PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
durability of their effectiveness can be limited. Resistance to these therapies is often related …
durability of their effectiveness can be limited. Resistance to these therapies is often related …
[HTML][HTML] Selective estrogen receptor modulators (SERMs) and selective estrogen receptor degraders (SERDs) in cancer treatment
HK Patel, T Bihani - Pharmacology & therapeutics, 2018 - Elsevier
Breast cancer is the most frequently diagnosed cancer in women, with estrogen receptor
positive (ER+) breast cancer making up approximately 75% of all breast cancers diagnosed …
positive (ER+) breast cancer making up approximately 75% of all breast cancers diagnosed …
Systemic therapy for estrogen receptor–positive, HER2-negative breast cancer
HJ Burstein - New England Journal of Medicine, 2020 - Mass Medical Soc
Estrogen Receptor–Positive Breast Cancer ER-positive, HER2-negative breast cancer,
which accounts for about 70% of all breast cancers, is heterogeneous. Antiestrogen therapy …
which accounts for about 70% of all breast cancers, is heterogeneous. Antiestrogen therapy …
Next-generation selective estrogen receptor degraders and other novel endocrine therapies for management of metastatic hormone receptor-positive breast cancer …
MR Lloyd, SA Wander, E Hamilton… - Therapeutic …, 2022 - journals.sagepub.com
Endocrine therapy (ET) is a pivotal strategy to manage early-and advanced-stage estrogen
receptor-positive (ER+) breast cancer. In patients with metastatic breast cancer (MBC) …
receptor-positive (ER+) breast cancer. In patients with metastatic breast cancer (MBC) …
Discovery of ERD-308 as a highly potent proteolysis targeting chimera (PROTAC) degrader of estrogen receptor (ER)
J Hu, B Hu, M Wang, F Xu, B Miao… - Journal of medicinal …, 2019 - ACS Publications
The estrogen receptor (ER) is a validated target for the treatment of estrogen receptor-
positive (ER+) breast cancer. Here, we describe the design, synthesis, and extensive …
positive (ER+) breast cancer. Here, we describe the design, synthesis, and extensive …
Heterogeneity and clinical significance of ESR1 mutations in ER-positive metastatic breast cancer patients receiving fulvestrant
JM Spoerke, S Gendreau, K Walter, J Qiu… - Nature …, 2016 - nature.com
Mutations in ESR1 have been associated with resistance to aromatase inhibitor (AI) therapy
in patients with ER+ metastatic breast cancer. Little is known of the impact of these mutations …
in patients with ER+ metastatic breast cancer. Little is known of the impact of these mutations …
Structural underpinnings of oestrogen receptor mutations in endocrine therapy resistance
JA Katzenellenbogen, CG Mayne… - Nature Reviews …, 2018 - nature.com
Oestrogen receptor-α (ERα), a key driver of breast cancer, normally requires oestrogen for
activation. Mutations that constitutively activate ERα without the need for hormone binding …
activation. Mutations that constitutively activate ERα without the need for hormone binding …
Latest generation estrogen receptor degraders for the treatment of hormone receptor-positive breast cancer
Introduction The selective estrogen receptor degrader (SERD) and full receptor antagonist
provides an important therapeutic option for hormone receptor (HR)-positive breast cancer …
provides an important therapeutic option for hormone receptor (HR)-positive breast cancer …
Nuclear receptors: recent drug discovery for cancer therapies
L Zhao, S Zhou, JÅ Gustafsson - Endocrine reviews, 2019 - academic.oup.com
Nuclear receptors (NRs) are transcription factors actively involved in many aspects of human
physiology and pathology, serving as sensors of stimuli, master regulators of downstream …
physiology and pathology, serving as sensors of stimuli, master regulators of downstream …
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 …