基于Retro-2的PROTACs的合成和生物评估揭示了PEG-linker的长度和弹头对GSPT1降解的影响

Marine Michon1, Sebastien Curpanen2, Ombeline Pessey1

  • 1Universite Paris-Saclay, CEA, INRAE, Medicaments et Technologies pour la Sante (MTS), SIMoS, Gif-sur-Yvette, 91191, France.

概括

蛋白质溶解向金马 (PROTACs) 是一种新型的双功能分子. 这项研究表明,特定的PROTACs可以降解GSPT1蛋白质,降解效率受到链接器长度的影响,这挑战了以前关于它们机制的假设.

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