ArticleBritish journal of pharmacology2001
Pharmacological and biochemical characterization of adenosine receptors in the human malignant melanoma A375 cell line.
Article in British journal of pharmacology, 2001. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 35 papers.
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Who cites it
35 citing papers in PubMed, 122 citations in OpenAlex.
- IFC-305, an adenosine derivative, inhibits the osteolytic metastases of triple-negative breast cancer.Journal of bone oncology · 2025Article
- Adenosine and Its Receptors in the Pathogenesis and Treatment of Inflammatory Skin Diseases.International journal of molecular sciences · 2024Review
- Ultrasonic-assisted synthesis and antitumor evaluation of novel variant heterocyclic compounds based on piperidine ring.Future medicinal chemistry · 2024Article
- Ultrasonic-induced synthesis of novel diverse arylidenesRSC advances · 2023Article
- Role of adenosine A2a receptor in cancers and autoimmune diseases.Immunity, inflammation and disease · 2023Review
- A1 adenosine receptor antagonist induces cell apoptosis in KYSE-30 and YM-1 esophageal cancer cell lines.BioMedicine · 2023Article
- Sentinel Lymph Node Gene Expression Signature Predicts Recurrence-Free Survival in Cutaneous Melanoma.Cancers · 2022Article
- Inhibition of Metastasis by Polypyridyl Ru(II) Complexes through Modification of Cancer Cell Adhesion -Journal of medicinal chemistry · 2022Article
- Cancer-Related Somatic Mutations in Transmembrane Helices Alter Adenosine A1 Receptor Pharmacology.Molecules (Basel, Switzerland) · 2022Article
- Metabolic Interplay between the Immune System and Melanoma Cells: Therapeutic Implications.Biomedicines · 2021Review
- Differential effect of adenosine on rhabdomyosarcoma migration and proliferation.Archives of medical science : AMS · 2020Article
- Involvement of AJournal of molecular neuroscience : MN · 2019Article
- ADA activity is decreased in lymphocytes from patients with advanced stage of lung cancer.Medical oncology (Northwood, London, England) · 2019Article
- Prognostic Impact of Adenosine Receptor 2 (A2aR) and Programmed Cell Death Ligand 1 (PD-L1) Expression in Colorectal Cancer.BioMed research international · 2019Article
- Targeting Adenosine Receptor Signaling in Cancer Immunotherapy.International journal of molecular sciences · 2018Review
- AMedicinal research reviews · 2018Review
- Discovery of benzothiazolylquinoline conjugates as novel human ARoyal Society open science · 2018Article
- Multifaceted Effects of Extracellular Adenosine Triphosphate and Adenosine in the Tumor-Host Interaction and Therapeutic Perspectives.Frontiers in immunology · 2017Review
- Inosine Released from Dying or Dead Cells Stimulates Cell ProliferationFrontiers in immunology · 2017Article
- Hide and seek: a comparative autoradiographic in vitro investigation of the adenosine A3 receptor.European journal of nuclear medicine and molecular imaging · 2015Article
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Authors and funding
8 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
1. The present work characterizes, from a pharmacological and biochemical point of view, adenosine receptors in the human malignant melanoma A375 cell line. 2. Adenosine receptors were detected by RT - PCR experiments. A1 receptors were characterized using [3H]-DPCPX binding with a KD of 1.9+/-0.2 nM and Bmax of 23+/-7 fmol x mg(-1) of protein. A2A receptors were studied with [3H]-SCH 58261 binding and revealed a KD of 5.1+/-0.2 nM and a Bmax of 220+/-7 fmol x mg(-1) of protein. A3 receptors were studied with the new A3 adenosine receptor antagonist [3H]-MRE 3008F20, the only A3 selective radioligand currently available. Saturation experiments revealed a single high affinity binding site with KD of 3.3+/-0.7 nM and Bmax of 291+/-50 fmol x mg(-1) of protein. 3. The pharmacological profile of radioligand binding on A375 cells was established using typical adenosine ligands which displayed a rank order of potency typical of the different adenosine receptor subtype. 4. Thermodynamic data indicated that radioligand binding to adenosine receptor subtypes in A375 cells was entropy- and enthalpy-driven. 5. In functional assays the high affinity A2A agonists HE-NECA, CGS 21680 and A2A - A2B agonist NECA were able to increase cyclic AMP accumulation in A375 cells whereas A3 agonists Cl-IB-MECA, IB-MECA and NECA were able to stimulate Ca2+ mobilization. In conclusion, all these data indicate, for the first time, that adenosine receptors with a pharmacological and biochemical profile typical of the A1, A2A, A2B and A3 receptor subtype are present on A375 melanoma cell line.
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