Synonyms: MD224
Compound class:
Synthetic organic
Comment: MD-224 is a PROTAC class degrader molecule of the MDM2 proto-oncogene (an E3 ubiquitin-protein ligase that acts as a negative regulator of the p53 tumour suppressor). PROTACs that recruit MDM2 simultaneously antagonise interaction with p53, promote MDM2 degradation and increase intracellular p53 [1-2]. MD-224 was designed to demonstrate the anti-tumour effect of this strategy.
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References |
1. Fang Y, Liao G, Yu B. (2020)
Small-molecule MDM2/X inhibitors and PROTAC degraders for cancer therapy: advances and perspectives. Acta Pharm Sin B, 10 (7): 1253-1278. [PMID:32874827] |
2. Vicente ATS, Salvador JAR. (2022)
MDM2-Based Proteolysis-Targeting Chimeras (PROTACs): An Innovative Drug Strategy for Cancer Treatment. Int J Mol Sci, 23 (19). [PMID:36232374] |
3. Wang S, Li Y, Yang J, Aguilar A, Zhou B, Hu J, Xu F, Rej R, Han X. (2017)
Mdm2 protein degraders. Patent number: WO2017176957A1. Assignee: The Regents Of The University Of Michigan. Priority date: 06/04/2017. Publication date: 12/10/2017. |