Reciprocal Regulation of ERα and ERβ Stability and Activity by Diptoindonesin G

Zhao, Zibo; Wang, Lu; James, Taryn T.; Jung, Young-Eun; Kim, Ikyon; Tan, Renxiang; Hoffmann, F. M.; Xu, Wei

doi:10.1016/j.chembiol.2015.10.011

Cited by 34 publications

(33 citation statements)

References 68 publications

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“…These correlations are in line with the previous studies indicating that PR is a typical estrogen dependent target gene which is positively regulated by ERα and negatively regulated by ERβ 41 , 42 . Furthermore, ERα and ERβ expression levels were reversely regulated by several mechanisms such as proteasome pathway 43 , 44 and some microRNAs 45 , 46 . As for ERα36, EGFR and HER2, there was a significant positive correlation between ERα36, EGFR and HER2 protein expression in PTCs.…”

Section: Discussionmentioning

confidence: 99%

Concomitant high expression of ERα36, EGFR and HER2 is associated with aggressive behaviors of papillary thyroid carcinomas

Dai

Qiu

Jiang

et al. 2017

Sci Rep

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ERα, ERβ, PR, ERα36, EGFR and HER2 mRNA and protein expression in papillary thyroid carcinoma (PTC) were examined by real time RT-PCR and immunohistochemical staining. The mRNA and protein expression of ERα and PR were gradually increased and those of ERβ were gradually decreased from normal thyroid tissues to nodular hyperplasias (P < 0.05) and to PTCs (P < 0.05). However, the mRNA and protein expression of ERα36, EGFR and HER2 were only significantly increased in PTCs when compared with those in normal thyroid tissues (P < 0.001) and nodular hyperplasias (P < 0.001). There was some correlation between ERα, ERβ and PR, and between ERα36, EGFR and HER2 protein expression in PTCs. As for ERα, ERβ and PR, there was a significant positive correlation between ERα and PR, and a significant negative correlation between ERα and ERβ and between PR and ERβ protein expression. As for ERα36, EGFR and HER2, there was a significant positive correlation between ERα36, EGFR and HER2 protein expression in PTCs. Concomitant high expression of ERα36, EGFR and HER2 was strongly associated with aggressive behaviors including extrathyroidal extension (ETE), lymph node metastasis (LNM) and high TNM stage in PTCs (P < 0.001).

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Section: Discussionmentioning

confidence: 99%

Concomitant high expression of ERα36, EGFR and HER2 is associated with aggressive behaviors of papillary thyroid carcinomas

Dai

Qiu

Jiang

et al. 2017

Sci Rep

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“…With improved oral bioavailability, this compound shows promising preclinical results in mice (12–14) and is now in Phase I clinical trials. Other compounds with oral bioavailability and high potency have also been described by AstraZeneca (15–19), Pfizer (20), and other research groups (21). …”

Section: Selective Estrogen Receptor Downregulatorsmentioning

confidence: 95%

Targeted Protein Degradation by Small Molecules

Bondeson

Crews²

2017

Annu. Rev. Pharmacol. Toxicol.

152

142

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Protein homeostasis networks are highly regulated systems responsible for maintaining the health and productivity of cells. Whereas therapeutics have been developed to disrupt protein homeostasis, more recently identified techniques have been used to repurpose homeostatic networks to effect degradation of disease-relevant proteins. Here, we review recent advances in the use of small molecules to degrade proteins in a selective manner. First, we highlight all-small-molecule techniques with direct clinical application. Second, we describe techniques that may find broader acceptance in the biomedical research community that require little or no synthetic chemistry. In addition to serving as innovative research tools, these new approaches to control intracellular protein levels offer the potential to develop novel therapeutics targeting proteins that are not currently pharmaceutically vulnerable.

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“…Although generated by individual genes, ERα and ERβ have almost 100% amino acid homology in their DNA-binding domain and about 60% amino acid homology in their protein-interacting domains [56]. Interestingly, in vivo and in vitro experiments demonstrated differential or opposite effects of ERα and ERβ on biological features of breast cancer cells [57]. ERα-regulated gene expressions facilitate the growth and survival of breast cancer cells in response to estrogens [58], whereas the impact of ERβ on breast cancer cells is controversial [59].…”

Section: Impacts Of Alternative Splicing Events On Apoptosismentioning

confidence: 99%

Differential Impacts of Alternative Splicing Networks on Apoptosis

Lin

Tsao

Lin

2016

IJMS

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Apoptosis functions as a common mechanism to eliminate unnecessary or damaged cells during cell renewal and tissue development in multicellular organisms. More than 200 proteins constitute complex networks involved in apoptotic regulation. Imbalanced expressions of apoptosis-related factors frequently lead to malignant diseases. The biological functions of several apoptotic factors are manipulated through alternative splicing mechanisms which expand gene diversity by generating discrete variants from one messenger RNA precursor. It is widely observed that alternatively-spliced variants encoded from apoptosis-related genes exhibit differential effects on apoptotic regulation. Alternative splicing events are meticulously regulated by the interplay between trans-splicing factors and cis-responsive elements surrounding the regulated exons. The major focus of this review is to highlight recent studies that illustrate the influences of alternative splicing networks on apoptotic regulation which participates in diverse cellular processes and diseases.

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Reciprocal Regulation of ERα and ERβ Stability and Activity by Diptoindonesin G

Cited by 34 publications

References 68 publications

Concomitant high expression of ERα36, EGFR and HER2 is associated with aggressive behaviors of papillary thyroid carcinomas

Concomitant high expression of ERα36, EGFR and HER2 is associated with aggressive behaviors of papillary thyroid carcinomas

Targeted Protein Degradation by Small Molecules

Differential Impacts of Alternative Splicing Networks on Apoptosis

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