Complete elimination of estrogen receptor α by PROTAC estrogen receptor α degrader ERD-148 in breast cancer cells
B Hu, J Hu - Breast Cancer Research and Treatment, 2024 - Springer
Abstract Purpose Estrogen Receptor α (ERα) is a well-established therapeutic target for
Estrogen Receptor (ER)-positive breast cancers. Both Selective Estrogen Receptor …
Estrogen Receptor (ER)-positive breast cancers. Both Selective Estrogen Receptor …
Discovery of ERD-3111 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader with Strong Antitumor Activity
Estrogen receptor α (ERα) is a prime target for the treatment of ER-positive (ER+) breast
cancer. Despite the development of several effective therapies targeting ERα signaling …
cancer. Despite the development of several effective therapies targeting ERα signaling …
[HTML][HTML] The oral selective oestrogen receptor degrader (SERD) AZD9496 is comparable to fulvestrant in antagonising ER and circumventing endocrine resistance
A Nardone, H Weir, O Delpuech, H Brown… - British journal of …, 2019 - nature.com
Background The oestrogen receptor (ER) is an important therapeutic target in ER-positive
(ER+) breast cancer. The selective ER degrader (SERD), fulvestrant, is effective in patients …
(ER+) breast cancer. The selective ER degrader (SERD), fulvestrant, is effective in patients …
Targeted degradation of activating estrogen receptor α ligand-binding domain mutations in human breast cancer
Purpose Studies have identified several estrogen receptor α (ERα) ligand-binding domain
(LBD) somatic mutations in endocrine therapy resistant, metastatic ER-positive breast …
(LBD) somatic mutations in endocrine therapy resistant, metastatic ER-positive breast …
The turnover of estrogen receptor α by the selective estrogen receptor degrader (SERD) fulvestrant is a saturable process that is not required for antagonist efficacy
It has become apparent of late that even in tamoxifen and/or aromatase resistant breast
cancers, ERα remains a bona fide therapeutic target. Not surprisingly, therefore, there has …
cancers, ERα remains a bona fide therapeutic target. Not surprisingly, therefore, there has …
Identification of SAR439859, an orally bioavailable selective estrogen receptor degrader (SERD) that has strong anti-tumor activity in wild-type and mutant ER+ breast …
M Shomali, Y El-Ahmad, F Halley, J Cheng… - Cancer Research, 2018 - AACR
Nearly 70% or more of newly diagnosed cases of breast cancer (BC) are estrogen receptor
positive (ER+) where endocrine therapy is a primary treatment. However, substantial …
positive (ER+) where endocrine therapy is a primary treatment. However, substantial …
Abstract P6-13-02: A phase 1 dose escalation study of RAD1901, an oral selective estrogen receptor degrader, in healthy postmenopausal women
G Hattersley, F David, A Harris, M Clarkin, K Banks… - Cancer Research, 2016 - AACR
Estrogen and the estrogen receptor (ER) are known to be prominent drivers of breast
tumourigenesis and breast cancer progression. Hormonal agents that target the ER such as …
tumourigenesis and breast cancer progression. Hormonal agents that target the ER such as …
Not all selective estrogen receptor degraders are equal-Preclinical comparison of AZD9833, AZD9496 and fulvestrant
M Lawson, N Cureton, M DuPont, O Delpuech… - Cancer Research, 2020 - AACR
Anti-hormonal therapy has been the mainstay treatment for estrogen receptor (ER)+ ve
breast cancer for> 40 years. The selective ER degrader (SERD) fulvestrant has …
breast cancer for> 40 years. The selective ER degrader (SERD) fulvestrant has …
Discovery of AZD9833, an oral small molecule selective degrader of the estrogen receptor (SERD)
The estrogen receptor alpha (ERα) is expressed in> 70% of breast cancers and is a
clinically validated target in oncology. Anti-hormonal therapies that block ER function directly …
clinically validated target in oncology. Anti-hormonal therapies that block ER function directly …
Abstract P3-04-05: Identification of SAR439859, an orally bioavailable selective estrogen receptor degrader (SERD) that has strong antitumor activity in wild-type and …
M Shomali, J Cheng, M Koundinya, M Weinstein… - Cancer research, 2017 - AACR
Estrogen receptor positive (ER+) breast cancer accounts for 70% of all breast cancers and is
primarily treated with endocrine therapy. Approximately 40% of patients on endocrine …
primarily treated with endocrine therapy. Approximately 40% of patients on endocrine …