ArticleInternational journal of molecular sciences2023
Targeting the Gastrin-Releasing Peptide Receptor (GRP-R) in Cancer Therapy: Development of Bombesin-Based Peptide-Drug Conjugates.
Article in International journal of molecular sciences, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 26 citations in OpenAlex.
- Potential medical applicability of N-β-Ala and N-His dipeptidomimetics against breast cancer: short in vitro and in silico screening.Scientific reports · 2026Article
- Neuropilin-1-Targeted Cell-Penetrating Tandem Peptide-Drug Conjugate Exhibits Potent In Vivo Antiglioma and Antiangiogenic Activity.Journal of medicinal chemistry · 2026Article
- Unveiling prognostic genes and regulatory mechanisms of stress granules in gastric cancers: an integrated analysis of bulk transcriptomics and single-cell RNA sequencing.Frontiers in oncology · 2026Article
- Review
- Comparative Enzymatic and Stability Assays Reveal GPLG as an Effective Cathepsin B Cleavable Linker for Tumor-Targeting Drug Conjugates.ACS omega · 2025Article
- PD-L1-targeted polymer-peptide-immune nanomedicine synergizes radiotherapy for durable tumor control.Bioactive materials · 2025Article
- Bispecific Radioligands (BRLs): Two Is Better Than One.Journal of clinical medicine · 2025Review
- Peptide-Drug Conjugates as Next-Generation Therapeutics: Exploring the Potential and Clinical Progress.Bioengineering (Basel, Switzerland) · 2025Review
- Bombesin-Targeted Delivery of β-Carboline-Based Ir(III) and Ru(II) Photosensitizers for a Selective Photodynamic Therapy of Prostate Cancer.Inorganic chemistry · 2024Article
- Oxime-Linked Peptide-Daunomycin Conjugates as Good Tools for Selection of Suitable Homing Devices in Targeted Tumor Therapy: An Overview.International journal of molecular sciences · 2024Review
- Targeting the Melanocortin 1 Receptor in Melanoma: Biological Activity of α-MSH-Peptide Conjugates.International journal of molecular sciences · 2024Article
- Stabilizing Scaffold for Short Peptides Based on Knottins.Current cancer drug targets · 2024Article
- Design and Characterization of a Multistage Peptide-Based Vaccine Platform to TargetBioconjugate chemistry · 2023Article
- Optimizing the enzymatic release of MMAE fromFrontiers in pharmacology · 2023Article
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Authors and funding
10 authors at 3 institutions in 1 country.
Funding
Abstract
Targeted tumour therapy has proved to be an efficient alternative to overcome the limitations of conventional chemotherapy. Among several receptors upregulated in cancer cells, the gastrin-releasing peptide receptor (GRP-R) has recently emerged as a promising target for cancer imaging, diagnosing and treatment due to its overexpression on cancerous tissues such as breast, prostate, pancreatic and small-cell lung cancer. Herein, we report on the in vitro and in vivo selective delivery of the cytotoxic drug daunorubicin to prostate and breast cancer, by targeting GRP-R. Exploiting many bombesin analogues as homing peptides, including a newly developed peptide, we produced eleven daunorubicin-containing peptide-drug conjugates (PDCs), acting as drug delivery systems to safely reach the tumour environment. Two of our bioconjugates revealed remarkable anti-proliferative activity, an efficient uptake by all three tested human breast and prostate cancer cell lines, high stability in plasma and a prompt release of the drug-containing metabolite by lysosomal enzymes. Moreover, they revealed a safe profile and a consistent reduction of the tumour volume in vivo. In conclusion, we highlight the importance of GRP-R binding PDCs in targeted cancer therapy, with the possibility of further tailoring and optimisation.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.