ERα/ESR1 Cancer Research Results

ERα/ESR1, Estrogen Receptor alpha: Click to Expand ⟱
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Type:
ERα (Estrogen Receptor alpha) is a subtype of estrogen receptor that plays a crucial role in the development and progression of various types of cancer.
Cancers with high ERα expression (>50%):BC(80%),EC(80%),OC,Uterine sarcoma
Cancers with moderate ERα expression (20-50%):CRC, PCa, Vulvar
Cancers with low ERα expression (<20%):Lung, PC, GC

ESR1 is used as a clinical biomarker for Endocrine Therapy
Scientific Papers found: Click to Expand⟱
1279- And,    Andrographolide Exhibits Anticancer Activity against Breast Cancer Cells (MCF-7 and MDA-MB-231 Cells) through Suppressing Cell Proliferation and Inducing Cell Apoptosis via Inactivation of ER-α Receptor and PI3K/AKT/mTOR Signaling
- in-vitro, BC, MDA-MB-231 - in-vitro, BC, MCF-7
Apoptosis↑,
Bcl-2↓,
BAX↑,
ERα/ESR1↓, ER-positive
PI3K↓, ER-positive
mTOR↓, ER-positive BC

1348- And,    Andrographolide Inhibits ER-Positive Breast Cancer Growth and Enhances Fulvestrant Efficacy via ROS-FOXM1-ER-α Axis
- in-vitro, BC, MCF-7 - in-vitro, BC, T47D - in-vivo, NA, NA
ERα/ESR1↓,
TumCG↓,
ROS↑,
FOXM1↓,
eff↑, In addition, AD in combination with fulvestrant (FUL) synergistically down-regulated ER-α expression to inhibit ER-positive breast cancer both in vitro and in vivo.

976- ART/DHA,    Artemisinin selectively decreases functional levels of estrogen receptor-alpha and ablates estrogen-induced proliferation in human breast cancer cells
- in-vitro, BC, MCF-7
ERα/ESR1↓, downregulated ERα protein and transcripts without altering expression or activity of ERβ

1174- Ash,    Withaferin A Suppresses Estrogen Receptor-α Expression in Human Breast Cancer Cells
- in-vitro, BC, MCF-7 - in-vivo, BC, MDA-MB-231 - in-vitro, BC, T47D
p‑P53↑,
Apoptosis↑,
ERα/ESR1↓, marked decrease in protein levels of ER-α (but not ER-β)

6181- Cro,    Crocetin: A Systematic Review
- Review, Var, NA - Review, AD, NA
cardioP↑, According to modern pharmacological investigations, crocetin possesses cardioprotective, hepatoprotective, neuroprotective, antidepressant, antiviral, anticancer, atherosclerotic, antidiabetic, and memory-enhancing properties.
hepatoP↑,
*neuroP↑,
AntiCan↑,
*AntiDiabetic↑,
*memory↑,
*BioAv↓, poor bioavailability hinders therapeutic applications, derivatization and formulation preparation technologies have broadened the application prospects for crocetin.
*ROS↓, Crocetin can act via different mechanisms, such as enhancing the rate of oxygen transport and diffusivity, inhibiting pro-inflammatory mediators, protecting cells from reactive oxygen species (ROS) damage, and stimulating apoptosis in cancer cells
Apoptosis↑,
*lipid-P↓, Myocardial hypertrophy rats Decreases the LPO content and increases the activities of GSH-Px and SOD
*SOD↑,
SOD↓, MCF-7 cells Crocetin (200 μmol/L) Inhibits SOD activity by affecting copper binding sites
ERα/ESR1↓, MCF-7 cells Crocetin glucosyl ester IC50 from 31.25 to 1,000 μg/ml Inhibits estrogen receptor α and HDAC2 mediated signaling cascade
HDAC2↓,
TumCCA↑, KYSE-150 cells Crocetin (0, 12.5, 25, 50, 100, 200 μmol/L) S-phase cell arrest
Bax:Bcl2↑, AGS cells Crocetin (50–240 μmol/L) Decreases the Bcl-2/Bax ratio of AGS cells
IL6↓, HCT116 cells Crocetin (30 µM) Downregulates inflammation-related genes, HMGB1, IL-6, and IL-8
IL8↓,
Shh↓, Cancer stem cells (CSC) Inhibits the expression of Sonic hedgehog (SHH)
COX2↑, HeLa cells Upregulates COX-2 expression
*GSK‐3β↓, Alzheimer’s disease (AD) SH-SY5Y and PC12 cells Inhibits the active forms of GSK3β and ERK 1/2 kinases and significantly reduces the total tau protein and tau protein phosphorylation
*ERK↓,
*tau↓,
*ROS↓, crocetin-induced inhibition of Aβ1-42-induced hippocampal HT22 cell death could be mediated via reduced ROS production.
*GSTs↑, The activities of antioxidant enzymes [GSH-Px, GSH reductase (GR), GST, CAT, and SOD]
*Catalase↑,
*SOD↑,
*BioAv↑, The bioavailability of crocetin can be improved by formulating a crocetin injection

6246- Cyc,    Cyclopamine is a novel Hedgehog signaling inhibitor with significant anti-proliferative, anti-invasive and anti-estrogenic potency in human breast cancer cells
- in-vitro, BC, MCF-7 - in-vitro, BC, MDA-MB-231
HH↓, cyclopamine, a naturally occurring Hedgehog-specific small-molecule inhibitor, causes profound inhibition of tumor growth.
TumCP↓, cyclopamine displayed a significant potency in suppressing the proliferation of both estrogen-responsive (MCF-7) and estrogen-independent (MDA-MB-231) human breast cancer cells.
TumCCA↓, Cyclopamine induced a robust G1 cell cycle arrest and elicited notable effects on the expression of cyclin D1 through modulation of the MAPK/ERK signaling pathway.
TumCI↓, Cyclopamine also inhibited the invasive ability of both breast cancer cell lines by suppressing the expression levels of NF-κB, MMP2 and MMP9 protein
NF-kB↓,
MMP2↓,
MMP9↓,
ERα/ESR1↓, cyclopamine significantly downregulated the production of estrogen receptor-α protein.
cycD1/CCND1↓, expression level of cyclin D1 decreased in cyclopamine-treated cells.

1154- HNK,  MET,    Honokiol inhibits the growth of hormone-resistant breast cancer cells: its promising effect in combination with metformin
- in-vitro, BC, MCF-7 - in-vitro, BC, SkBr3 - in-vitro, BC, MDA-MB-231
cl‑PARP↑,
Bcl-2↓,
ERα/ESR1↓, combination of honokiol with metformin.

4932- PEITC,    Pharmacokinetics and Pharmacodynamics of Phenethyl Isothiocyanate: Implications in Breast Cancer Prevention
- Review, BC, NA
TumCCA↑, pharmacodynamics of PEITC in breast cancer that include cancer cell apoptosis by upregulation of apoptotic genes, cell cycle arrest at G2/M phase by generation of reactive oxygen species and depletion of intracellular glutathione
ROS↑,
GSH↓,
ERα/ESR1↓, downregulation of the estrogen receptor, decrease in sensitivity to estrogen, and inhibition of tumor metastasis.
TumMeta↓,
angioG↓, Inhibition of angiogenesis is one of the recently reported mechanisms of breast cancer prevention by PEITC.

977- SK,    A novel antiestrogen agent Shikonin inhibits estrogen-dependent gene transcription in human breast cancer cells
- in-vitro, BC, T47D - in-vitro, BC, MDA-MB-231 - in-vitro, BC, MCF-7 - in-vitro, Nor, HMEC
TumCG↓, SK inhibits tumor cell growth in estrogen receptor alpha (ERalpha)-positive, but not ERalpha-negative breast cancer cells.
ERα/ESR1↓, SK inhibits ERa expression, and suppresses ERa signaling
selectivity↑, non-malignant HME cells show undetectable ERa protein (Fig. 2a). Treatment with increased concentrations of SK for 72 h has no effect on cell growth
*toxicity↓, In addition, SK shows low cytoxicity in normal human mammary epithelia cells.

984- SSE,    Effects of selenite on estrogen receptor-alpha expression and activity in MCF-7 breast cancer cells
- in-vitro, BC, MCF-7
ERα/ESR1↓, 1 uM of sodium selenite resulted in a 40% decrease in the amount of estrogen receptor-alpha
PR↑, 2.6x
pS2/TFF1↑, pS2 mRNA increased 2.4-fold after selenite treatment.
Catalase↑, three- to five-fold increase in CAT activity


Showing Research Papers: 1 to 10 of 10

* indicates research on normal cells as opposed to diseased cells
Total Research Paper Matches: 10

Pathway results for Effect on Cancer / Diseased Cells:


Redox & Oxidative Stress ⓘ

Catalase↑, 1,   GSH↓, 1,   ROS↑, 2,   SOD↓, 1,  

Cell Death ⓘ

Apoptosis↑, 3,   BAX↑, 1,   Bax:Bcl2↑, 1,   Bcl-2↓, 2,   pS2/TFF1↑, 1,  

DNA Damage & Repair ⓘ

p‑P53↑, 1,   cl‑PARP↑, 1,  

Cell Cycle & Senescence ⓘ

cycD1/CCND1↓, 1,   TumCCA↓, 1,   TumCCA↑, 2,  

Proliferation, Differentiation & Cell State ⓘ

FOXM1↓, 1,   HDAC2↓, 1,   HH↓, 1,   mTOR↓, 1,   PI3K↓, 1,   PR↑, 1,   Shh↓, 1,   TumCG↓, 2,  

Migration ⓘ

MMP2↓, 1,   MMP9↓, 1,   TumCI↓, 1,   TumCP↓, 1,   TumMeta↓, 1,  

Angiogenesis & Vasculature ⓘ

angioG↓, 1,  

Immune & Inflammatory Signaling ⓘ

COX2↑, 1,   IL6↓, 1,   IL8↓, 1,   NF-kB↓, 1,  

Hormonal & Nuclear Receptors ⓘ

ERα/ESR1↓, 10,  

Drug Metabolism & Resistance ⓘ

eff↑, 1,   selectivity↑, 1,  

Clinical Biomarkers ⓘ

ERα/ESR1↓, 10,   FOXM1↓, 1,   IL6↓, 1,  

Functional Outcomes ⓘ

AntiCan↑, 1,   cardioP↑, 1,   hepatoP↑, 1,  
Total Targets: 41

Pathway results for Effect on Normal Cells:


Redox & Oxidative Stress ⓘ

Catalase↑, 1,   GSTs↑, 1,   lipid-P↓, 1,   ROS↓, 2,   SOD↑, 2,  

Proliferation, Differentiation & Cell State ⓘ

ERK↓, 1,   GSK‐3β↓, 1,  

Synaptic & Neurotransmission ⓘ

tau↓, 1,  

Drug Metabolism & Resistance ⓘ

BioAv↓, 1,   BioAv↑, 1,  

Functional Outcomes ⓘ

AntiDiabetic↑, 1,   memory↑, 1,   neuroP↑, 1,   toxicity↓, 1,  
Total Targets: 14

Scientific Paper Hit Count for: ERα/ESR1, Estrogen Receptor alpha
2 Andrographis
1 Artemisinin
1 Ashwagandha(Withaferin A)
1 Crocetin
1 Cyclopamine
1 Honokiol
1 Metformin
1 Phenethyl isothiocyanate
1 Shikonin
1 Selenite (Sodium)
Query results interpretion may depend on "conditions" listed in the research papers.
Such Conditions may include : 
  -low or high Dose
  -format for product, such as nano of lipid formations
  -different cell line effects
  -synergies with other products 
  -if effect was for normal or cancerous cells

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