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Title: The human immunodeficiency virus(HIV) inhibitor 9-(2-phosphonylmethoxyethyl)adenine (PMEA) is a strong inducer of differentiation of several tumor cell lines
Authors: Balzarini, Jan ×
Verstuyf, Annemieke
Hatse, Sigrid
Goebels, Jozef
Sobis, H
Vandeputte, Michel
De Clercq, Erik #
Issue Date: Mar-1995
Series Title: International Journal of Cancer vol:61 issue:1 pages:130-7
Abstract: 9-(2-phosphonylmethoxyethyl)adenine (PMEA) is the prototype compound of a series of acyclic nucleoside phosphonate derivatives endowed with potent and selective anti-retroviral activity in vitro and in vivo. We have now found that PMEA is also a potent inducer of differentiation of a number of tumor cells, including human erythroleukemia K562 cells, rat choriocarcinoma RCHO cells and human acute promyelocytic leukemic HL-60 cells. At 10 microM PMEA, rat RCHO cell cultures could be almost fully differentiated, and at 50 microM PMEA, approximately 50% of the K562 cells could be triggered to produce hemoglobin. The differentiating activity of butyric acid was at least partially additive to that of PMEA when both drugs were combined in K562 cell cultures. PMEA needs to be present for at least 2 or 3 days in the K562 cell cultures to achieve optimal differentiating activity. This suggests that either a PMEA metabolite and/or its anti-metabolic effects may be responsible for differentiation of the tumor cells.
ISSN: 0020-7136
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Laboratory of Virology and Chemotherapy (Rega Institute)
Clinical and Experimental Endocrinology
Laboratory of Experimental Transplantation
Laboratory of Experimental Oncology
× corresponding author
# (joint) last author

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