Development of LM98, a Small-Molecule TEAD Inhibitor Derived from Flufenamic Acid was written by 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. And the article was included in ChemMedChem in 2021.Electric Literature of C8H6BrFO2 This article mentions the following:
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, Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9Electric Literature of C8H6BrFO2).
Methyl 2-bromo-4-fluorobenzoate (cas: 653-92-9) belongs to organobromine compounds. Organo bromine compounds are versatile compounds and are widely used in diverse fields. Organo bromine derivatives are used in the dye sector, as an indicator in analytical chemistry (Bromothymol blue is a popular indicator). Bromine-containing agents predominate because not only are they more efficient than similar chlorine-containing species, but also the high atomic weight of bromine ensures that it is present in a high mass fraction within most organobromine compounds.Electric Literature of C8H6BrFO2
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary