《Selective targeting of the αC and DFG-out pocket in p38 MAPK》 was written by Roehm, Sandra; Schroeder, Martin; Dwyer, Jessica E.; Widdowson, Caroline S.; Chaikuad, Apirat; Berger, Benedict-Tilman; Joerger, Andreas C.; Kraemer, Andreas; Harbig, Jule; Dauch, Daniel; Kudolo, Mark; Laufer, Stefan; Bagley, Mark C.; Knapp, Stefan. Safety of 3,5-Dibromoaniline And the article was included in European Journal of Medicinal Chemistry in 2020. The article conveys some information:
The p38 MAPK cascade is a key signaling pathway linked to a multitude of physiol. functions and of central importance in inflammatory and autoimmune diseases. Although studied extensively, little is known about how conformation-specific inhibitors alter signaling outcomes. Here, we have explored the highly dynamic back pocket of p38 MAPK with allosteric urea fragments. However, screening against known off-targets showed that these fragments maintained the selectivity issues of their parent compound BIRB-796, while combination with the hinge-binding motif of VPC-00628 greatly enhanced inhibitor selectivity. Further efforts focused therefore on the exploration of the αC-out pocket of p38 MAPK, yielding compound 137 as a highly selective type-II inhibitor. Even though 137 is structurally related to a recent p38 type-II chem. probe, SR-318, the data presented here provide valuable insights into back-pocket interactions that are not addressed in SR-318 and it provides an alternative chem. tool with good cellular activity targeting also the p38 back pocket. The experimental process involved the reaction of 3,5-Dibromoaniline(cas: 626-40-4Safety of 3,5-Dibromoaniline)
3,5-Dibromoaniline(cas: 626-40-4) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Safety of 3,5-Dibromoaniline
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary