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Related Concept Videos

G Protein-coupled Receptors01:15

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G Protein-Coupled Receptors or GPCRs are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to sensory stimuli such as light, odors, hormones, cytokines, or neurotransmitters.
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G Protein–Coupled Receptors (GPCRs) are membrane-bound receptors that transiently associate with heterotrimeric G proteins and induce an appropriate response to various stimuli. GPCRs regulate critical physiological pathways and are excellent drug targets for treating diseases such as diabetes, cancer, obesity, depression, or Alzheimer's. Nearly 35% of approved drugs implement their therapeutic effects by selectively interacting with specific GPCRs.
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Mitogens and their receptors play a crucial role in controlling the progression of the cell cycle. However, the loss of mitogenic control over cell division leads to tumor formation. Therefore, mitogens and mitogen receptors play an important role in cancer research. For instance, the epidermal growth factor (EGF) - a type of mitogen and its transmembrane receptor (EGFR), decides the fate of the cell's proliferation. When EGF binds to EGFR, a member of the ErbB family of tyrosine kinase...
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Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
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Retraction notice to "17β-Estradiol, Genistein, and 4-Hydroxytamoxifen Induce the Proliferation of Thyroid Cancer Cells through the G Protein-Coupled Receptor GPR30" [Mol Pharmacol 70 (2006) 1414-1423].

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GPER Function in Breast Cancer: An Overview.

Rosamaria Lappano1, Assunta Pisano1, Marcello Maggiolini1

  • 1Department of Pharmacy, Health and Nutritional Sciences, University of Calabria , Rende , Italy.

Frontiers in Endocrinology
|May 17, 2014
PubMed
Summary

The G-protein-coupled estrogen receptor-1 (GPER) mediates estrogen signaling in breast cancer, potentially driving tumor progression and tamoxifen resistance. GPER is also a promising biomarker for triple-negative breast cancer assessment.

Keywords:
GPERGPR30breast cancerestrogenestrogen receptor

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Area of Science:

  • Endocrinology
  • Oncology
  • Molecular Biology

Background:

  • G-protein-coupled estrogen receptor-1 (GPER), also known as GPR30, mediates estrogenic signaling.
  • GPER plays a role in various cell types, including hormone-sensitive tumors like breast cancer.
  • Epidermal growth factor receptor activation is a key integration point for GPER-mediated biological actions.

Purpose of the Study:

  • To explore the role of GPER in breast cancer.
  • To investigate the association between GPER and tumor progression, tamoxifen resistance, and its potential as a biomarker.

Main Methods:

  • Review of existing literature on GPER function in breast cancer.
  • Analysis of GPER's involvement in estrogenic signaling pathways.
  • Examination of GPER's correlation with tumor characteristics and treatment response.

Main Results:

  • GPER activation by various compounds, including estrogens and anti-estrogens, stimulates breast cancer.
  • GPER up-regulation and activation are linked to breast tumor progression and tamoxifen resistance.
  • GPER is identified as a potential biomarker for triple-negative breast cancer.

Conclusions:

  • GPER is a significant mediator of estrogenic effects in breast cancer.
  • GPER's role in tumor progression and resistance highlights its therapeutic relevance.
  • GPER presents a novel avenue for breast tumor patient assessment and biomarker development.