http://www.cnr.it/ontology/cnr/individuo/prodotto/ID98877
O6-methylguanine-DNA methyltransferase (MGMT) expression in acquired resistance of melanoma cells to temozolomide (TMZ) (Abstract/Poster in convegno)
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- O6-methylguanine-DNA methyltransferase (MGMT) expression in acquired resistance of melanoma cells to temozolomide (TMZ) (Abstract/Poster in convegno) (literal)
- Anno
- 2005-01-01T00:00:00+01:00 (literal)
- Alternative label
1)Alvino Ester; 2) Lacal Pedro; 2)Castiglia Daniele; 2)Caporaso Patrizia; 2)Caporali Simona; 2)Arcelli Diego; 2)Zambruno Gianna; 2)Bonmassar Enzo; D'Atri Stefania (2005)
O6-methylguanine-DNA methyltransferase (MGMT) expression in acquired resistance of melanoma cells to temozolomide (TMZ)
in XLVI Congresso Nazionale della Società Italiana di Cancerologia (SIC), Pisa, 24-27 Ottobre 2004
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- 1)Alvino Ester; 2) Lacal Pedro; 2)Castiglia Daniele; 2)Caporaso Patrizia; 2)Caporali Simona; 2)Arcelli Diego; 2)Zambruno Gianna; 2)Bonmassar Enzo; D'Atri Stefania (literal)
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- 24-27 Ottobre 2004, Pisa
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- 1) Institute of Neurobiology and Molecular Medicine, National Council of Research, Rome Italy
2) Istituto Dermopatico dell'Immacolata-IRCCS, Rome, Italy (literal)
- Titolo
- O6-methylguanine-DNA methyltransferase (MGMT) expression in acquired resistance of melanoma cells to temozolomide (TMZ) (literal)
- Abstract
- O6-METHYLGUANINE-DNA
METHYLTRANSFERASE (MGMT) EXPRESSION
IN ACQUIRED RESISTANCE OF MELANOMA
CELLS TO TEMOZOLOMIDE (TMZ)
Alvino E.1, Lacal P.M.2, Castiglia D.2, Caporaso P.2,
Caporali S.2, Arcelli D.2, Zambruno G.2, Bonmassar E.2,
D'Atri S.2
1Institute of Neurobiology and Molecular Medicine, National
Research Council, Rome, Italy; 2Istituto Dermopatico
dell'Immacolata (IDI-IRCCS), Rome, Italy.
Clinically achievable concentrations of TMZ, an antitumor
methylating agent presently in phase II/III clinical trials,
exert cytotoxic effects only in cells with a functional
mismatch repair (MMR) system and low MGMT activity.
Aim of this study was to elucidate TMZ-induced
molecular changes leading to acquired resistance to the
drug in melanoma cells. Three MMR-proficient melanoma
cell clones with low MGMT activity, derived from 3
different cell lines, were treated with 50 mM TMZ (daily
for 5 days, to mimic patient exposure to a single cycle of
chemotherapy), alone or in the presence of 5 mM O6-
benzylguanine (BG), a specific MGMT inhibitor. When
exponential growth resumed, the cells were tested for
sensitivity to TMZ or TMZ+BG, MGMT activity, and
expression of MMR proteins. Both TMZ- and TMZ+BGtreated
sublines showed a marked increase of MGMT
activity and resistance to TMZ alone, while the expression
of MMR proteins was nearly unaltered. The increase of
MGMT activity was dependent on increased levels of
MGMT mRNA and protein. However, the CpG
34 Cellular and molecular basis of cancer therapya
methylation pattern of the MGMT promoter was unaltered
in drug-treated sublines. Acquired resistance to TMZ was
only partially reversed by BG. Six additional TMZ- or
TMZ+BG-treated sublines were generated for each of the
three parental melanoma clones. All drug-treated sublines
showed increased MGMT activity, with the exception of
two sublines in the TMZ+BG group. However, also these
two sublines were resistant to TMZ.
In conclusion, treatment of melanoma cells with TMZ,
alone or combined with BG, rapidly induces drug
resistance mainly, but not exclusively, through upregulation
of MGMT activity. Studies are in progress to
identify genes differentially expressed in the parental
clones and drug-resistant sublines possibly involved in
MGMT-independent chemoresistance.
Supported by the Italian Ministry of Health. (literal)
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