Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2 was written by Scheuermann, Thomas H.;Stroud, Daniel;Sleet, Christopher E.;Bayeh, Liela;Shokri, Cameron;Wang, Hanzhi;Caldwell, Charles G.;Longgood, Jamie;MacMillan, John B.;Bruick, Richard K.;Gardner, Kevin H.;Tambar, Uttam K.. And the article was included in Journal of Medicinal Chemistry in 2015.Name: Methyl 3-bromo-5-fluorobenzoate This article mentions the following:
Hypoxia inducible factor (HIF) transcription factors reside at the center of signaling pathways used by mammalian cells to sense and respond to low oxygen levels. While essential to maintain oxygen homeostasis, misregulation of HIF protein activity correlates with tumor development and metastasis. To provide artificial routes to target misregulated HIF activity, the authors identified small mol. antagonists of the HIF-2 transcription factor that bind an internal cavity within the C-terminal PAS domain of the HIF-2浼?subunit. Here the authors describe a new class of chiral small mol. ligands that provide the highest affinity binding, the most effective, isoform-selective inhibition of HIF-2 in cells, and trigger the largest protein conformation changes reported to date. The current results further illuminate the mol. mechanism of HIF-2 antagonism and suggest addnl. routes to develop higher affinity and potency HIF-2 antagonists. In the experiment, the researchers used many compounds, for example, Methyl 3-bromo-5-fluorobenzoate (cas: 334792-52-8Name: Methyl 3-bromo-5-fluorobenzoate).
Methyl 3-bromo-5-fluorobenzoate (cas: 334792-52-8) belongs to organobromine compounds. Bromo compounds are employed in a variety of metal-catalyzed coupling reactions. They are also ideal candidates for the synthesis of Grignard reagents that have wide-applicability in organic synthesis. alpha-Bromoesters are employed in the Reformatsky reaction for the synthesis of beta-hydroxyesters. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Name: Methyl 3-bromo-5-fluorobenzoate
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary