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GSPT1 degraders: research progress, development strategies and challenges.

Bioorganic & medicinal chemistry 2025 Vol.131() p. 118390

Liu C, Peng H, Chen P, Li Y, Deng Z, Li S, Yang T, Liu K, Wang Z, Liu L

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Dysregulation of GSPT1 which is a critical translation termination factor plays an important role in oncogenesis and cancer progression.

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BibTeX ↓ RIS ↓
APA Liu C, Peng H, et al. (2025). GSPT1 degraders: research progress, development strategies and challenges.. Bioorganic & medicinal chemistry, 131, 118390. https://doi.org/10.1016/j.bmc.2025.118390
MLA Liu C, et al.. "GSPT1 degraders: research progress, development strategies and challenges.." Bioorganic & medicinal chemistry, vol. 131, 2025, pp. 118390.
PMID 41004880
DOI 10.1016/j.bmc.2025.118390

Abstract

Dysregulation of GSPT1 which is a critical translation termination factor plays an important role in oncogenesis and cancer progression. However, GSPT1 lacks suitable binding pockets and has long been considered an "undruggable" target. Recent studies have revealed that Cereblon E3 Ligase Modulators (CELMoDs), a class of molecular glue-type protein degraders, can bind to the E3 ubiquitin ligase substrate receptor Cereblon and induce Cereblon to recruit GSPT1, leading to GSPT1 degradation. This breakthrough provides a novel therapeutic strategy for GSPT1-related cancers. Currently, several selective GSPT1-degraders have entered clinical trials. This review summarized the research progress of various GSPT1 degraders with an emphasis on their design, activity studies and development strategy, aiming to provide valuable insights for the further development of GSPT1 degraders.

MeSH Terms

Humans; Ubiquitin-Protein Ligases; Proteolysis; Drug Development; Peptide Termination Factors; Animals; Antineoplastic Agents; Neoplasms; Molecular Structure; Adaptor Proteins, Signal Transducing

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