Nuclear receptors and their selective pharmacologic modulators
Nuclear receptors are ligand-activated transcription factors and include the receptors for
steroid hormones, lipophilic vitamins, sterols, and bile acids. These receptors serve as …
steroid hormones, lipophilic vitamins, sterols, and bile acids. These receptors serve as …
Cellular and molecular pharmacology of antiestrogen action and resistance
R Clarke, F Leonessa, JN Welch, TC Skaar - Pharmacological reviews, 2001 - ASPET
Antiestrogen therapy remains one of the most widely used and effective treatments for the
management of endocrine responsive breast cancers. This reflects the ability of …
management of endocrine responsive breast cancers. This reflects the ability of …
ICI 182,780 (Faslodex™) development of a novel,“pure” antiestrogen
A Howell, CK Osborne, C Morris… - … International Journal of …, 2000 - Wiley Online Library
BACKGROUND The nonsteroidal antiestrogen tamoxifen is well established as an effective
treatment for patients with breast carcinoma, both for the treatment of metastatic disease and …
treatment for patients with breast carcinoma, both for the treatment of metastatic disease and …
Comparison of the Short-Term Biological Effects of 7α-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)-nonyl]estra-1,3,5, (10)-triene-3,17β-diol (Faslodex) versus Tamoxifen in …
JF Robertson, RI Nicholson, NJ Bundred, E Anderson… - Cancer research, 2001 - AACR
Abstract 7α-[9-(4, 4, 5, 5, 5-Pentafluoropentylsulfinyl)-nonyl] estra-1, 3, 5,(10)-triene-3, 17β-
diol (ICI 182,780; Faslodex) is a novel steroidal antiestrogen. This partially blind …
diol (ICI 182,780; Faslodex) is a novel steroidal antiestrogen. This partially blind …
[PDF][PDF] Similarities and distinctions in the mode of action of different classes of antioestrogens.
AE Wakeling - Endocrine-related cancer, 2000 - scholar.archive.org
Since the description of the first antioestrogen, MER 25, more than four decades ago (Lerner
et al. 1958), and of tamoxifen ten years later (Harper & Walpole 1967a, b), a large number of …
et al. 1958), and of tamoxifen ten years later (Harper & Walpole 1967a, b), a large number of …
Functional role of estrogen in pituitary tumor pathogenesis
AP Heaney, M Fernando… - The Journal of clinical …, 2002 - Am Soc Clin Investig
Pituitary hyperplasia and lactotroph replication are induced by estrogen. The product of the
pituitary tumor transforming gene (PTTG) exhibits in vitro and in vivo transforming activity …
pituitary tumor transforming gene (PTTG) exhibits in vitro and in vivo transforming activity …
The use of selective estrogen receptor modulators and selective estrogen receptor down-regulators in breast cancer
Tamoxifen is one of the most effective treatments for breast cancer through its ability to
antagonize estrogen-dependent growth by binding estrogen receptors (ERs) and inhibiting …
antagonize estrogen-dependent growth by binding estrogen receptors (ERs) and inhibiting …
Structure-guided identification of novel dual-targeting estrogen receptor α degraders with aromatase inhibitory activity for the treatment of endocrine-resistant breast …
L Xin, J Min, H Hu, Y Li, C Du, B Xie, Y Cheng… - European Journal of …, 2023 - Elsevier
Drug resistance is a major challenge in conventional endocrine therapy for estrogen
receptor (ER) positive breast cancer (BC). BC is a multifactorial disease, in which …
receptor (ER) positive breast cancer (BC). BC is a multifactorial disease, in which …
EM-652 (SCH 57068), a third generation SERM acting as pure antiestrogen in the mammary gland and endometrium
F Labrie, C Labrie, A Bélanger, J Simard… - The Journal of steroid …, 1999 - Elsevier
Breast cancer is the most frequent cancer in women while it is the second cause of cancer
death. Estrogens are well recognized to play the predominant role in breast cancer …
death. Estrogens are well recognized to play the predominant role in breast cancer …
Oestrogen receptor-mediated modulation of the EGFR/MAPK pathway in tamoxifen-resistant MCF-7 cells
IR Hutcheson, JM Knowlden, TA Madden… - Breast cancer research …, 2003 - Springer
Oestrogen receptor (ER) levels are usually maintained on acquisition of tamoxifen
resistance in the clinic, however, tumour re-growth is associated with increased expression …
resistance in the clinic, however, tumour re-growth is associated with increased expression …