Identification of Pirin as a Molecular Target of the CCG-1423/CCG-203971 Series of Antifibrotic and Antimetastatic Compounds was written by Lisabeth, Erika M.;Kahl, Dylan;Gopallawa, Indiwari;Haynes, Sarah E.;Misek, Sean A.;Campbell, Phillip L.;Dexheimer, Thomas S.;Khanna, Dinesh;Fox, David A.;Jin, Xiangshu;Martin, Brent R.;Larsen, Scott D.;Neubig, Richard R.. And the article was included in ACS Pharmacology & Translational Science in 2019.Computed Properties of C8H7BrO3 This article mentions the following:
A series of compounds (including CCG-1423 and CCG-203971) discovered through an MRTF/SRF-dependent luciferase screen has shown remarkable efficacy in a variety of in vitro and in vivo models, including significant reduction of melanoma metastasis and bleomycin-induced fibrosis. Although these compounds are efficacious in these disease models, the mol. target is unknown. Here, we describe affinity isolation-based target identification efforts which yielded pirin, an iron-dependent cotranscription factor, as a target of this series of compounds Using biophys. techniques including isothermal titration calorimetry and X-ray crystallog., we verify that pirin binds these compounds in vitro. We also show with genetic approaches that pirin modulates MRTF-dependent luciferase reporter activity. Finally, using both siRNA and a previously validated pirin inhibitor, we show a role for pirin in TGF-β-induced gene expression in primary dermal fibroblasts. A recently developed analog, CCG-257081, which cocrystallizes with pirin, is also effective in the prevention of bleomycin-induced dermal fibrosis. In the experiment, the researchers used many compounds, for example, Methyl 3-bromo-5-hydroxybenzoate (cas: 192810-12-1Computed Properties of C8H7BrO3).
Methyl 3-bromo-5-hydroxybenzoate (cas: 192810-12-1) 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. The principal reactions for organobromides include dehydrobromination, Grignard reactions, reductive coupling, and nucleophilic substitution.Computed Properties of C8H7BrO3
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary