ArticleRSC medicinal chemistry2024
A novel hydrophobic tag leads to the efficient degradation of programmed death-ligand 1.
Article in RSC medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Who cites it
2 citing papers in PubMed.
- Hydrophobic Tag Protein Degraders: An Emerging Therapeutic Strategy for Cancer.Pharmaceuticals (Basel, Switzerland) · 2026Review
- Hydrophobic tagging: A promising paradigm for targeted protein degradation.Cell insight · 2026Review
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Authors and funding
7 authors.
Funding
Abstract
The interaction of PD-L1 and PD-1 transmits the inhibitory signal to reduce the proliferation of antigen-specific T-cells in lymph nodes. The expression of PD-L1 confers a potential escaping mechanism of tumors from the host immune system. Blocking the interaction of PD-1 and PD-L1 enables tumor-reactive T cells to overcome regulatory mechanisms and induce an effective antitumor response. The hydrophobic tag tethering degrader (HyTTD) contains a hydrophobic moiety, binding to the protein of interest (POI) to mimic the misfolding state of the POI, thereby inducing the degradation of POI. In this work, using the HyTTD strategy, we selected the diphenylmethyl derivatives as the PD-L1 binding motif for PD-L1 to develop the degraders for PD-L1, and multiple hydrophobic tags were attached. As a result, two HyTTDs Z2d and Z3d efficiently decreased the protein level of PD-L1 in both NCI-H460 and HT-1080 cells with low cytotoxicity. Meanwhile, the reduction of PD-L1 protein levels by Z2d/Z3d was counteracted by
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Registered trials
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