De-Novo Design of Cereblon (CRBN) Effectors Guided by Natural Hydrolysis Products of Thalidomide Derivatives was written by Heim, Christopher;Pliatsika, Dimanthi;Mousavizadeh, Farnoush;Baer, Kerstin;Hernandez Alvarez, Birte;Giannis, Athanassios;Hartmann, Marcus D.. And the article was included in Journal of Medicinal Chemistry in 2019.Quality Control of tert-Butyl (cis-4-(hydroxymethyl)cyclohexyl)carbamate This article mentions the following:
Targeted protein degradation via cereblon (CRBN), a substrate receptor of an E3 ubiquitin ligase complex, is an increasingly important strategy in various clin. settings, in which the substrate specificity of CRBN is altered via the binding of small-mol. effectors. To date, such effectors are derived from thalidomide and confer a broad substrate spectrum that is far from being fully characterized. Here, we employed a rational and modular approach to design novel and minimalistic CRBN effectors. In this approach, we took advantage of the binding modes of hydrolyzed metabolites of several thalidomide-derived effectors, which we elucidated via crystallog. These yielded key insights for the optimization of the minimal core binding moiety and its linkage to a chem. moiety that imparts substrate specificity. Based on this scaffold, we present a first active de-novo CRBN effector that is able to degrade the neo-substrate IKZF3 in the cell culture. In the experiment, the researchers used many compounds, for example, tert-Butyl (cis-4-(hydroxymethyl)cyclohexyl)carbamate (cas: 223131-01-9Quality Control of tert-Butyl (cis-4-(hydroxymethyl)cyclohexyl)carbamate).
tert-Butyl (cis-4-(hydroxymethyl)cyclohexyl)carbamate (cas: 223131-01-9) belongs to alcohols. Similar to water, an alcohol can be pictured as having an sp3 hybridized tetrahedral oxygen atom with nonbonding pairs of electrons occupying two of the four sp3 hybrid orbitals. Alcohols may be oxidized to give ketones, aldehydes, and carboxylic acids. These functional groups are useful for further reactions. Oxidation of organic compounds generally increases the number of bonds from carbon to oxygen (or another electronegative element, such as a halogen), and it may decrease the number of bonds to hydrogen.Quality Control of tert-Butyl (cis-4-(hydroxymethyl)cyclohexyl)carbamate
Referemce:
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Alcohols – Chemistry LibreTexts