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Drug-Target Interaction

Drug

show drug details
PubChem ID:2733525
Structure:
Synonyms:
(Z)-(2-(4-(1,2-Diphenylbut-1-enyl)phenoxy)ethyl)dimethylammonium dihydrogen 2-hydroxypropane-1,2,3-tricarboxylate
(Z)-1-(p-Dimethylaminoethoxyphenyl)-1,2-diphenyl-1-butene
(Z)-2-(p-(1,2-Diphenyl-1-butenyl)phenoxy)-N,N-dimethylethylamine citrate (1:1)
10540-29-1
2-{4-[(1Z)-1,2-diphenylbut-1-en-1-yl]phenoxy}-N,N-dimethylethanamine 2-hydroxypropane-1,2,3-tricarboxylate (salt)
54965-24-1
7244-97-5
Ambap2118
Apo-Tamox
CAS-54965-24-1
CCRIS 6718
D00966
EINECS 259-415-2
Emblon
Ethanamine, 2-(4-(1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethyl, (Z)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
Ethanamine, 2-(4-(1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethyl-, (Z)-, 2-hydroxy-1,2,3-propanetricarboxylate
Ethanamine, 2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethyl-, (Z)-, 2-hydroxy-1,2,3-propane-tricarboxylate (1:1)
Ethanamine, 2-[4-(1,2-diphenyl-1-butenyl)phenoxy]-N,N-dimethyl-, (Z)-, 2-hydroxy-1,2,3-propanetricarboxylate (1:1)
Ethylamine, 2-(p-(1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethyl-, citrate
Ethylamine, 2-(p-(1,2-diphenyl-1-butenyl)phenoxy)-N,N-dimethyl-, citrate (Z)-
EU-0101203
Farmifeno
Genox
Ginarsan
I.C.I. 46474 citrate
ICI 46,474
ICI 46474
ICI 46474 citrate
ICI-46474
Jenoxifen
Kessar
Ledertam
Lopac-T-9262
LS-68202
MLS001055370
MLS002154210
N,N-Dimethyl-2-(p-(1,2-diphenyl-1-butenyl)phenoxy)ethylamine citrate
NCGC00016206-01
NCGC00016206-02
NCGC00024928-02
NCGC00094450-01
NCGC00094450-02
NCGC00094450-03
NCGC00094450-04
Nolgen
Noltam
Nolvadex
Nolvadex (TN)
Nourytan
Noxitem
NSC 180973
NSC180973
Oncotam
Prestwick_458
SMR000677949
Soltamox
SPECTRUM1500557
T9262_SIGMA
Tafoxen
Tamax
Tamofen
Tamoplex
Tamox-Puren
Tamoxasta
TAMOXIFEN
Tamoxifen citrate
TAMOXIFEN CITRATE (1:1)
TAMOXIFEN CITRATE (1:X)
Tamoxifen citrate (JAN/USP)
Tamoxifen citrate salt
Tamoxifen citrate [USAN:JAN]
Tamoxifen, citrate salt
Taxus
Terimon
TMX
trans-1-(p-beta-Dimethylaminoethoxyphenyl)-1,2-diphenylbut-1-ene citrate
Z-Tamoxifen citrate
Zemide
Zitazonium
Zynoplex
ATC-Codes:

Target

show target details
Uniprot ID:Q9UBT1_HUMAN
Synonyms:
Estrogen receptor
EC-Numbers:-
Organism:Homo sapiens
Human
PDB IDs:-

Binding Affinities:

Ki: Kd:Ic 50:Ec50/Ic50:
----
----

References:

12771030
Resveratrol activates adenylyl-cyclase in human breast cancer cells: a novel, estrogen receptor-independent cytostatic mechanism.. Abdalla M El-Mowafy; Moussa Alkhalaf (2003) Carcinogenesis display abstract
Resveratrol (RSVL) is a well-established chemopreventive agent in human breast cancer models. The molecular basis of its action is far less characterized. We investigated the effects of RSVL on activity of adenylate- and guanylate-cyclase (AC, GC) enzymes; two known cytostatic cascades in MCF-7 breast cancer cells. RSVL increased cAMP levels in both time- and concentration-dependent manners (t(1/2), 6.2 min; EC(50) 0.8 micro M). In contrast, it had no effect on cGMP levels. The stimulatory effects for RSVL on AC were not altered either by the protein synthesis inhibitor (actinomycin-D, 5 micro M) or the estrogen-receptor (ER) blockers (tamoxifen and ICI182,780, 1 micro M each). Likewise, cAMP formation by RSVL was insensitive to either the broad-spectrum phosphodiesterase (PDE) inhibitor (IBMX, 0.5 mM) or the cAMP-specific PDE inhibitor (rolipram, 10 micro M). Instead, these PDE inhibitors significantly augmented maximal cAMP formation by RSVL. Parallel experiments showed that either RSVL or rolipram inhibited the proliferation of these cells in a concentration-responsive manner. Further, concurrent treatment with RSVL and rolipram significantly enhanced their individual cytotoxic responses. The antiproliferative effects were appreciably reversed by the kinase-A inhibitors, Rp-cAMPS (100-300 micro M) or KT-5720 (10 micro M). Pretreatment with the cPLA(2) inhibitor arachidonyl trifluoromethyl ketone (10 micro M) markedly antagonized the cytotoxic effects of RSVL, but had no effect on that of rolipram. Altogether, the present study demonstrates, for the first time, that the chemotherapeutic agent RSVL is an agonist for the cAMP/kinase-A system, a documented pro-apoptic and cell-cycle suppressor in breast cancer cells.
7954293
The potential for hormonal prevention trials.. L G Ford; O W Brawley; J A Perlman; S G Nayfield; K A Johnson; B S Kramer (1994) Cancer display abstract
Breast and prostate cancer are significant causes of morbidity and mortality and are very similar in etiology, epidemiology, and modalities of treatment. Investigational strategies in the prevention of these malignancies also have strong parallels. The National Cancer Institute is sponsoring several large scale clinical trials involving hormonal manipulation and cancer prevention. In the Breast Cancer Prevention Trial, 16,000 women at high risk for breast cancer are being randomized to receive the antiestrogen agent tamoxifen or placebo for 5 years in an effort to determine if breast cancer development can be inhibited. In a similar trial, the Prostate Cancer Prevention Trial, 18,000 men older than 55 years of age will be randomized to receive finasteride, a 5-alpha-reductase inhibitor, or placebo to determine if inhibition of dihydrotestosterone synthesis in the prostate over a prolonged period will lead to a decreased incidence of prostate cancer. Both clinical trials offer the possibility of demonstrating that a hormonal intervention can decrease an individual's risk of developing breast or prostate cancer. They also have the potential of providing critical information about cancer risk, etiology, screening, and genetics, as well as quantifying the risks and benefits of specific preventive interventions.