Quality Control of Ethyl 3-bromopropanoateIn 2021 ,《Discovery of a cryptic site at the interface 2 of TEAD – Towards a new family of YAP/TAZ-TEAD inhibitors》 appeared in European Journal of Medicinal Chemistry. The author of the article were Sturbaut, Manon; Bailly, Fabrice; Coevoet, Mathilde; Sileo, Pasquale; Pugniere, Martine; Liberelle, Maxime; Magnez, Romain; Thuru, Xavier; Chartier-Harlin, Marie-Christine; Melnyk, Patricia; Gelin, Muriel; Allemand, Frederic; Guichou, Jean-Francois; Cotelle, Philippe. The article conveys some information:
The Hippo pathway is involved in organ size control and tissue homeostasis by regulating cell growth, proliferation and apoptosis. It controls the phosphorylation of the transcription co-activator YAP (Yes associated protein) and TAZ (Transcriptional coactivator with PDZ-binding motif) in order to control their nuclear import and their interaction with TEAD (Transcriptional Enhanced Associated Domain). YAP, TAZ and TEADs are dysregulated in several cancers making YAP/TAZ-TEAD interaction a new emerging anti-cancer target. We report the synthesis of a set of trisubstituted pyrazoles which bind to hTEAD2 at the interface 2 revealing for the first time a cryptic pocket created by the movement of the phenol ring of Y382. Compound I disrupts YAP/TAZ-TEAD interaction in HEK293T cells and inhibits TEAD target genes and cell proliferation in MDA-MB-231 cells. Compound I is therefore the first inhibitor of YAP/TAZ-TEAD targeting interface 2. This mol. could serve with other pan-TEAD inhibitors such as interface 3 ligands, for the delineation of the relative importance of VGLL vs YAP/TAZ in a given cellular model. The results came from multiple reactions, including the reaction of Ethyl 3-bromopropanoate(cas: 539-74-2Quality Control of Ethyl 3-bromopropanoate)
Ethyl 3-bromopropanoate(cas: 539-74-2) belongs to organobromine compounds.Depending on the type of carbon to which the bromine is bonded, organic bromide could be alkyl, alkenyl, alkynyl, or aryl. Quality Control of Ethyl 3-bromopropanoate Due to the reactivity of bromide, they are used as potential precursors or important intermediates in organic synthesis.
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary