, and clinical response may be predictable based on a MAPK gene signature.
The study of a recurrent breast cancer MAGI3 truncation reveals the role of MAGI3 in regulating the Hippo effector YAP and highlights premature mRNA cleavage and polyadenylation as a mechanism underlying cancer development.