Article
Pharmacology & Pharmacy
Haobin Li, Lingling Wang, Fei Cao, Dehua Yu, Jing Yang, Xuefei Yu, Jinyun Dong, Jiang-Jiang Qin, Xiaoqing Guan
Summary: The study reports the design and synthesis of a class of STAT3 degraders based on proteolysis-targeting chimeras (PROTACs). The SDL-1 compound achieved degradation of STAT3 protein in vitro and exhibited good anti-gastric cancer cell proliferation activity, as well as inhibiting invasion and metastasis.
FRONTIERS IN PHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
Le Guo, Yaxian Zhou, Xueqing Nie, Zhongrui Zhang, Zhen Zhang, Chunrong Li, Taobo Wang, Weiping Tang
Summary: PROTAC is a commonly used technology for targeted protein degradation, and the Rapid-TAC platform enables rapid synthesis of PROTAC through traceless coupling reaction, saving time and facilitating screening of active protein degraders.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Chao Wang, Cangxin Zheng, Han Wang, Liangren Zhang, Zhenming Liu, Ping Xu
Summary: Protein degradation technology has made significant progress since its first report in 2001. Various degradation technologies based on PROTAC have been developed for different targets, expanding the possibilities for treating cancer, neurodegenerative diseases, and viral diseases. Over 15 targeted degraders have entered clinical trials to date.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Pharmacology & Pharmacy
Tian Zhang, Shuai Guo, Fangzhou Li, Xinmiao Lan, Yaru Jia, Jinchao Zhang, Yuanyu Huang, Xing-Jie Liang
Summary: This review emphasizes the importance of timely and accurate assessment and diagnosis for various diseases, introduces the application of molecular imaging technology in disease diagnosis and treatment, and aims to promote the development of related technologies and fields.
ADVANCED DRUG DELIVERY REVIEWS
(2022)
Review
Food Science & Technology
Rosalba Leuci, Leonardo Brunetti, Viviana Poliseno, Antonio Laghezza, Fulvio Loiodice, Paolo Tortorella, Luca Piemontese
Summary: This article reviews the recent literature on the discovery of secondary metabolites from plants and fungi, including isolation, structural elucidation, and evaluation of biological effects. The potential use of these bioactive molecules in preventing and treating cardiovascular and neurodegenerative diseases is discussed.
Article
Chemistry, Medicinal
Wenqing Li, Jiabin Zhang, Li Guo, Qiantao Wang
Summary: This study explores the use of molecular dynamics simulation and molecular mechanics combined with the generalized Born and surface area continuum solvation (MM/GBSA) method to solve the three-body problem in PROTAC modeling. The results validate the accuracy of the approach and demonstrate the qualitative and quantitative importance of PROTAC-induced protein-protein interactions in its modeling.
JOURNAL OF CHEMICAL INFORMATION AND MODELING
(2022)
Review
Pharmacology & Pharmacy
Zhimin Yang, Yanyu Li, Zihua Wang
Summary: Exosomes are important communication carriers between cells and can be used for disease diagnosis and treatment. MSCs-Exo, as a natural drug delivery carrier, has therapeutic effects and is increasingly used in the treatment of cardiovascular diseases and neurodegenerative diseases.
Review
Medicine, Research & Experimental
Roshanak Amirian, Mehdi Azadi Badrbani, Hossein Derakhshankhah, Zhila Izadi, Mohammad-Ali Shahbazi
Summary: Parkinson's disease is a neurodegenerative disorder characterized by the misfolding and aggregation of α-synuclein. Targeted Protein Degradation is an emerging approach that shows promise in treating Parkinson's disease by selectively breaking down specific proteins.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Review
Biochemistry & Molecular Biology
Wen Li, Reham M. Elhassan, Xuben Hou, Hao Fang
Summary: The PROTAC technology, based on the ubiquitin-proteasome system, has become a potential strategy for targeted cancer therapy. It has advantages over traditional small-molecule inhibitors in terms of pharmacodynamics, selectivity, and drug resistance. Several small molecule PROTACs are currently in Phase I clinical trial, showing promising advances in targeted anticancer research.
CURRENT MEDICINAL CHEMISTRY
(2021)
Review
Immunology
Yinwei Chen, Jinghua Zhou, Li Wang
Summary: The human gut microbiome plays a crucial role in human health, and dysbiosis may lead to various chronic diseases. The mechanisms of its impact on neurodegenerative diseases, cardiovascular diseases, metabolic diseases, and gastrointestinal diseases are extremely complex.
FRONTIERS IN CELLULAR AND INFECTION MICROBIOLOGY
(2021)
Review
Pharmacology & Pharmacy
Weipeng Wei, Denglei Ma, Lin Li, Lan Zhang
Summary: Multiple sclerosis is an autoimmune and chronic inflammatory demyelinating disease of the central nervous system, with no complete cure currently available but drugs that can slow down its progression. Traditional therapies mainly focus on disease-modifying drugs to control severity, while new drugs and treatment strategies are being developed.
FRONTIERS IN PHARMACOLOGY
(2021)
Review
Chemistry, Physical
Tanima Bhattacharya, Giselle Amanda Borges e Soares, Hitesh Chopra, Md. Mominur Rahman, Ziaul Hasan, Shasank S. Swain, Simona Cavalu
Summary: The strategies for therapeutics development for neurodegenerative disorders are complex and challenging due to the blood-brain barrier. Nanotechnology combined with phytomedicine shows promise in enhancing drug delivery to the brain and reducing adverse effects.
Article
Chemistry, Medicinal
Shulei Zhu, Jieyu Liu, Donghuai Xiao, Peipei Wang, Jingkun Ma, Xiaobei Hu, Jingfeng Fu, Yubo Zhou, Jia Li, Wei Lu
Summary: This study reports a novel Wee1 degrader based on PROTAC technology, which effectively degrades cellular Wee1 protein and has potential applications in cancer therapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
You-lu Pan, Shen-xin Zeng, Rong-rong Hao, Mei-hao Liang, Zheng-rong Shen, Wen-hai Huang
Summary: This review summarizes the current research progress of inhibitors and degraders targeting BCR-ABL for the treatment of CML, including first, second, and third-generation tyrosine kinase inhibitors targeting different mutations, as well as allosteric inhibitors and proteolysis-targeting chimeras (PROTAC) based on different E3 ligands.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Lucja Justyna Walczak-Nowicka, Mariola Herbet
Summary: Acetylcholinesterase (AChE) plays a crucial role in the pathogenesis of neurodegenerative diseases, with ongoing research focusing on identifying new AChE inhibitors to potentially treat these diseases. The review highlights the importance of AChE inhibitors and their potential use in developing therapies for neurodegenerative diseases. Further investigations into designing and discovering new drugs targeting AChE may lead to effective treatments for neurodegenerative diseases in the future.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)