Molecular glues targeting GSPT1 in cancers: A potent therapy
Dandan Zhang1, Pei Lin1, Jun Lin1
1School of Life sciences and Health Engineering, Jiangnan University, Wuxi 214122, China.
Abstract:
G1 to S phase transition 1 (GSPT1) is a key translation termination factor that significantly overexpressed in various cancer tissues and cells. Molecular glue is a kind of small molecule, which can bind to an E3 ligase such as cereblon (CRBN) and subsequently recruit neosubstrate proteins for ubiquitination-proteasomal degradation. This emerging therapeutic approach shows great potential in treating cancers and other diseases. This review aims to introduce current understanding of antitumor mechanism of molecular glues targeting GSPT1, summarize pharmacology profiles of existing molecular glues, and outline development strategies of novel molecular glues. The insights provided in this review will be valuable for future studies.
Insights
Molecular glues targeting GSPT1 offer a novel therapeutic strategy for cancer. By hijacking the ubiquitination-proteasomal system, these compounds degrade overexpressed GSPT1, showing promise in cancer treatment.
Area of Science:
- Oncology
- Molecular Biology
- Drug Discovery
Background:
- G1 to S phase transition 1 (GSPT1) is overexpressed in various cancers.
- Molecular glues are small molecules that recruit neosubstrate proteins for degradation via E3 ligases like cereblon (CRBN).
- This approach holds potential for treating cancers and other diseases.
Conclusions:
- Molecular glues targeting GSPT1 represent a promising anticancer strategy.
- Further research into their pharmacology and development is warranted.
- This review provides insights for future studies in this field.
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