Melin, Lea; Abdullayev, Shuay; Fnaiche, Ahmed; Vu, Victoria; Gonzalez Suarez, Narjara; Zeng, Hong; Szewczyk, Magdalena M.; Li, Fengling; Senisterra, Guillermo; Allali-Hassani, Abdellah; Chau, Irene; Dong, Aiping; Woo, Simon; Annabi, Borhane; Halabelian, Levon; LaPlante, Steven R.; Vedadi, Masoud; Barsyte-Lovejoy, Dalia; Santhakumar, Vijayaratnam; Gagnon, Alexandre published their research in ChemMedChem in 2021. The article was titled 《Development of LM98, a Small-Molecule TEAD Inhibitor Derived from Flufenamic Acid》.HPLC of Formula: 1530-32-1 The article contains the following contents:
The YAP-TEAD transcriptional complex is responsible for the expression of genes that regulate cancer cell growth and proliferation. Dysregulation of the Hippo pathway due to overexpression of TEAD has been reported in a wide range of cancers. Inhibition of TEAD represses the expression of associated genes, demonstrating the value of this transcription factor for the development of novel anti-cancer therapies. We report herein the design, synthesis and biol. evaluation of LM98, a flufenamic acid analog. LM98 shows strong affinity to TEAD, inhibits its autopalmitoylation and reduces the YAP-TEAD transcriptional activity. Binding of LM98 to TEAD was supported by 19F-NMR studies while co-crystallization experiments confirmed that LM98 is anchored within the palmitic acid pocket of TEAD. LM98 reduces the expression of CTGF and Cyr61, inhibits MDA-MB-231 breast cancer cell migration and arrests cell cycling in the S phase during cell division. In the experiment, the researchers used many compounds, for example, Ethyltriphenylphosphonium bromide(cas: 1530-32-1HPLC of Formula: 1530-32-1)
Ethyltriphenylphosphonium bromide(cas: 1530-32-1) is a phase transfer catalyst, used to accelerate the cure of phenolic-based epoxy resins, certain fluoroelastomer resins and thermosetting powder coatings. It is also used as catalysts in the synthesis of certain organic compounds and as a pharmaceutical intermediate.HPLC of Formula: 1530-32-1
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary