ESR1 Mutations Take Center Stage in Metastatic ER-Positive Breast Cancer

Jane De Lartigue, PhD
Published: Wednesday, Aug 01, 2018
breast cancer
Although endocrine therapies that block the production or subsequent effects of estrogen have been a bedrock of the treatment for hormonally driven breast cancer for more than 40 years, resistance poses a major threat to their efficacy and has become a focus of ongoing research.

Despite gaps in current knowledge, investigators are already working toward the development of novel treatment strategies to combat the effects of the mutations and wrestle back control of ER-positive tumor growth.

ER Signaling

As the cellular orchestrator of the effects of the estrogen hormones, ERs play an important role in a plethora of processes, including its most renowned functions in reproduction and sexual development and in modulating the immune system.1,2

Figure. Key Components of Estrogen Receptor Signaling

FIGURE. KEY COMPONENTS OF ESTROGEN RECEPTOR SIGNALING
Estrogens are steroid hormones that pass freely across the cell membrane and do not need to bind to a membrane-bound receptor to transmit their signal into the cell. Although they can be found in the membranes, ERs predominantly reside in the nucleus, where, after binding to an estrogen ligand, they can act directly as a transcription factor.

ER-Driven Breast Cancer

ER signaling has been shown to be indispensable to mammary gland development,6,7 although the precise mechanisms through which it regulates the proliferation and differentiation of human breast cells is unclear. A relatively small number of cells in the normal mammary gland express ERs.8
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Online CME Activities
TitleExpiration DateCME Credits
Community Practice Connections™: PARP Inhibition in Breast Cancer: Practical Methods to Interpret and Apply the Evidence for Your PatientsAug 30, 20191.5
Provider and Caregiver Connection™: Addressing Patient Concerns in the Management of Premenopausal Breast CancerAug 31, 20192.0
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