Targeted intracellular protein degradation induced by a small molecule: En route to chemical proteomics

AR Schneekloth, M Pucheault, HS Tae…

文献索引：Schneekloth, Ashley R.; Pucheault, Mathieu; Tae, Hyun Seop; Crews, Craig M. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 22 p. 5904 - 5908

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被引用次数: 47

摘要

We have developed a heterobifunctional all-small molecule PROTAC (PROteolysis TArgeting Chimera) capable of inducing proteasomal degradation of the androgen receptor. This cell permeable PROTAC consists of a non-steroidal androgen receptor ligand (SARM) and the MDM2 ligand known as nutlin, connected by a PEG-based linker. The SARM–nutlin PROTAC recruits the androgen receptor to MDM2, which functions as an E3 ubiquitin ...