Structure-based design of high-affinity fluorescent probes for the neuropeptide Y Y1 receptor was written by Mueller, Christoph;Gleixner, Jakob;Tahk, Maris-Johanna;Kopanchuk, Sergei;Laasfeld, Tonis;Weinhart, Michael;Schollmeyer, Dieter;Betschart, Martin U.;Luedeke, Steffen;Koch, Pierre;Rinken, Ago;Keller, Max. And the article was included in Journal of Medicinal Chemistry in 2022.Recommanded Product: 1-Bromopyrrolidine-2,5-dione This article mentions the following:
The recent crystallization of the neuropeptide Y Y1 receptor (Y1R) in complex with the argininamide-type Y1R selective antagonist UR-MK299 (2) opened up a new approach toward structure-based design of nonpeptidic Y1R ligands. We designed novel fluorescent probes showing excellent Y1R selectivity and, in contrast to previously described fluorescent Y1R ligands, considerably higher (~100-fold) binding affinity. This was achieved through the attachment of different fluorescent dyes to the diphenylacetyl moiety in 2 via an amine-functionalized linker. The fluorescent ligands exhibited picomolar Y1R binding affinities (pKi values of 9.36-9.95) and proved to be Y1R antagonists, as validated in a Fura-2 calcium assay. The versatile applicability of the probes as tool compounds was demonstrated by flow cytometry- and fluorescence anisotropy-based Y1R binding studies (saturation and competition binding and association and dissociation kinetics) as well as by widefield and total internal reflection fluorescence (TIRF) microscopy of live tumor cells, revealing that fluorescence was mainly localized at the plasma membrane. In the experiment, the researchers used many compounds, for example, 1-Bromopyrrolidine-2,5-dione (cas: 128-08-5Recommanded Product: 1-Bromopyrrolidine-2,5-dione).
1-Bromopyrrolidine-2,5-dione (cas: 128-08-5) belongs to organobromine compounds. Many of the organo bromine compounds are relatively nonpolar. Bromine is more electronegative than carbon (2.8 vs 2.5) and hence the carbon in a carbonbromine bond is electrophilic in nature. One prominent application of synthetic organobromine compounds is the use of polybrominated diphenyl ethers as fire-retardants, and in fact fire-retardant manufacture is currently the major industrial use of the element bromine.Recommanded Product: 1-Bromopyrrolidine-2,5-dione
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary