PROTAC'ing oncoproteins: targeted protein degradation for cancer therapy

JM Kelm, DS Pandey, E Malin, H Kansou, S Arora… - Molecular Cancer, 2023 - Springer
Molecularly targeted cancer therapies substantially improve patient outcomes, although the
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 …

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 …

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) …

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 …

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 …

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 …

Latest generation estrogen receptor degraders for the treatment of hormone receptor-positive breast cancer

YC Chen, J Yu, C Metcalfe, T De Bruyn… - Expert Opinion on …, 2022 - Taylor & Francis
Introduction The selective estrogen receptor degrader (SERD) and full receptor antagonist
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 …

Discovery of ERD-3111 as a Potent and Orally Efficacious Estrogen Receptor PROTAC Degrader with Strong Antitumor Activity

Z Chen, B Hu, RK Rej, D Wu, RK Acharyya… - Journal of Medicinal …, 2023 - ACS Publications
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 …