Abstract
The growth inhibitory effects of Breqinar Sodium (DUP-785; NSC 368390) in 7 different cell lines were related to growth rates and to the inhibition of dihydroorotic acid dehydrogenase (DHO-DH) activity. IC50 values were between 0.2 and 5.8 μM; the fastest growing cell line was least sensitive. Despite a large variation in sensitivity, basal activity of DHO-DH showed little variation (only 2-fold) between the different cell lines. Residual activity of DHO-DH in the presence of Brequinar Sodium varied 30-fold. Drug sensitivity correlated with this residual DHO-DH activity; DHO-DH activity was only slightly inhibited by Breqinar Sodium in the most resistant lines, and almost completely in the most sensitive.
Original language | English (US) |
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Pages (from-to) | 123-127 |
Number of pages | 5 |
Journal | Cancer Letters |
Volume | 46 |
Issue number | 2 |
DOIs | |
State | Published - Jul 15 1989 |
Externally published | Yes |
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Keywords
- Breqinar Sodium (DUP-785)
- dihydroorotic acid dehydrogenase
- growth inhibition
- pyrimidine de novo
ASJC Scopus subject areas
- Cancer Research
- Molecular Biology
- Oncology
Cite this
The relation between inhibition of cell growth and of dihydroorotic acid dehydrogenase by Brequinar Sodium. / de Kant, E.; Pinedo, H. M.; Laurensse, E.; Peters, G. J.
In: Cancer Letters, Vol. 46, No. 2, 15.07.1989, p. 123-127.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - The relation between inhibition of cell growth and of dihydroorotic acid dehydrogenase by Brequinar Sodium
AU - de Kant, E.
AU - Pinedo, H. M.
AU - Laurensse, E.
AU - Peters, G. J.
PY - 1989/7/15
Y1 - 1989/7/15
N2 - The growth inhibitory effects of Breqinar Sodium (DUP-785; NSC 368390) in 7 different cell lines were related to growth rates and to the inhibition of dihydroorotic acid dehydrogenase (DHO-DH) activity. IC50 values were between 0.2 and 5.8 μM; the fastest growing cell line was least sensitive. Despite a large variation in sensitivity, basal activity of DHO-DH showed little variation (only 2-fold) between the different cell lines. Residual activity of DHO-DH in the presence of Brequinar Sodium varied 30-fold. Drug sensitivity correlated with this residual DHO-DH activity; DHO-DH activity was only slightly inhibited by Breqinar Sodium in the most resistant lines, and almost completely in the most sensitive.
AB - The growth inhibitory effects of Breqinar Sodium (DUP-785; NSC 368390) in 7 different cell lines were related to growth rates and to the inhibition of dihydroorotic acid dehydrogenase (DHO-DH) activity. IC50 values were between 0.2 and 5.8 μM; the fastest growing cell line was least sensitive. Despite a large variation in sensitivity, basal activity of DHO-DH showed little variation (only 2-fold) between the different cell lines. Residual activity of DHO-DH in the presence of Brequinar Sodium varied 30-fold. Drug sensitivity correlated with this residual DHO-DH activity; DHO-DH activity was only slightly inhibited by Breqinar Sodium in the most resistant lines, and almost completely in the most sensitive.
KW - Breqinar Sodium (DUP-785)
KW - dihydroorotic acid dehydrogenase
KW - growth inhibition
KW - pyrimidine de novo
UR - http://www.scopus.com/inward/record.url?scp=0024410414&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0024410414&partnerID=8YFLogxK
U2 - 10.1016/0304-3835(89)90019-0
DO - 10.1016/0304-3835(89)90019-0
M3 - Article
C2 - 2546667
AN - SCOPUS:0024410414
VL - 46
SP - 123
EP - 127
JO - Cancer Letters
JF - Cancer Letters
SN - 0304-3835
IS - 2
ER -