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Enhanced Tumor Targeting and Penetration of Proteolysis-Targeting Chimeras through iRGD Peptide Conjugation: A Strategy for Precise Protein Degradation in Breast Cancer

He, Shipeng, Fang, Yuxin, Wu, Minghao, Zhang, Peifeng, Gao, Fei, Hu, Honggang, Sheng, Chunquan, Dong, Guoqiang·2023·Journal of Medicinal Chemistry
DOI 10.1021/acs.jmedchem.3c01539
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Abstract

Proteolysis-targeting chimeras (PROTACs) have recently emerged as a promising technology for drug development. However, poor water solubility, limited tissue selectivity, and inadequate tumor penetration pose significant challenges for PROTAC-based therapies in cancer treatment. Herein, we developed an iRGD-PROTAC conjugation strategy utilizing tumor-penetrating cyclic peptide iRGD (CRGDK/RGPD/EC) to deliver PROTACs deep into breast cancer tissues. As a conceptual validation study, iRGD peptides were conjugated with a bromodomain-containing protein 4 (BRD4) PROTAC through a GSH-responsive linker. The resulting iRGD-PROTAC conjugate iPR showed enhanced water solubility, tumor-targeting capability, and penetration within tumor tissues, resulting in increased antibreast cancer efficacy in animal models and patient-derived organoids. This study demonstrates the advantages of combining iRGD and PROTACs in improving drug delivery and highlights the importance of tissue selectivity and penetration ability in PROTAC-based therapeutics.

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Metadata

Authors
He, S., Fang, Y., Wu, M., Zhang, P., Gao, F., Hu, H., Sheng, C., & Dong, G.
Venue
Journal of Medicinal Chemistry
Publisher
American Chemical Society (ACS)
Published
2023-12-06
Volume
66
Issue
24
Pages
16828-16842
ISSN
  • 0022-2623
  • 1520-4804
DOI
10.1021/acs.jmedchem.3c01539
Cited by
42
References
8
Language
en
Licence
Funders
  • National Key Research and Development Program of China (2022YFC3401500)
  • National Natural Science Foundation of China (82030105, 82273779, 82003567)
  • Shanghai Rising-Star Program (23QA1403500)

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CoChat. (2026). Citation check: Enhanced Tumor Targeting and Penetration of Proteolysis-Targeting Chimeras through iRGD Peptide Conjugation: A Strategy for Precise Protein Degradation in Breast Cancer. https://app.cochat.ai/papers/10.1021/acs.jmedchem.3c01539
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He, S., Fang, Y., Wu, M., Zhang, P., Gao, F., Hu, H., Sheng, C., & Dong, G. (2023). Enhanced Tumor Targeting and Penetration of Proteolysis-Targeting Chimeras through iRGD Peptide Conjugation: A Strategy for Precise Protein Degradation in Breast Cancer. Journal of Medicinal Chemistry. https://doi.org/10.1021/acs.jmedchem.3c01539