P2X7 receptor activation mediates organic cation uptake into human myeloid leukaemic KG-1 cells

Safina Gadeock, Aleta Pupovac, Vanessa Sluyter, Mari Spildrejorde, Ronald Sluyter

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18 Citations (Scopus)


The P2X7 purinergic receptor is an ATP-gated cation channel with an emerging role in neoplasia. In this study we demonstrate that the human KG-1 cell line, a model of acute myelogenous leukaemia, expresses functional P2X7. RT-PCR and immunochemical techniques demonstrated the presence of P2X7 mRNA and protein respectively in KG-l cells, as well as in positive control multiple myeloma RPMI 8226 cells. Flow cytometric measurements demonstrated that ATP induced ethidium+ uptake into KG-l cells suspended in sucrose medium (EC50 of ∼3 μM), but not into cells in NaCl medium. In contrast, ATP induced ethidium+ uptake into RPMI 8226 cells suspended in either sucrose or NaCl medium (EC50 of ∼3 or ∼99 μM, respectively), as well as into RPMI 8226 cells in KCl medium (EC50 of ∼18 μM). BzATP and to a lesser extent ATPγS and αβ-methylene ATP, but not ADP or UTP, also induced ethidium+ uptake into KG-1 cells. ATP-induced ethidium+ uptake was completely impaired by the P2X7 antagonists, AZ10606120 and A-438079. ATP-induced ethidium+uptake was also impaired by probenecid but not by carbenoxolone, both pannexin-1 antagonists. ATP induced YO-PRO-12+ and propidium2+ uptake into KG-1 cells. Finally, sequencing of full-length P2X7 cDNA identified several single nucleotide polymorphisms (SNPs) in KG-1 cells including H155Y, A348T, T357S and Q460R. RPMI 8226 cells contained A348T, A433V and H521Q SNPs. In conclusion, the KG-1 cell line expresses functional P2X7. This cell line may help elucidate the signalling pathways involved in P2X7-induced survival and invasiveness of myeloid leukaemic cells.

Original languageEnglish
Pages (from-to)669-676
Number of pages8
JournalPurinergic Signalling
Issue number4
Publication statusPublished - Dec 2012
Externally publishedYes


  • Acute myelogenous leukaemia
  • Cation channel
  • Extracellular ATP
  • Purinergic receptor
  • Single nucleotide polymorphism

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