An overview of current and emerging SERMs

BS Komm, S Mirkin - The Journal of steroid biochemistry and molecular …, 2014 - Elsevier
Selective estrogen receptor modulators (SERMs) are compounds that exhibit tissue-specific
estrogen receptor (ER) agonist or antagonist activity, and are used for various indications …

Selectively targeting estrogen receptors for cancer treatment

EK Shanle, W Xu - Advanced drug delivery reviews, 2010 - Elsevier
Estrogens regulate growth and development through the action of two distinct estrogen
receptors (ERs), ERα and ERβ, which mediate proliferation and differentiation of cells. For …

Allosteric modulators of steroid hormone receptors: structural dynamics and gene regulation

R Kumar, IJ McEwan - Endocrine reviews, 2012 - academic.oup.com
Steroid hormones are synthesized from cholesterol primarily in the adrenal gland and the
gonads and play vital roles in normal physiology, the control of development, differentiation …

[HTML][HTML] A novel IMP1 inhibitor, BTYNB, targets c-Myc and inhibits melanoma and ovarian cancer cell proliferation

L Mahapatra, N Andruska, C Mao, J Le… - Translational oncology, 2017 - Elsevier
The oncofetal mRNA-binding protein, IMP1 or insulin-like growth factor-2 mRNA-binding
protein 2 (IGF2BP1), binds to and stabilizes c-Myc, β-TrCP1, and other oncogenic mRNAs …

Computer-aided ligand discovery for estrogen receptor alpha

D Bafna, F Ban, PS Rennie, K Singh… - International Journal of …, 2020 - mdpi.com
Breast cancer (BCa) is one of the most predominantly diagnosed cancers in women.
Notably, 70% of BCa diagnoses are Estrogen Receptor α positive (ERα+) making it a critical …

Minireview: Not picking pockets: nuclear receptor alternate-site modulators (NRAMs)

TW Moore, CG Mayne… - Molecular …, 2010 - academic.oup.com
Because of their central importance in gene regulation and mediating the actions of many
hormones, the nuclear receptors (NRs) have long been recognized as very important …

Proinflammatory Cytokines Enhance Estrogen-dependent Expression of the Multidrug Transporter Gene ABCG2 through Estrogen Receptor and NFκB Cooperativity …

M Pradhan, LA Bembinster, SC Baumgarten… - Journal of Biological …, 2010 - ASBMB
Constitutive activation of NFκB in estrogen receptor (ER)-positive breast cancer is
associated with tumor recurrence and development of anti-estrogen resistance …

Minireview: dynamic structures of nuclear hormone receptors: new promises and challenges

SS Simons Jr, DP Edwards, R Kumar - Molecular endocrinology, 2014 - academic.oup.com
Therapeutic targeting of nuclear receptors (NRs) is presently restricted due to 2 constraints:
1) a limited knowledge of the structural dynamics of intact receptor when complexed to DNA …

Estradiol enhances object recognition memory in Swiss female mice by activating hippocampal estrogen receptor α

LM Pereira, CP Bastos, JM de Souza… - Neurobiology of learning …, 2014 - Elsevier
Abstract In rodents, 17β-estradiol (E2) enhances hippocampal function and improves
performance in several memory tasks. Regarding the object recognition paradigm, E2 …

Regulation of estrogen receptor-mediated long range transcription via evolutionarily conserved distal response elements

YF Pan, KDSA Wansa, MH Liu, B Zhao, SZ Hong… - Journal of Biological …, 2008 - ASBMB
Nuclear signaling by estrogens rapidly induces the global recruitment of estrogen receptors
(ERs) to thousands of highly specific locations in the genome. Here, we have examined …