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THE ANTIPROLIFERATIVE PROPERTIES OF 4-BENZYLPHENOXY ETHANAMINE DERIVATIVES ARE MEDIATED BY THE ANTIESTROGEN BINDING-SITE (ABS), WHEREAS THE ANTIESTROGENIC EFFECTS OF TRIFLUOPROMAZINE ARE NOT
被引:14
作者
:
POIROT, M
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,ENDOCR EXP LAB,INSERM,U168,F-31054 TOULOUSE,FRANCE
POIROT, M
GARNIER, M
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,ENDOCR EXP LAB,INSERM,U168,F-31054 TOULOUSE,FRANCE
GARNIER, M
BAYARD, F
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,ENDOCR EXP LAB,INSERM,U168,F-31054 TOULOUSE,FRANCE
BAYARD, F
RIVIERE, I
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,ENDOCR EXP LAB,INSERM,U168,F-31054 TOULOUSE,FRANCE
RIVIERE, I
TRAORE, M
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,ENDOCR EXP LAB,INSERM,U168,F-31054 TOULOUSE,FRANCE
TRAORE, M
WILSON, M
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,ENDOCR EXP LAB,INSERM,U168,F-31054 TOULOUSE,FRANCE
WILSON, M
FARGIN, A
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,ENDOCR EXP LAB,INSERM,U168,F-31054 TOULOUSE,FRANCE
FARGIN, A
FAYE, JC
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,ENDOCR EXP LAB,INSERM,U168,F-31054 TOULOUSE,FRANCE
FAYE, JC
机构
:
[1]
CHU RANGUEIL,ENDOCR EXP LAB,INSERM,U168,F-31054 TOULOUSE,FRANCE
[2]
UNIV TOULOUSE 3,CHIM BIOORGAN LAB,F-31062 TOULOUSE,FRANCE
来源
:
BIOCHEMICAL PHARMACOLOGY
|
1990年
/ 40卷
/ 03期
关键词
:
D O I
:
10.1016/0006-2952(90)90539-W
中图分类号
:
R9 [药学];
学科分类号
:
1007 ;
摘要
:
We compared the anti-proliferative properties of 4-benzylphenoxy-N ethyl morpholine (mor-pho-BPE) and trifluopromazine (TFP) on both the human breast cancer cell lines, MCF7, and its tamoxifen-resistant variant RTx6. We found that the calmodulin antagonist trifluopromazine (TFP) which bound ABS weakly, inhibited MCF7 cell growth but did not follow the relationship observed for diphenylmethane derivatives between MCF7-inhibitory potencies and their Ki. Regarding the tamoxifenresistant RTx6 cells, TFP but not morpho-BPE induced inhibition of the proliferation. Using a tritiated derivative of morpho-BPE, two distinct binding sites could be demonstrated. Indeed, a low affinity binding site was present in both cell lines whereas a high affinity binding site was mainly found in MCF7 cells although being in lower concentration (<10%) in rtx6 cells. Both tamoxifen and TFP displaced morpho-BPE from the two binding sites. The uptake and efflux of the tritiated drug were similar in the two cell lines. The drug did not appear to be metabolized. We concluded that TFP and morpho-BPE belong to distinct classes of molecules and that ABS mediates the anti-proliferative action of diphenylmethane derivatives but not the inhibitory effect of the calmodulin antagonist TFP. © 1990.
引用
收藏
页码:425 / 429
页数:5
相关论文
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CYTOPLASMIC AND NUCLEAR ESTRADIOL AND PROGESTERONE RECEPTORS IN HUMAN ENDOMETRIUM
BAYARD, F
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INSERM, RECH METAB MOLEC & PHYSIOPATHOL STEROIDES UNITE, BICETRE, FRANCE
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DAMILANO, S
ROBEL, P
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0
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INSERM, RECH METAB MOLEC & PHYSIOPATHOL STEROIDES UNITE, BICETRE, FRANCE
ROBEL, P
BAULIEU, EE
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INSERM, RECH METAB MOLEC & PHYSIOPATHOL STEROIDES UNITE, BICETRE, FRANCE
BAULIEU, EE
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A DIPHENYLMETHANE DERIVATIVE SPECIFIC FOR THE ANTIESTROGEN BINDING-SITE FOUND IN RAT-LIVER MICROSOMES
BRANDES, LJ
论文数:
0
引用数:
0
h-index:
0
机构:
MANITOBA CANC TREATMENT & RES FDN,MANITOBA INST CELL BIOL,WINNIPEG R3E OV9,MANITOBA,CANADA
MANITOBA CANC TREATMENT & RES FDN,MANITOBA INST CELL BIOL,WINNIPEG R3E OV9,MANITOBA,CANADA
BRANDES, LJ
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MANITOBA CANC TREATMENT & RES FDN,MANITOBA INST CELL BIOL,WINNIPEG R3E OV9,MANITOBA,CANADA
MANITOBA CANC TREATMENT & RES FDN,MANITOBA INST CELL BIOL,WINNIPEG R3E OV9,MANITOBA,CANADA
HERMONAT, MW
[J].
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[4]
FURTHER EVIDENCE FOR A BIOLOGICAL ROLE OF ANTI-ESTROGEN-BINDING SITES IN MEDIATING THE GROWTH INHIBITORY-ACTION OF DIPHENYLMETHANE DERIVATIVES
FARGIN, A
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
FARGIN, A
BAYARD, F
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
BAYARD, F
FAYE, JC
论文数:
0
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0
h-index:
0
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CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
FAYE, JC
TRAORE, M
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0
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0
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CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
TRAORE, M
POIROT, M
论文数:
0
引用数:
0
h-index:
0
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CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
POIROT, M
KLAEBE, A
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CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
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PERIE, JJ
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0
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0
机构:
CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
PERIE, JJ
[J].
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1988,
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[5]
SOLUBILIZATION OF A TAMOXIFEN-BINDING PROTEIN - ASSESSMENT OF ITS MOLECULAR MASS
FARGIN, A
论文数:
0
引用数:
0
h-index:
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机构:
UNIV PAUL SABATIER, CHU RANGUEIL, INSERM, U168, DEPT ENDOCRINOL, F-31054 TOULOUSE, FRANCE
FARGIN, A
FAYE, JC
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UNIV PAUL SABATIER, CHU RANGUEIL, INSERM, U168, DEPT ENDOCRINOL, F-31054 TOULOUSE, FRANCE
FAYE, JC
LEMAIRE, M
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BAYARD, F
POTIER, M
论文数:
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h-index:
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UNIV PAUL SABATIER, CHU RANGUEIL, INSERM, U168, DEPT ENDOCRINOL, F-31054 TOULOUSE, FRANCE
POTIER, M
BEAUREGARD, G
论文数:
0
引用数:
0
h-index:
0
机构:
UNIV PAUL SABATIER, CHU RANGUEIL, INSERM, U168, DEPT ENDOCRINOL, F-31054 TOULOUSE, FRANCE
BEAUREGARD, G
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FAYE JC, 1983, P NATL ACAD SCI-BIOL, V80, P3158, DOI 10.1073/pnas.80.11.3158
[7]
ANTI-ESTROGEN SPECIFIC, HIGH-AFFINITY SATURABLE BINDING-SITES IN RAT UTERINE CYTOSOL
FAYE, JC
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BAYARD, F
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BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,
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FAYE, JC
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FARGIN, A
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VALETTE, A
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VALETTE, A
BAYARD, F
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JORDAN VC, 1984, PHARMACOL REV, V36, P245
←
1
2
→
共 19 条
[1]
CYTOPLASMIC AND NUCLEAR ESTRADIOL AND PROGESTERONE RECEPTORS IN HUMAN ENDOMETRIUM
BAYARD, F
论文数:
0
引用数:
0
h-index:
0
机构:
INSERM, RECH METAB MOLEC & PHYSIOPATHOL STEROIDES UNITE, BICETRE, FRANCE
BAYARD, F
DAMILANO, S
论文数:
0
引用数:
0
h-index:
0
机构:
INSERM, RECH METAB MOLEC & PHYSIOPATHOL STEROIDES UNITE, BICETRE, FRANCE
DAMILANO, S
ROBEL, P
论文数:
0
引用数:
0
h-index:
0
机构:
INSERM, RECH METAB MOLEC & PHYSIOPATHOL STEROIDES UNITE, BICETRE, FRANCE
ROBEL, P
BAULIEU, EE
论文数:
0
引用数:
0
h-index:
0
机构:
INSERM, RECH METAB MOLEC & PHYSIOPATHOL STEROIDES UNITE, BICETRE, FRANCE
BAULIEU, EE
[J].
JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM,
1978,
46
(04)
: 635
-
648
[2]
A DIPHENYLMETHANE DERIVATIVE SPECIFIC FOR THE ANTIESTROGEN BINDING-SITE FOUND IN RAT-LIVER MICROSOMES
BRANDES, LJ
论文数:
0
引用数:
0
h-index:
0
机构:
MANITOBA CANC TREATMENT & RES FDN,MANITOBA INST CELL BIOL,WINNIPEG R3E OV9,MANITOBA,CANADA
MANITOBA CANC TREATMENT & RES FDN,MANITOBA INST CELL BIOL,WINNIPEG R3E OV9,MANITOBA,CANADA
BRANDES, LJ
HERMONAT, MW
论文数:
0
引用数:
0
h-index:
0
机构:
MANITOBA CANC TREATMENT & RES FDN,MANITOBA INST CELL BIOL,WINNIPEG R3E OV9,MANITOBA,CANADA
MANITOBA CANC TREATMENT & RES FDN,MANITOBA INST CELL BIOL,WINNIPEG R3E OV9,MANITOBA,CANADA
HERMONAT, MW
[J].
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,
1984,
123
(02)
: 724
-
728
[3]
Dixon M., 1964, ENZYMES, P328
[4]
FURTHER EVIDENCE FOR A BIOLOGICAL ROLE OF ANTI-ESTROGEN-BINDING SITES IN MEDIATING THE GROWTH INHIBITORY-ACTION OF DIPHENYLMETHANE DERIVATIVES
FARGIN, A
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
FARGIN, A
BAYARD, F
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
BAYARD, F
FAYE, JC
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
FAYE, JC
TRAORE, M
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
TRAORE, M
POIROT, M
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
POIROT, M
KLAEBE, A
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
KLAEBE, A
PERIE, JJ
论文数:
0
引用数:
0
h-index:
0
机构:
CHU RANGUEIL,DEPT ENDOCRINOL,INSERM,4168,CHEMIN VALLON,F-31054 TOULOUSE,FRANCE
PERIE, JJ
[J].
CHEMICO-BIOLOGICAL INTERACTIONS,
1988,
66
(1-2)
: 101
-
109
[5]
SOLUBILIZATION OF A TAMOXIFEN-BINDING PROTEIN - ASSESSMENT OF ITS MOLECULAR MASS
FARGIN, A
论文数:
0
引用数:
0
h-index:
0
机构:
UNIV PAUL SABATIER, CHU RANGUEIL, INSERM, U168, DEPT ENDOCRINOL, F-31054 TOULOUSE, FRANCE
FARGIN, A
FAYE, JC
论文数:
0
引用数:
0
h-index:
0
机构:
UNIV PAUL SABATIER, CHU RANGUEIL, INSERM, U168, DEPT ENDOCRINOL, F-31054 TOULOUSE, FRANCE
FAYE, JC
LEMAIRE, M
论文数:
0
引用数:
0
h-index:
0
机构:
UNIV PAUL SABATIER, CHU RANGUEIL, INSERM, U168, DEPT ENDOCRINOL, F-31054 TOULOUSE, FRANCE
LEMAIRE, M
BAYARD, F
论文数:
0
引用数:
0
h-index:
0
机构:
UNIV PAUL SABATIER, CHU RANGUEIL, INSERM, U168, DEPT ENDOCRINOL, F-31054 TOULOUSE, FRANCE
BAYARD, F
POTIER, M
论文数:
0
引用数:
0
h-index:
0
机构:
UNIV PAUL SABATIER, CHU RANGUEIL, INSERM, U168, DEPT ENDOCRINOL, F-31054 TOULOUSE, FRANCE
POTIER, M
BEAUREGARD, G
论文数:
0
引用数:
0
h-index:
0
机构:
UNIV PAUL SABATIER, CHU RANGUEIL, INSERM, U168, DEPT ENDOCRINOL, F-31054 TOULOUSE, FRANCE
BEAUREGARD, G
[J].
BIOCHEMICAL JOURNAL,
1988,
256
(01)
: 229
-
236
[6]
FAYE JC, 1983, P NATL ACAD SCI-BIOL, V80, P3158, DOI 10.1073/pnas.80.11.3158
[7]
ANTI-ESTROGEN SPECIFIC, HIGH-AFFINITY SATURABLE BINDING-SITES IN RAT UTERINE CYTOSOL
FAYE, JC
论文数:
0
引用数:
0
h-index:
0
FAYE, JC
LASSERRE, B
论文数:
0
引用数:
0
h-index:
0
LASSERRE, B
BAYARD, F
论文数:
0
引用数:
0
h-index:
0
BAYARD, F
[J].
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS,
1980,
93
(04)
: 1225
-
1231
[8]
ANTIESTROGENS, DIFFERENT SITES OF ACTION THAN THE ESTROGEN-RECEPTOR
FAYE, JC
论文数:
0
引用数:
0
h-index:
0
FAYE, JC
FARGIN, A
论文数:
0
引用数:
0
h-index:
0
FARGIN, A
VALETTE, A
论文数:
0
引用数:
0
h-index:
0
VALETTE, A
BAYARD, F
论文数:
0
引用数:
0
h-index:
0
BAYARD, F
[J].
HORMONE RESEARCH,
1987,
28
(2-4)
: 202
-
211
[9]
GULINO A, 1986, CANCER RES, V46, P6274
[10]
JORDAN VC, 1984, PHARMACOL REV, V36, P245
←
1
2
→