1.PROTAC targeted protein degraders: the pastis prologue. Nat Rev Drug Discov. 2022 Jan 18 : 1–20.
下篇，我们将继续分享：PROTAC的设计、开发的难点与挑战、新一代PROTAC布局分享。参考文献：[1] Brandon Dale et al. Advancing targeted protein degradation for cancer therapy. Nat. Rev. Cancer 2021, 21(10): 638-654.[2] Miklós Békés et al. PROTAC targeted protein degraders: the past is prolog...
PROTAC targeted protein degraders: the past is prologue. Nat. Rev. Drug Discov.2022, 21(3): 181-200.[3] Aleša Bricelj et al. E3 Ligase Ligands in Successful PROTACs: An Overview of Syntheses and Linker Attachment Points. Front. Chem. 2021, 9: 707317.[4] Chao Wang et al. New-...
1.PROTAC targeted protein degraders: the pastis prologue. Nat Rev Drug Discov. 2022 Jan 18 : 1–20.
[6] Cromm P M, Crews C M. Targeted protein degradation: from chemical biology to drug discovery. Cell Chem Biol, 2017, 24(9): 1181-1190 [7] Bekes M, Langley D R, Crews C M. PROTAC targeted protein degraders: the past is prologue. Nat Rev Drug Discovery, 2022, 21(3): 181-200...
2、Neklesa, T.K.; Winkler, J.D.; Crews, C.M. Targeted protein degradation by PROTACs. Pharmacol. Ther. 2017, 174, 138–144.3、PROTAC targeted protein degraders: The past is prologue. Nat. Rev. Drug Discov. 2022, 21,181–200.4、PROteolysis TArgeting Chimeras (PROTACs)—Past, present...
[26] Békés, Miklós, David R. Langley, and Craig M. Crews. "PROTAC targeted protein degraders: the past is prologue." Nature Reviews Drug Discovery 21.3 (2022): 181-200.[27] Zou, Yutian, Danhui Ma, and Yinyin Wang. "The PROTAC technology in drug development." Cell biochemistry ...
3、PROTAC targeted protein degraders: The past is prologue. Nat. Rev. Drug Discov. 2022, 21,181–200. 4、PROteolysis TArgeting Chimeras (PROTACs)—Past, present and future. Drug Discov. T oday T echnol.2019, 31, 15–27. 5、《PROTAC递送系统最新研究进展及未来发展趋势》.同写意 ...
Targeted protein degraders crowd into the clinic. Nat. Rev. Drug Discov. 20, 247–250 (2021). CAS PubMed Google Scholar Wu, T. et al. Targeted protein degradation as a powerful research tool in basic biology and drug target discovery. Nat. Struct. Mol. Biol. 27, 605–614 (2020). ...
其实就是年前Craig那篇综述与展望,PROTAC targeted protein degraders: the past is prologue,这里想看其中几处比较细节的地方。 PROTAC binder所需的affinity范围 或者说最差需要多少的affinity——因为PROTAC一个优势就是不需要很强的binding,从而可能克服一些难成药靶点——那最低需要什么样的affinity呢?