scholarly journals Small-Molecule Antagonists of p53-MDM2 Binding: Research Tools and Potential Therapeutics

Cell Cycle ◽  
2004 ◽  
Vol 3 (4) ◽  
pp. 417-419 ◽  
Author(s):  
Lyubomir T. Vassilev
Author(s):  
Eman M. El-labbad ◽  
Xingyue Ji ◽  
Khaled A.M. Abouzid ◽  
Binghe Wang

SO2 is emerging as a possible endogenous signaling molecule in mammals. In addition, SO2 has also shown pharmacological effects, presenting SO2 as a promising potential therapeutic agent. The past decade has witnessed steady advances in the development of small molecule-based SO2 prodrugs/donors with varied release mechanisms. Herein, we summarize various strategies employed for SO2 prodrug design. The remaining challenges and issues will also be discussed.


Author(s):  
Bin Yu ◽  
Zekun Du ◽  
Yuming Zhang ◽  
Zhiyu Li ◽  
Jinlei Bian

Proteolysis-targeting chimeras are a new modality of chemical tools and potential therapeutics involving the induction of protein degradation. Cyclin-dependent kinase (CDK) protein, which is involved in cycles and transcription cycles, participates in regulation of the cell cycle, transcription and splicing. Proteolysis-targeting chimeras targeting CDKs show several advantages over traditional CDK small-molecule inhibitors in potency, selectivity and drug resistance. In addition, the discovery of molecule glues promotes the development of CDK degraders. Herein, the authors describe the existing CDK degraders and focus on the discussion of the structural characteristics and design of these degraders.


2012 ◽  
Vol 24 (4) ◽  
pp. 609-628 ◽  
Author(s):  
M. Manning ◽  
A. Misicka ◽  
A. Olma ◽  
K. Bankowski ◽  
S. Stoev ◽  
...  

2019 ◽  
Vol 55 (12) ◽  
pp. 1821-1824 ◽  
Author(s):  
Christian Steinebach ◽  
Hannes Kehm ◽  
Stefanie Lindner ◽  
Lan Phuong Vu ◽  
Simon Köpff ◽  
...  

Small-molecule heterobifunctional degraders can effectively control protein levels and are useful research tools.


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