ArticleScientific reports2019
The β2-adrenergic receptor antagonist ICI-118,551 blocks the constitutively activated HIF signalling in hemangioblastomas from von Hippel-Lindau disease.
Article in Scientific reports, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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18 citing papers in PubMed, 25 citations in OpenAlex.
- Dysregulation of the ubiquitin-proteasome system in von Hippel-Lindau syndrome: molecular insights and clinical perspectives.Clinical and experimental medicine · 2025Review
- Local tumor control and neurological outcomes after surgery for spinal hemangioblastomas in sporadic and von Hippel-Lindau disease: A multicenter study.Neuro-oncology · 2025Observational
- S- and R-Carvedilol Prevent Benzo(a)pyrene-Induced Lung Carcinogenesis.Thoracic cancer · 2025Article
- Spinal cord hemangioblastomas in von Hippel-Lindau disease.Neuro-oncology advances · 2024Review
- The Role of Radiotherapy, Chemotherapy, and Targeted Therapies in Adult Intramedullary Spinal Cord Tumors.Cancers · 2024Review
- β-Adrenoceptors in Cancer: Old Players and New Perspectives.Handbook of experimental pharmacology · 2024Review
- β-Adrenoreceptors as Therapeutic Targets for Ocular Tumors and Other Eye Diseases-Historical Aspects and Nowadays Understanding.International journal of molecular sciences · 2023Review
- Repurposing beta-blockers for combinatory cancer treatment: effects on conventional and immune therapies.Frontiers in pharmacology · 2023Review
- Propranolol: A "Pick and Roll" Team Player in Benign Tumors and Cancer Therapies.Journal of clinical medicine · 2022Review
- In Vitro Toxicological Profile of Labetalol-Folic Acid/Folate Co-Administration in H9c2(2-1) and HepaRG Cells.Medicina (Kaunas, Lithuania) · 2022Article
- β3-Adrenoceptor, a novel player in the round-trip from neonatal diseases to cancer: Suggestive clues from embryo.Medicinal research reviews · 2022Review
- The Role of Propranolol as a Repurposed Drug in Rare Vascular Diseases.International journal of molecular sciences · 2022Review
- Blockade of β2-Adrenergic Receptor Reduces Inflammation and Oxidative Stress in Clear Cell Renal Cell Carcinoma.International journal of molecular sciences · 2022Article
- Article
- An Extract fromAntioxidants (Basel, Switzerland) · 2021Article
- Central Nervous System Hemangioblastoma in a Pediatric Patient Associated With Von Hippel-Lindau Disease: A Case Report and Literature Review.Frontiers in oncology · 2021Review
- Targeting β2-Adrenergic Receptors Shows Therapeutical Benefits in Clear Cell Renal Cell Carcinoma from Von Hippel-Lindau Disease.Journal of clinical medicine · 2020Article
- Von Hippel-Lindau Disease: Current Challenges and Future Prospects.OncoTargets and therapy · 2020Review
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Authors and funding
8 authors at 5 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
One of the major consequences of the lack of a functional VHL protein in von Hippel-Lindau disease, a rare cancer, is the constitutive activation of the HIF pathway. This activation ends up in the generation of Central Nervous System (CNS) Hemangioblastomas among other tumours along the lifespan of the patient. Nowadays, only surgery has been proven efficient as therapy since the systemic attempts have failed. Propranolol, a non-specific β1-and β2-adrenergic receptor antagonist, was recently designated as the first therapeutic (orphan) drug for VHL disease. Nevertheless, its β1 affinity provokes the decrease in blood pressure, being not recommended for low or regular blood pressure VHL patients. In order to overcome the β1-drawback, the properties of a high specific β2-adrenergic receptor blocker named ICI-118,551 have been studied. ICI-118,551 was able to decrease Hemangioblastomas cell viability in a specific manner, by triggering apoptosis. Moreover, ICI-118,551 also impaired the nuclear internalization of HIF-1α in Hemangioblastomas and hypoxic primary endothelial cells, reducing significantly the activation of HIF-target genes and halting the tumour-related angiogenic processes. In this work, we demonstrate the therapeutical properties of ICI-118,551 in VHL-derived CNS-Hemangioblastoma primary cultures, becoming a promising drug for VHL disease and other HIF-related diseases.
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