Ester is a chemical compound derived from an oxoacid (organic or inorganic) in which at least one –OH hydroxyl group is replaced by an –O– alkyl (alkoxy) group, 87-13-8, formula is C10H16O5, Name is Diethyl 2-(ethoxymethylene)malonate. as in the substitution reaction of a carboxylic acid and an alcohol. Synthetic Route of 87-13-8.
Veits, Gesine K.;Henderson, Christina S.;Vogelaar, Abigail;Eron, Scott J.;Lee, Linda;Hart, Ashley;Deibler, Richard W.;Baddour, Joelle;Elam, W. Austin;Agafonov, Roman V.;Freda, Jessica;Chaturvedi, Prasoon;Ladd, Brendon;Carlson, Mark W.;Vora, Harit U.;Scott, Thomas G.;Tieu, Trang;Jain, Arushi;Chen, Chi-Li;Kibbler, Emily S.;Pop, Marius S.;He, Minsheng;Kern, Gunther;Maple, Hannah J.;Marsh, Graham P.;Norley, Mark C.;Oakes, Catherine S.;Henderson, James A.;Sowa, Mathew E.;Phillips, Andrew J.;Proia, David A.;Park, Eunice S.;Patel, Joe Sahil;Fisher, Stewart L.;Nasveschuk, Christopher G.;Zeid, Rhamy research published 《 Development of an AchillesTAG degradation system and its application to control CAR-T activity》, the research content is summarized as follows. In addition to the therapeutic applicability of targeted protein degradation (TPD), the modality also harbors unique properties that enable the development of innovative chem. biol. tools to interrogate complex biol. TPD offers an all-chem. strategy capable of the potent, durable, selective, reversible, and time-resolved control of the levels of a given target protein in both in vitro and in vivo contexts. These properties are particularly well-suited for enabling the precise perturbation of a given gene to understand its biol., identify dependencies/vulnerabilities in disease contexts, and as a strategy to control gene therapies. To leverage these elegant properties, we developed the AchillesTag (aTAG) degradation system to serve as a tool in target identification and validation efforts. The aTAG degradation system provides a novel degradation tag based on the MTH1 protein paired with three fully validated bifunctional degraders with both in vitro and in vivo applicability. We catalog the development of the aTAG system from selection and validation of the novel MTH1 aTAG, alongside a comprehensive SAR campaign to identify high performing tool degraders. To demonstrate the utility of the aTAG system to dissect a complex biol. system, we apply the technol. to the control of Chimeric Antigen Receptor (CAR) activity. Using aTAG, we demonstrate the ability to potently and selectively control CAR protein levels, resulting in the exquisite rheostat control of CAR mediated T-cell activity. Furthermore, we showcase the in vivo application of the system via degradation of the aTAG-fused CAR protein in a human xenograft model. The aTAG degradation system provides a complete chem. biol. tool to aid foundational target validation efforts that inspire drug discovery campaigns towards therapeutic applicability.
87-13-8, Diethyl ethoxymethylenemalonate is a useful research compound. Its molecular formula is C10H16O5 and its molecular weight is 216.23 g/mol. The purity is usually 95%.
Diethyl ethoxymethylidenemalonate is a matrix effect reagent used in analytical chemistry. It is often used as a substrate for the cycloaddition process, which produces malondialdehyde and hydrochloric acid. The UV-absorption of the malondialdehyde can be measured to determine the concentration of the sample. Diethyl ethoxymethylidenemalonate is also used as a dna template in binding constants, where it binds with amines to form complexes that are then analyzed by light emission. It has been shown to have an inhibitory effect on gyrase and trifluoroacetic acid, both enzymes involved in DNA replication., Synthetic Route of 87-13-8
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics