On December 31, 2022, Ma, Shenghong; Tang, Tracy; Probst, Gary; Konradi, Andrei; Jin, Chunyu; Li, Fulong; Silvio Gutkind, J.; Fu, Xiang-Dong; Guan, Kun-Liang published an article.Quality Control of Bis(2,5-dioxopyrrolidin-1-yl) glutarate The title of the article was Transcriptional repression of estrogen receptor alpha by YAP reveals the Hippo pathway as therapeutic target for ER+ breast cancer. And the article contained the following:
Extensive knowledge has been gained on the transcription network controlled by ERα, however, the mechanism underlying ESR1 (encoding ERα) expression is less understood. We recently discovered that the Hippo pathway is required for the proper expression of ESR1. YAP/TAZ are transcription coactivators that are phosphorylated and inhibited by the Hippo pathway kinase LATS. Here we delineated the mol. mechanisms underlying ESR1 transcription repression by the Hippo pathway. Mechanistically, YAP binds to TEAD to increase local chromatin accessibility to stimulate transcription of nearby genes. Among the YAP target genes, Vestigial-Like Protein 3 (VGLL3) competes with YAP/TAZ for binding to TEAD transcription factor and recruits the NCOR2/SMRT repressor to the super-enhancer of ESR1 gene, leading to epigenetic alteration and transcriptional silencing. We developed a potent LATS inhibitor VT02956. Targeting the Hippo pathway by VT02956 represses ESR1 expression and inhibits the growth of ER+ breast cancer cells as well as patient-derived tumor organoids. Moreover, histone deacetylase inhibitors, such as Entinostat, induce VGLL3 expression to inhibit ER+ breast cancer cells. Our study suggests LATS as unexpected cancer therapeutic targets, especially for endocrine-resistant breast cancers. The experimental process involved the reaction of Bis(2,5-dioxopyrrolidin-1-yl) glutarate(cas: 79642-50-5).Quality Control of Bis(2,5-dioxopyrrolidin-1-yl) glutarate
The Article related to esr alpha therapeutic target er breast cancer transcriptional repression, Placeholder for records without volume info and other aspects.Quality Control of Bis(2,5-dioxopyrrolidin-1-yl) glutarate
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics