Dr ZHEYING ZHU's Outputs (69)

Discovery of Norbornene as a Novel Hydrophobic Tag Applied in Protein Degradation (2023)
Journal Article
Xie, S., Zhan, F., Zhu, J., Sun, Y., Zhu, H., Liu, J., Chen, J., Zhu, Z., Yang, D.-H., Chen, Z.-S., Yao, H., Xu, J., & Xu, S. (2023). Discovery of Norbornene as a Novel Hydrophobic Tag Applied in Protein Degradation. Angewandte Chemie International Edition, 62(13), Article e202217246. https://doi.org/10.1002/anie.202217246

Hydrophobic tagging (HyT) is a potential therapeutic strategy for targeted protein degradation (TPD). Norbornene was discovered as an unprecedented hydrophobic tag in this study and was used to degrade the anaplastic lymphoma kinase (ALK) fusion prot... Read More about Discovery of Norbornene as a Novel Hydrophobic Tag Applied in Protein Degradation.

An update on the recent advances and discovery of novel tubulin colchicine binding inhibitors (2023)
Journal Article
Weng, H., Li, J., Zhu, H., Carver Wong, K. F., Zhu, Z., & Xu, J. (2023). An update on the recent advances and discovery of novel tubulin colchicine binding inhibitors. Future Medicinal Chemistry, 15(1), 73-95. https://doi.org/10.4155/fmc-2022-0212

Microtubules, formed by α- and β-tubulin heterodimer, are considered as a major target to prevent the proliferation of tumor cells. Microtubule-targeted agents have become increasingly effective anticancer drugs. However, due to the relatively sophis... Read More about An update on the recent advances and discovery of novel tubulin colchicine binding inhibitors.

Design, synthesis and biological evaluation of novel 9-N-substituted-13-alkylberberine derivatives from Chinese medicine as anti-hepatocellular carcinoma agents (2023)
Journal Article
Chen, J., Duan, Y., Yang, K., Wang, J., Yan, J., Gu, C., Wang, S., Zhu, Z., Liu, E.-H., & Xu, J. (2023). Design, synthesis and biological evaluation of novel 9-N-substituted-13-alkylberberine derivatives from Chinese medicine as anti-hepatocellular carcinoma agents. Bioorganic and Medicinal Chemistry, 79, Article 117156. https://doi.org/10.1016/j.bmc.2023.117156

A series of novel 9-N-substituted-13-alkylberberine derivatives from Chinese medicine were designed and synthesized with improved anti-hepatocellular carcinoma (HCC) activities. The optimal compound 4d showed strong activities against HepG2, Sk-Hep-1... Read More about Design, synthesis and biological evaluation of novel 9-N-substituted-13-alkylberberine derivatives from Chinese medicine as anti-hepatocellular carcinoma agents.

Design, synthesis, and biological evaluation of novel protopanoxadiol derivatives based PROTACs technology for the treatment of lung cancer (2022)
Journal Article
Wang, P., Zhu, H., Liu, J., xie, S., Xu, S., Chen, Y., Xu, J., Zhao, Y., Zhu, Z., & Xu, J. (2023). Design, synthesis, and biological evaluation of novel protopanoxadiol derivatives based PROTACs technology for the treatment of lung cancer. Bioorganic Chemistry, 131, Article 106327. https://doi.org/10.1016/j.bioorg.2022.106327

Protopanoxadiol is a key active ingredient derived from Panax ginseng that is well-known to exhibit anti-tumor activity. Previous research focused on the natural protopanaxadiol derivative AD-1 has demonstrated that it possesses broad spectrum anti-t... Read More about Design, synthesis, and biological evaluation of novel protopanoxadiol derivatives based PROTACs technology for the treatment of lung cancer.

Current development of bicyclic peptides (2022)
Journal Article
Feng, D., Liu, L., Shi, Y., Du, P., Xu, S., Zhu, Z., Xu, J., & Yao, H. (2023). Current development of bicyclic peptides. Chinese Chemical Letters, 34(6), Article 108026. https://doi.org/10.1016/j.cclet.2022.108026

Bicyclic peptides, a class of polypeptides with two loops within their structure, have emerged as powerful tools in the development of new peptide drugs. They have the potential to bind to challenged drug targets, with antibody-like affinity and sele... Read More about Current development of bicyclic peptides.

Development of p-Tau Differentiated Cell Model of Alzheimer’s Disease to Screen Novel Acetylcholinesterase Inhibitors (2022)
Journal Article
Uras, G., Li, X., Manca, A., Pantaleo, A., Bo, M., Xu, J., Allen, S., & Zhu, Z. (2022). Development of p-Tau Differentiated Cell Model of Alzheimer’s Disease to Screen Novel Acetylcholinesterase Inhibitors. International Journal of Molecular Sciences, 23(23), Article 14794. https://doi.org/10.3390/ijms232314794

Alzheimer’s disease (AD) is characterized by an initial accumulation of amyloid plaques and neurofibrillary tangles, along with the depletion of cholinergic markers. The currently available therapies for AD do not present any disease-modifying effect... Read More about Development of p-Tau Differentiated Cell Model of Alzheimer’s Disease to Screen Novel Acetylcholinesterase Inhibitors.

Design, Synthesis, and Biological Evaluation of Novel Chromanone Derivatives as Multifunctional Agents for the Treatment of Alzheimer's Disease (2022)
Journal Article
Li, X., Li, T., Zhan, F., Cheng, F., Lu, L., Zhang, B., Li, J., Hu, Z., Zhou, S., Jia, Y., Allen, S., White, L., Phillips, J., Zhu, Z., Xu, J., & Yao, H. (2022). Design, Synthesis, and Biological Evaluation of Novel Chromanone Derivatives as Multifunctional Agents for the Treatment of Alzheimer's Disease. ACS Chemical Neuroscience, 13(23), 3488-3501. https://doi.org/10.1021/acschemneuro.2c00520

Based on a multitarget strategy, a series of novel chromanone-1-benzyl-1,2,3,6-tetrahydropyridin hybrids were identified for the potential treatment of Alzheimer's disease (AD). Biological evaluation demonstrated that these hybrids exhibited signific... Read More about Design, Synthesis, and Biological Evaluation of Novel Chromanone Derivatives as Multifunctional Agents for the Treatment of Alzheimer's Disease.

Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease (2022)
Journal Article
Li, X., Li, T., Zhang, P., Li, X., Lu, L., Sun, Y., Zhang, B., Allen, S., White, L., Phillips, J., Zhu, Z., Yao, H., & Xu, J. (2022). Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease. European Journal of Medicinal Chemistry, 244, Article 114841. https://doi.org/10.1016/j.ejmech.2022.114841

Based on the multitarget strategy, a series of novel clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine hybrids were identified for the potential treatment of Alzheimer's disease (AD). Biological evaluation in vitro revealed that these hybrids exhibited... Read More about Discovery of novel hybrids containing clioquinol−1-benzyl-1,2,3,6-tetrahydropyridine as multi-target-directed ligands (MTDLs) against Alzheimer's disease.

Mineral metabolism and ferroptosis in non-alcoholic fatty liver diseases (2022)
Journal Article
Ma, C., Han, L., Zhu, Z., Heng Pang, C., & Pan, G. (2022). Mineral metabolism and ferroptosis in non-alcoholic fatty liver diseases. Biochemical Pharmacology, 205, Article 115242. https://doi.org/10.1016/j.bcp.2022.115242

Nonalcoholic fatty liver disease (NAFLD) has become the most prevalent chronic liver disease worldwide. Minerals including iron, copper, zinc, and selenium, fulfil an essential role in various biochemical processes. Moreover, the identification of fe... Read More about Mineral metabolism and ferroptosis in non-alcoholic fatty liver diseases.

Development of novel 9-O-substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents (2022)
Journal Article
Chen, J., Duan, Y., Yu, X., Zhong, J., Bai, J., Li, N. G., Zhu, Z., & Xu, J. (2022). Development of novel 9-O-substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents. Journal of Enzyme Inhibition and Medicinal Chemistry, 37(1), 2423-2433. https://doi.org/10.1080/14756366.2022.2118268

A series of novel 9-O-substituted-13-octylberberine derivatives were designed, synthesised and evaluated for their anti-hepatocellular carcinoma (HCC) activities. Compound 6k showed the strongest activity against three human hepatoma cells including... Read More about Development of novel 9-O-substituted-13-octylberberine derivatives as potential anti-hepatocellular carcinoma agents.

Design and synthesis of NAD(P)H: Quinone oxidoreductase (NQO1)-activated prodrugs of 23-hydroxybetulinic acid with enhanced antitumor properties (2022)
Journal Article
Zhu, H., Lu, L., Zhu, W., Tan, Y., Duan, Y., Liu, J., Ye, W., Zhu, Z., Xu, J., & Xu, S. (2022). Design and synthesis of NAD(P)H: Quinone oxidoreductase (NQO1)-activated prodrugs of 23-hydroxybetulinic acid with enhanced antitumor properties. European Journal of Medicinal Chemistry, 240, Article 114575. https://doi.org/10.1016/j.ejmech.2022.114575

A series of NQO1 selectively activated prodrugs were designed and synthesized by introducing indolequinone moiety to the C-3, C-23 or C-28 position of 23-hydroxybetulinic acid (23-HBA) and its analogues. Among them, the representative compound 32j ex... Read More about Design and synthesis of NAD(P)H: Quinone oxidoreductase (NQO1)-activated prodrugs of 23-hydroxybetulinic acid with enhanced antitumor properties.

New Insights into Neuroinflammation Involved in Pathogenic Mechanism of Alzheimer’s Disease and Its Potential for Therapeutic Intervention (2022)
Journal Article
Li, T., Lu, L., Pember, E., Li, X., Zhang, B., & Zhu, Z. (2022). New Insights into Neuroinflammation Involved in Pathogenic Mechanism of Alzheimer’s Disease and Its Potential for Therapeutic Intervention. Cells, 11(12), Article 1925. https://doi.org/10.3390/cells11121925

Alzheimer’s disease (AD) is the most common form of dementia, affecting more than 50 million people worldwide with an estimated increase to 139 million people by 2050. The exact pathogenic mechanisms of AD remain elusive, resulting in the fact that t... Read More about New Insights into Neuroinflammation Involved in Pathogenic Mechanism of Alzheimer’s Disease and Its Potential for Therapeutic Intervention.

Novel and Potent Acetylcholinesterase Inhibitors for the Treatment of Alzheimer’s Disease from Natural (±)-7,8-Dihydroxy-3-methyl-isochroman-4-one (2022)
Journal Article
Li, X., Jia, Y., Li, J., Zhang, P., Li, T., Lu, L., Yao, H., Liu, J., Zhu, Z., & Xu, J. (2022). Novel and Potent Acetylcholinesterase Inhibitors for the Treatment of Alzheimer’s Disease from Natural (±)-7,8-Dihydroxy-3-methyl-isochroman-4-one. Molecules, 27(10), Article 3090. https://doi.org/10.3390/molecules27103090

Alzheimer’s disease (AD) is a neurodegenerative disease that causes memory and cognitive decline as well as behavioral problems. It is a progressive and well recognized complex disease; therefore, it is very urgent to develop novel and effective anti... Read More about Novel and Potent Acetylcholinesterase Inhibitors for the Treatment of Alzheimer’s Disease from Natural (±)-7,8-Dihydroxy-3-methyl-isochroman-4-one.

Molecular glues modulate protein functions by inducing protein aggregation: A promising therapeutic strategy of small molecules for disease treatment (2022)
Journal Article
Wu, H., Yao, H., He, C., Jia, Y., Zhu, Z., Xu, S., Li, D., & Xu, J. (2022). Molecular glues modulate protein functions by inducing protein aggregation: A promising therapeutic strategy of small molecules for disease treatment. Acta Pharmaceutica Sinica B, 12(9), 3548-3566. https://doi.org/10.1016/j.apsb.2022.03.019

Molecular glues can specifically induce aggregation between two or more proteins to modulate biological functions. In recent years, molecular glues have been widely used as protein degraders. In addition, however, molecular glues play a variety of vi... Read More about Molecular glues modulate protein functions by inducing protein aggregation: A promising therapeutic strategy of small molecules for disease treatment.

Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease (2022)
Journal Article
Liu, Y., Uras, G., Onuwaje, I., Li, W., Yao, H., Xu, S., Li, X., Li, X., Phillips, J., Allen, S., Gong, Q., Zhang, H., Zhu, Z., Liu, J., & Xu, J. (2022). Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease. European Journal of Medicinal Chemistry, 235, Article 114305. https://doi.org/10.1016/j.ejmech.2022.114305

A series of sulfone analogs of donepezil were designed and synthesized as novel acetylcholinesterase (AChE) inhibitors with the potent inhibiting Aβ aggregation and providing neuroprotective effects as potential modalities for Alzheimer's disease (AD... Read More about Novel inhibitors of AChE and Aβ aggregation with neuroprotective properties as lead compounds for the treatment of Alzheimer's disease.

Gastroretentive technologies in tandem with controlled-release strategies: A potent answer to oral drug bioavailability and patient compliance implications (2021)
Journal Article
Vrettos, N. N., Roberts, C. J., & Zhu, Z. (2021). Gastroretentive technologies in tandem with controlled-release strategies: A potent answer to oral drug bioavailability and patient compliance implications. Pharmaceutics, 13(10), 1-36. https://doi.org/10.3390/pharmaceutics13101591

There have been many efforts to improve oral drug bioavailability and therapeutic efficacy and patient compliance. A variety of controlled-release oral delivery systems have been developed to meet these needs. Gastroretentive drug delivery technologi... Read More about Gastroretentive technologies in tandem with controlled-release strategies: A potent answer to oral drug bioavailability and patient compliance implications.

In vivo Evaluation of a Newly Synthesized Acetylcholinesterase Inhibitor in a Transgenic Drosophila Model of Alzheimer’s Disease (2021)
Journal Article
Uras, G., Manca, A., Zhang, P., Markus, Z., Mack, N., Allen, S., Bo, M., Xu, S., Xu, J., Georgiou, M., & Zhu, Z. (2021). In vivo Evaluation of a Newly Synthesized Acetylcholinesterase Inhibitor in a Transgenic Drosophila Model of Alzheimer’s Disease. Frontiers in Neuroscience, 15, Article 691222. https://doi.org/10.3389/fnins.2021.691222

Alzheimer’s disease is a neurodegenerative disease characterized by disrupted memory, learning functions, reduced life expectancy, and locomotor dysfunction, as a result of the accumulation and aggregation of amyloid peptides that cause neuronal dama... Read More about In vivo Evaluation of a Newly Synthesized Acetylcholinesterase Inhibitor in a Transgenic Drosophila Model of Alzheimer’s Disease.

Magnesium isoglycyrrhizinate reduces hepatic lipotoxicity through regulating metabolic abnormalities (2021)
Journal Article
Lu, L., Hao, K., Hong, Y., Liu, J., Zhu, J., Jiang, W., Zhu, Z., Wang, G., & Peng, Y. (2021). Magnesium isoglycyrrhizinate reduces hepatic lipotoxicity through regulating metabolic abnormalities. International Journal of Molecular Sciences, 22(11), Article 5884. https://doi.org/10.3390/ijms22115884

The excessive accumulation of lipids in hepatocytes induces a type of cytotoxicity called hepatic lipotoxicity, which is a fundamental contributor to liver metabolic diseases (such as NAFLD). Magnesium isoglycyrrhizinate (MGIG), a magnesium salt of t... Read More about Magnesium isoglycyrrhizinate reduces hepatic lipotoxicity through regulating metabolic abnormalities.

Discovery of Novel Tacrine–Pyrimidone Hybrids as Potent Dual AChE/GSK-3 Inhibitors for the Treatment of Alzheimer’s Disease (2021)
Journal Article
Yao, H., Uras, G., Zhang, P., Xu, S., Yin, Y., Liu, J., Qin, S., Li, X., Allen, S., Bai, R., Gong, Q., Zhang, H., Zhu, Z., & Xu, J. (2021). Discovery of Novel Tacrine–Pyrimidone Hybrids as Potent Dual AChE/GSK-3 Inhibitors for the Treatment of Alzheimer’s Disease. Journal of Medicinal Chemistry, 64(11), 7483-7506. https://doi.org/10.1021/acs.jmedchem.1c00160

Based on a multitarget strategy, a series of novel tacrine–pyrimidone hybrids were identified for the potential treatment of Alzheimer’s disease (AD). Biological evaluation results demonstrated that these hybrids exhibited significant inhibitory acti... Read More about Discovery of Novel Tacrine–Pyrimidone Hybrids as Potent Dual AChE/GSK-3 Inhibitors for the Treatment of Alzheimer’s Disease.

Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities (2021)
Journal Article
Zhu, H., Li, W., Shuai, W., Liu, Y., Yang, L., Tan, Y., Zheng, T., Yao, H., Xu, J., Zhu, Z., Yang, D.-H., Chen, Z.-S., & Xu, S. (2021). Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities. European Journal of Medicinal Chemistry, 216, Article 113316. https://doi.org/10.1016/j.ejmech.2021.113316

A series of novel N-benzylbenzamide derivatives were designed and synthesized as tubulin polymerization inhibitors. Among fifty-one target compounds, compound 20b exhibited significant antiproliferative activities with IC50 values ranging from 12 to... Read More about Discovery of novel N-benzylbenzamide derivatives as tubulin polymerization inhibitors with potent antitumor activities.