On September 1, 2020, Donoghue, Craig; Cubillos-Rojas, Monica; Gutierrez-Prat, Nuria; Sanchez-Zarzalejo, Carolina; Verdaguer, Xavier; Riera, Antoni; Nebreda, Angel R. published an article.Application of 1216805-11-6 The title of the article was Optimal linker length for small molecule PROTACs that selectively target p38α and p38β for degradation. And the article contained the following:
We report the design of hetero-bifunctional small mols. that selectively target p38α and p38β for degradation These proteolysis targeted chimeras (PROTACs) are based on an ATP competitive inhibitor of p38α and p38β, which is linked to thalidomide analogs to recruit the Cereblon E3 ubiquitin ligase complex. Compound synthesis was facilitated by the use of a copper catalyzed “click” reaction. We show that optimization of the linker length and composition is crucial for the degradation-inducing activity of these PROTACs. We provide evidence that these chem. compounds can induce degradation of p38α and p38β but no other related kinases at nanomolar concentrations in several mammalian cell lines. Accordingly, the PROTACs inhibit stress and cytokine-induced p38α signaling. Our compounds contribute to understanding the development of PROTACs, and provide a useful tool to investigate functions of the p38 MAPK pathway and its involvement in diseases. The experimental process involved the reaction of 2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindoline-5-carboxylic acid(cas: 1216805-11-6).Application of 1216805-11-6
The Article related to preparation protacs targeting p38 alpha beta proteolysis, azide-alkyne click reaction, cereblon, protac linker optimization, protein degradation, thalidomide derivative, p38 mapk and other aspects.Application of 1216805-11-6
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem