Journal
MOLECULES
Volume 25, Issue 8, Pages -Publisher
MDPI
DOI: 10.3390/molecules25081948
Keywords
PROTACs; anticancer activity; protein degradation; IGF-1R; Src
Funding
- National Research Foundation of Korea (NRF) [NRF-2018R1A2B2005535, 2018R1A4A1021703]
- Korean government (MSIT)
- National Research Foundation of Korea [2018R1A4A1021703] Funding Source: Korea Institute of Science & Technology Information (KISTI), National Science & Technology Information Service (NTIS)
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A focused PROTAC library was developed to degrade both IGF-1R and Src proteins, which are associated with various cancers. PROTACs with IGF-1R and Src degradation potentials were synthesized by tethering different inhibitor warhead units and the E3 ligase (CRBN) recruiting-pomalidomide with various linkers. The designed PROTACs 12a-b inhibited the proliferation and migration of MCF7 and A549 cancer cells with low micromolar potency (1-5 mu M) in various cellular assays.
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