ArticleProceedings of the National Academy of Sciences of the United States of America2023
Structures of human gastrin-releasing peptide receptors bound to antagonist and agonist for cancer and itch therapy.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
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Who cites it
22 citing papers in PubMed, 38 citations in OpenAlex.
- GRPR-Targeted Radionuclide Conjugates: A Molecular Evolution Perspective.Chemistry & biodiversity · 2026Review
- Environmental Pollutants and Protein Destabilization in Lung Cancer: Anticancer Drug Strategies for Structural Stability.ACS omega · 2026Article
- Diagnostic performance of gastrin-releasing peptide receptor-targeted positron-emission tomography in biochemically recurrent prostate cancer-a systematic review and meta-analysis.Quantitative imaging in medicine and surgery · 2026Article
- The gastrin-releasing peptide receptor in oncology: a comprehensive review of recent advances in targeted radionuclide theranostics.Frontiers in oncology · 2026Review
- Advancements in Targeted Radiopharmaceuticals: Innovations in Diagnosis and Therapy for Enhanced Cancer Management.Chembiochem : a European journal of chemical biology · 2026Review
- GRPR-induced FAM135A expression promote perineural invasion in prostate cancer.Molecular cancer · 2025Article
- Article
- Distinctive biochemical properties of the μ-opioid receptor-corticotropin- releasing factor CRFPharmacological research · 2025Article
- De novo design of a fusion protein tool for GPCR research.Proceedings of the National Academy of Sciences of the United States of America · 2025Article
- Article
- Cryo-EM Structures and AlphaFold3 Models of Histamine Receptors Reveal Diverse Ligand Binding and G Protein Bias.Pharmaceuticals (Basel, Switzerland) · 2025Article
- Radiopharmaceuticals and their applications in medicine.Signal transduction and targeted therapy · 2025Review
- Overlapping features of atopic dermatitis and alopecia areata: from pathogenesis to treatment.Frontiers in immunology · 2025Review
- Evaluation of a tumor marker gastrin-releasing peptide precursor in the patients with kidney injuries.American journal of cancer research · 2025Article
- Peptide Aptamer-Paclitaxel Conjugates for Tumor Targeted Therapy.Pharmaceutics · 2024Review
- Gastrin-releasing peptide receptor (GRPR) as a novel biomarker and therapeutic target in prostate cancer.Annals of medicine · 2024Review
- Synthesis and Preclinical Evaluation of a Bispecific PSMA-617/RM2 Heterodimer Targeting Prostate Cancer.ACS medicinal chemistry letters · 2024Article
- Structure of endothelin ETCommunications biology · 2024Article
- IL-22 in Atopic Dermatitis.Cells · 2024Review
- Stabilizing Scaffold for Short Peptides Based on Knottins.Current cancer drug targets · 2024Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Gastrin releasing peptide receptor (GRPR), a member of the bombesin (BBN) G protein-coupled receptors, is aberrantly overexpressed in several malignant tumors, including those of the breast, prostate, pancreas, lung, and central nervous system. Additionally, it also mediates non-histaminergic itch and pathological itch conditions in mice. Thus, GRPR could be an attractive target for cancer and itch therapy. Here, we report the inactive state crystal structure of human GRPR in complex with the non-peptide antagonist PD176252, as well as two active state cryo-electron microscopy (cryo-EM) structures of GRPR bound to the endogenous peptide agonist gastrin-releasing peptide and the synthetic BBN analog [D-Phe
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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.