Lenalidomide-5-Br 是一种基于 Lenalidomide 的 E3 泛素连接酶 cereblon (CRBN) 配体，用于募集 cereblon 蛋白。Lenalidomide-5-Br 可通过 linker 连接到蛋白质配体上形成 PROTAC。
Lenalidomide-5-Br is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-Br can be connected to the ligand for protein by a linker to form PROTAC[1].
PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins[2].
[1]. Scheepstra M, et al. Bivalent Ligands for Protein Degradation in Drug Discovery. Comput Struct Biotechnol J. 2019;17:160-176. Published 2019 Jan 25.
[2]. Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985.
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