Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast Cancer

Ning, Wentao; Hu, Zhigang; Tang, Chu; Yang, Lu; Zhang, Silong; Dong, Chune; Huang, Jian; Zhou, Hai‐Bing

doi:10.1021/acs.jmedchem.8b00224

Cited by 30 publications

(37 citation statements)

References 61 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Ning et al developed dual targeting conjugates by joining Res and oxabicycloheptene sulfonate (OBHS), a structural motif of estrogen receptor (ER), with the aim of suppressing estrogenic and anti-inflammatory activities in breast cancer cells (MCF-7) [ 52 ]. The rationale of this design was inspired by evidence that ER/NF-κB interactions are implicated in the progression of breast cancer [ 79 , 80 ].…”

Section: Hybrid Compounds Containing Curcumin and Resveratrolmentioning

confidence: 99%

“…The most potent compound was found among the type II series and showed remarkable stereospecific binding to ER, excellent NO inhibition in macrophage RAW 264.7 cells, and cytotoxicity in the low micromolar range against MCF-7 cells ( Figure 16 ). In vivo experiments, performed in xenograft models of nude mice injected with MCF-7 cells, showed that this hybrid is more potent than reference tamoxifen [ 52 ].…”

Section: Hybrid Compounds Containing Curcumin and Resveratrolmentioning

confidence: 99%

“… Structure, activity, and SAR insights of the most potent conjugated hybrid derivative developed by Ning et al [ 52 ]. …”

Section: Figurementioning

confidence: 99%

“…Moreover, assays with the iron-chelating agent deferoxamine surprisingly indicated that this dimeric hybrid does not exert anticancer activity by means of the free radical formation variance exhibited by the other hybrids of this series of derivatives [64]. Ning et al developed dual targeting conjugates by joining Res and oxabicycloheptene sulfonate (OBHS), a structural motif of estrogen receptor (ER), with the aim of suppressing estrogenic and anti-inflammatory activities in breast cancer cells (MCF-7) [52]. The rationale of this design was inspired by evidence that ER/NF-κB interactions are implicated in the progression of breast cancer [79,80].…”

Section: Hybrid Compounds Containing Curcumin and Resveratrolmentioning

confidence: 99%

“…The most potent compound was found among the type II series and showed markable stereospecific binding to ER, excellent NO inhibition in macrophage RAW 2 cells, and cytotoxicity in the low micromolar range against MCF-7 cells (Figure 16). In v Ning et al developed dual targeting conjugates by joining Res and oxabicycloheptene sulfonate (OBHS), a structural motif of estrogen receptor (ER), with the aim of suppressing estrogenic and anti-inflammatory activities in breast cancer cells (MCF-7) [52]. The rationale of this design was inspired by evidence that ER/NF-κB interactions are implicated in the progression of breast cancer [79,80].…”

Section: Ning Et Al Developed Dual Targeting Conjugates By Joining Res and Oxabicycloh Tene Sulfonate (Obhs) A Structural Motif Of Estrogmentioning

confidence: 99%

See 4 more Smart Citations

Natural Product-Based Hybrids as Potential Candidates for the Treatment of Cancer: Focus on Curcumin and Resveratrol

et al. 2021

View full text Add to dashboard Cite

One of the main current strategies for cancer treatment is represented by combination chemotherapy. More recently, this strategy shifted to the “hybrid strategy”, namely the designing of a new molecular entity containing two or more biologically active molecules and having superior features compared with the individual components. Moreover, the term “hybrid” has further extended to innovative drug delivery systems based on biocompatible nanomaterials and able to deliver one or more drugs to specific tissues or cells. At the same time, there is an increased interest in plant-derived polyphenols used as antitumoral drugs. The present review reports the most recent and intriguing research advances in the development of hybrids based on the polyphenols curcumin and resveratrol, which are known to act as multifunctional agents. We focused on two issues that are particularly interesting for the innovative chemical strategy involved in their development. On one hand, the pharmacophoric groups of these compounds have been used for the synthesis of new hybrid molecules. On the other hand, these polyphenols have been introduced into hybrid nanomaterials based on gold nanoparticles, which have many potential applications for both drug delivery and theranostics in chemotherapy.

show abstract

Section: Hybrid Compounds Containing Curcumin and Resveratrolmentioning

confidence: 99%

Section: Hybrid Compounds Containing Curcumin and Resveratrolmentioning

confidence: 99%

“… Structure, activity, and SAR insights of the most potent conjugated hybrid derivative developed by Ning et al [ 52 ]. …”

Section: Figurementioning

confidence: 99%

Section: Hybrid Compounds Containing Curcumin and Resveratrolmentioning

confidence: 99%

Section: Ning Et Al Developed Dual Targeting Conjugates By Joining Res and Oxabicycloh Tene Sulfonate (Obhs) A Structural Motif Of Estrogmentioning

confidence: 99%

See 3 more Smart Citations

Natural Product-Based Hybrids as Potential Candidates for the Treatment of Cancer: Focus on Curcumin and Resveratrol

et al. 2021

View full text Add to dashboard Cite

show abstract

Targeted Recruitment and Degradation of Estrogen Receptor α by Photothermal Polydopamine Nanoparticles for Breast Tumor Ablation

Ding

Xie

Gao

et al. 2022

Adv Healthcare Materials

Self Cite

View full text Add to dashboard Cite

The major challenges of photothermal therapy (PTT) toward clinical application are the severe skin injury and inflammation response associated with high power laser irradiation. Herein, polydopamine nanoparticles (PDA-EST and PDA-RAL) targeted to estrogen receptor 𝜶 (ER𝜶) for efficient ablation of breast tumor under a low irradiation density of 0.1 W cm -2 are reported. These nanoparticles are capable of recruiting ER𝜶 on their surface and induce a complete ER𝜶 degradation via localized heat. Owing to the ER𝜶 targetability, PDA-EST and PDA-RAL strongly suppress the proliferation of breast cancer cells without causing significant inflammation. This work provides a generalized method for enhancing PTT efficacy under low irradiation density.

show abstract

Predicting molecular activity on nuclear receptors by multitask neural networks

Valsecchi

Collarile

Grisoni

et al. 2020

Journal of Chemometrics

View full text Add to dashboard Cite

The interest in multitask and deep learning strategies has been increasing in the last few years, in application to large and complex dataset for quantitative structure-activity relationship (QSAR) analysis. Multitask approaches allow the simultaneous prediction of molecular properties that are related, through information sharing, whereas deep learning strategies increase the potential of capturing nonlinear relationships. In this work, we compare the binary classification capability of multitask deep and shallow neural networks to singletask strategies used as benchmark (i.e., as k-nearest neighbours, N-nearest neighbours, random forest and Naïve Bayes), as well as multitask supervised self-organizing maps. Comparison was carried out with an extended QSAR dataset containing annotations of molecular binding, agonism and antagonism activity on 11 nuclear receptors, for a total of 14,963 molecules, divided into training and test sets and labelled for their bioactivity on at least one of 30 binary tasks. Additional 304 chemicals were used as external evaluation set to further validate models. Although no approach systematically overperformed the others, task-specific differences were found, suggesting the benefit of multitask learning for tasks that are less represented. On average, some of the single-task approaches and multitask deep learning strategies had similar performances. However, the latter can have advantages, such as a simpler management of predictions and applicability domain assessment for future samples. On the other hand, the parameter tuning required by neural networks are generally time expensive suggesting that the modelling strategy should be evaluated case by case.

show abstract

Novel Hybrid Conjugates with Dual Suppression of Estrogenic and Inflammatory Activities Display Significantly Improved Potency against Breast Cancer

Cited by 30 publications

References 61 publications

Natural Product-Based Hybrids as Potential Candidates for the Treatment of Cancer: Focus on Curcumin and Resveratrol

Natural Product-Based Hybrids as Potential Candidates for the Treatment of Cancer: Focus on Curcumin and Resveratrol

Targeted Recruitment and Degradation of Estrogen Receptor α by Photothermal Polydopamine Nanoparticles for Breast Tumor Ablation

Predicting molecular activity on nuclear receptors by multitask neural networks

Contact Info

Product

Resources

About