ArticleProceedings of the National Academy of Sciences of the United States of America2005
Antagonists of growth hormone-releasing hormone cross the blood-brain barrier: a potential applicability to treatment of brain tumors.
Article in Proceedings of the National Academy of Sciences of the United States of America, 2005. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
26 citing papers in PubMed, 43 citations in OpenAlex.
- Mesenchymal Stem cell therapy with GHRH receptor analog resolves post-stroke vasogenic edema via modulating AQP4 and mitochondria-ER crosstalk.Journal of translational medicine · 2026Article
- Growth hormone-releasing hormone attenuates amyloid deposition and neuroinflammation in Alzheimer's disease models.Cell death & disease · 2026Article
- Therapeutic potential of growth hormone-releasing hormone analogues in cardiovascular and cerebrovascular diseases: mechanisms and preclinical evidence.Frontiers in pharmacology · 2026Review
- Evaluation of the Therapeutic Potential of Synthetic Growth Hormone-Releasing Hormone Antagonist MIA-690 as a Cognitive Modulator in a Mouse Model of Gulf War Illness.International journal of molecular sciences · 2025Article
- GHRH and its analogues in central nervous system diseases.Reviews in endocrine & metabolic disorders · 2025Review
- Growth hormone-releasing hormone and cancer.Reviews in endocrine & metabolic disorders · 2025Review
- A longer time to relapse is associated with a larger increase in differences between paired primary and recurrent IDH wild-type glioblastomas at both the transcriptomic and genomic levels.Acta neuropathologica communications · 2024Article
- Growth hormone-releasing hormone antagonists protect against hydrochloric acid-induced endothelial injury in vitro.Environmental toxicology and pharmacology · 2023Article
- Growth Hormone-Releasing Hormone in Endothelial Inflammation.Endocrinology · 2022Review
- Identification of growth hormone receptor as a relevant target for precision medicine in low-EGFR expressing glioblastoma.Clinical and translational medicine · 2022Article
- Agonistic analog of growth hormone-releasing hormone promotes neurofunctional recovery and neural regeneration in ischemic stroke.Proceedings of the National Academy of Sciences of the United States of America · 2021Article
- A potentially effective drug for patients with recurrent glioma: sermorelin.Annals of translational medicine · 2021Article
- Magnetoelectric nanoparticles for delivery of antitumor peptides into glioblastoma cells by magnetic fields.Nanomedicine (London, England) · 2018Article
- Prognosis in human glioblastoma based on expression of ligand growth hormone-releasing hormone, pituitary-type growth hormone-releasing hormone receptor, its splicing variant receptors, EGF receptor and PTEN genes.Journal of cancer research and clinical oncology · 2014Article
- Potentiation of cytotoxic chemotherapy by growth hormone-releasing hormone agonists.Proceedings of the National Academy of Sciences of the United States of America · 2014Article
- Suppression of the proliferation of human U-87 MG glioblastoma cells by new antagonists of growth hormone-releasing hormone in vivo and in vitro.Targeted oncology · 2013Article
- Growth hormone releasing hormone (GHRH) signaling modulates intermittent hypoxia-induced oxidative stress and cognitive deficits in mouse.Journal of neurochemistry · 2013Article
- Protective effects of an anti-melanocortin-4 receptor scFv derivative in lipopolysaccharide-induced cachexia in rats.Journal of cachexia, sarcopenia and muscle · 2013Article
- Inhibition of U-87 MG glioblastoma by AN-152 (AEZS-108), a targeted cytotoxic analog of luteinizing hormone-releasing hormone.Oncotarget · 2013Article
- Targeting potassium channels for increasing delivery of imaging agents and therapeutics to brain tumors.Frontiers in pharmacology · 2013Article
Corrections and comments
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Authors and funding
4 authors at 3 institutions in 1 country.
Funding
Abstract
Hypothalamic growth hormone (GH)-releasing hormone (GHRH) stimulates the synthesis and release of GH from the pituitary gland. GHRH and its mRNA are also found in human cancers of the breast, ovary, prostate, lung, and other tumors, suggesting that GHRH is also a tumor growth factor. Various studies show that GHRH antagonists have antiproliferative effects in many tumor models; however, glioblastomas were examined only recently. Previous studies have demonstrated that s.c. administration of GHRH antagonist (JV-1-36) inhibited growth of s.c. U-87MG human glioblastomas and increased survival of nude mice with orthotopic implants of glioblastomas. Although treatment with JV-1-36 reduced tumorigenicity, it is not known whether peripherally administered GHRH antagonists can cross the blood-brain barrier. Brain endothelial cells joined by tight junctions form the blood-brain barrier, a "barrier" between the general circulation and the CNS. In this study, we administered a GHRH antagonist (JV-1-42) and showed that, after i.v. injection, iodinated JV-1-42 (131I-JV-1-42) enters the brain intact at a rate of 0.8514 mocrol/g per min with a serum half-life of 12.2 min. A one-site binding hyperbolic model indicated that the maximal percent of i.v. dose taken up per gram of brain was 0.41%. Coinjection of unlabeled JV-1-42 indicated that the transport from blood to brain is not saturable; however, transport from brain to blood is saturable and involves P-glycoprotein. Taken together, these results demonstrate that i.v.-administered 131I-JV-1-42 readily crosses the blood-brain barrier and accumulates in the brain. This finding indicates that GHRH antagonists could provide a potential treatment for malignant glioblastomas.
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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.