Chemo-proteomics exploration of HDAC degradability by small molecule degraders was written by Xiong, Yuan;Donovan, Katherine A.;Eleuteri, Nicholas A.;Kirmani, Nadia;Yue, Hong;Razov, Anthony;Krupnick, Noah M.;Nowak, Radoslaw P.;Fischer, Eric S.. And the article was included in Cell Chemical Biology in 2021.Quality Control of N-(5-Bromopentyl)phthalimide This article mentions the following:
Targeted protein degradation refers to the use of small mols. that recruit a ubiquitin ligase to a target protein for ubiquitination and subsequent proteasome-dependent degradation While degraders have been developed for many targets, key questions regarding degrader development and the consequences of acute pharmacol. degradation remain, specifically for targets that exist in obligate multi-protein complexes. Here, we synthesize a pan-histone deacetylase (HDAC) degrader library for the chemo-proteomic exploration of acute degradation of a key class of chromatin-modifying enzymes. Using chemo-proteomics, we not only map the degradability of the zinc-dependent HDAC family identifying leads for targeting HDACs 1-8 and 10 but also explore important aspects of degrading epigenetic enzymes. We discover cell line-driven target specificity and that HDAC degradation often results in collateral loss of HDAC-containing repressive complexes. These findings potentially offer a new mechanism toward controlling chromatin structure, and our resource will facilitate accelerated degrader design and development for HDACs. In the experiment, the researchers used many compounds, for example, N-(5-Bromopentyl)phthalimide (cas: 954-81-4Quality Control of N-(5-Bromopentyl)phthalimide).
N-(5-Bromopentyl)phthalimide (cas: 954-81-4) 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. Commercially available organobromine pharmaceuticals include the vasodilator nicergoline, the sedative brotizolam, the anticancer agent pipobroman, and the antiseptic merbromin. Quality Control of N-(5-Bromopentyl)phthalimide
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary