Pomalidomide-PEG2-azide is a synthetic E3 ligase ligand-linker conjugate that includes a Pomalidomide-based cereblon ligand and a 2-unit PEG linker used in proteolysis targeting chimeras (PROTAC) technology[1]. Pomalidomide-PEG2-azide is a click chemistry reagent containing an azide group that can react with alkynyl-containing molecules via a Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) reaction[2].
Click chemistry is a versatile reaction that can be used for the synthesis of a variety of conjugates. Virtually any biomolecule can be easily labelled with small molecules, such as fluorescent dyes, biotin, etc using click chemistry method.
Click chemistry reaction takes place between two components: azide and alkyne (terminal acetylene). Both azido and alkyne groups are nearly never encountered in natural biomolecules. Hence, the reaction is highly bioorthogonal and specific.
References:
[1] Zhang F, Wu Z, Chen P, et al. Discovery of a new class of PROTAC BRD4 degraders based on a dihydroquinazolinone derivative and lenalidomide/pomalidomide[J]. Bioorganic & medicinal chemistry, 2020, 28(1): 115228.
[2] Singh M S, Chowdhury S, Koley S. Advances of azide-alkyne cycloaddition-click chemistry over the recent decade[J]. Tetrahedron, 2016, 72(35): 5257-5283.
Pomalidomide-PEG2-azide是一种合成的E3连接酶配体-连接子缀合物，其中包含蛋白水解靶向嵌合体（PROTAC）技术中使用的基于Pomalidomide的cereblon配体和2单元PEG连接子[1]。 Pomalidomide-PEG2-azide是一种点击化学试剂，它含有叠氮基团，可以与含有炔基的分子发生Cu(I)催化的叠氮化物-炔环加成反应（CuAAC）[2]。
点击化学是一种多功能反应，可用于合成各种缀合物。事实上，任何生物分子都可以使用点击化学方法轻松地用小分子标记，例如荧光染料、生物素等。
点击化学反应发生在两种组分之间：叠氮化物和炔烃（末端乙炔）。叠氮基和炔基在天然生物分子中几乎从未遇到过。因此，该反应具有高度生物正交性和特异性。