Article
Biochemistry & Molecular Biology
Yingchun Wu, Jinqiu Xue, Jia Li
Summary: This study reports the use of AR-PROTAC to treat AR-positive TNBC, demonstrating its superior therapeutic efficacy compared to AR inhibitors.
ARCHIVES OF BIOCHEMISTRY AND BIOPHYSICS
(2022)
Article
Multidisciplinary Sciences
Ryan Kolb, Umasankar De, Sajid Khan, Yuewan Luo, Myung-Chul Kim, Haijun Yu, Chaoyan Wu, Jiao Mo, Xin Zhang, Peiyi Zhang, Xuan Zhang, Nicholas Borcherding, Daniel Koppel, Yang-Xin Fu, Song Guo Zheng, Dorina Avram, Guangrong Zheng, Daohong Zhou, Weizhou Zhang
Summary: The pharmacological degradation of BCL-X-L preferentially induces apoptosis of tumor-infiltrating Tregs, promoting CD8 T cell activation and effective suppression of tumor growth without causing damage to normal tissues or thrombocytopenia. This finding suggests that targeting BCL-X-L could be a potential therapeutic strategy for cancer immunotherapy.
NATURE COMMUNICATIONS
(2021)
Article
Chemistry, Medicinal
Xiangbo Yang, Zhijia Wang, Yuan Pei, Ning Song, Lei Xu, Bo Feng, Hanlin Wang, Xiaomin Luo, Xiaobei Hu, Xiaohui Qiu, Huijin Feng, Yaxi Yang, Yubo Zhou, Jia Li, Bing Zhou
Summary: SHP2, a non-receptor tyrosine phosphatase, plays a crucial role in various oncogenic cell signaling cascades. PROTAC has emerged as a promising strategy for degrading disease-related proteins. Through the design and evaluation of a series of thalidomide-based heterobifunctional molecules, a highly efficient SHP2 degrader was identified, providing a new strategy for SHP2-mediated cancer therapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Multidisciplinary
Kwang-Su Park, Lihuai Qin, Md Kabir, Kaixiu Luo, Brandon Dale, Yue Zhong, Arum Kim, Gang Greg Wang, Husnu Umit Kaniskan, Jian Jin
Summary: The study discovered MS147, the first degrader of PRC1 core components BMI1 and RING1B, through a novel protein complex degradation strategy. MS147 degrades BMI1 and RING1B by binding to an EED small-molecule binder linked to the E3 ligase von Hippel-Lindau (VHL), effectively reducing the level of H2AK119ub and inhibiting the proliferation of cancer cell lines insensitive to PRC2 inhibitors/degraders.
Article
Biochemistry & Molecular Biology
Se Yong Park, Raju Gurung, Jung Ho Hwang, Alam Zeb, Jong-Ik Hwang, Sung Jean Park, Han-Joo Maeng, Dongyun Shin, Seung Hyun Oh
Summary: Oxidative stress caused by excessive accumulation of reactive oxygen species (ROS) is a major factor in the development of human diseases. Activation of NRF2 by inhibiting KEAP1 has shown promising results in combating oxidative stress-related diseases. In this study, a proteolysis-targeting chimera (PROTAC) called SD2267 was developed, which induced the degradation of KEAP1 and subsequent activation of NRF2.
Review
Chemistry, Multidisciplinary
Shenxin Zeng, Hongjie Zhang, Zhengrong Shen, Wenhai Huang
Summary: The combination of photopharmacology and PROTACs is gaining momentum for the discovery and development of new therapies, improving drug specificity and reducing off-target effects. PROTACs degrade pathogenic proteins for disease treatment, while photopharmacology allows precise control of drug activity.
FRONTIERS IN CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Tianzhi Wen, Jian Chen, Wenqian Zhang, Jiyan Pang
Summary: In this study, a series of small-molecule degraders were designed and synthesized based on a known alpha-synuclein aggregation inhibitor sery384. Compound 5 exhibited significant degradation effect on alpha-synuclein aggregates in a time- and dose-dependent manner in vitro.
Article
Chemistry, Medicinal
Eva Reznickova, Sona Krajcovicova, Miroslav Perina, Marketa Kovalova, Miroslav Soural, Vladimir Krystof
Summary: A novel pomalidomide-based PROTAC has been designed and prepared for the degradation of FLT3-ITD and CDK9 proteins in AML patients. The results of biochemical and cellular experiments showed selectivity and proteasome-dependent mechanism of action, resulting in the blockage of FLT3-ITD downstream signaling pathways, activation of apoptosis, cell cycle arrest, and reduced expression of crucial genes involved in AML pathogenesis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Jingwei Shao, Yuqian Yan, Donglin Ding, Dejie Wang, Yundong He, Yunqian Pan, Wei Yan, Anupreet Kharbanda, Hong-yu Li, Haojie Huang
Summary: DNA-binding proteins, such as transcription factors (TFs), are crucial in cellular processes and disease pathogenesis, but are difficult to target therapeutically due to their lack of enzymatic catalytic sites. PROTAC technology involves engineering bifunctional molecules to induce degradation of target proteins through ubiquitination. O'PROTACs, which incorporate a TF-recognizing double-stranded oligonucleotide, have been shown to effectively degrade cancer-related transcription factors like LEF1 and ERG, inhibiting cancer cell growth both in vitro and in vivo. These programmable O'PROTACs show promise as a tool for targeting various TFs for disease treatment.
Review
Cell Biology
Ludovica Lospinoso Severini, Francesca Bufalieri, Paola Infante, Lucia Di Marcotullio
Summary: This paragraph discusses the importance of post-translational modifications, such as ubiquitylation, and introduces the PROteolysis-TArgeting Chimera (PROTAC) technology. PROTACs utilize the cell's Ubiquitin-Proteasome System to degrade target proteins and have potential therapeutic applications in cancer treatment.
FRONTIERS IN CELL AND DEVELOPMENTAL BIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Salma Darwish, Ehab Ghazy, Tino Heimburg, Daniel Herp, Patrik Zeyen, Rabia Salem-Altintas, Johannes Ridinger, Dina Robaa, Karin Schmidtkunz, Frank Erdmann, Matthias Schmidt, Christophe Romier, Manfred Jung, Ina Oehme, Wolfgang Sippl
Summary: This study developed proteolysis targeting chimeras (PROTACs) of HDAC8 based on potent and selective HDAC8 inhibitors. The selective HDAC8 PROTACs showed anti-neuroblastoma activity in cells, indicating their potential as targeted therapy for neuroblastoma.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Chemistry, Medicinal
Xiao-Xiao Xi, Hong-Yi Zhao, Yu-Ze Mao, Minhang Xin, San-Qi Zhang
Summary: The compound Os30, derived from osimertinib, exhibits potent inhibitory activities against EGFR with C797S mutation, both in vitro and in vivo.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Quanyu Liu, Guihui Tu, Yan Hu, Qingna Jiang, Jingwen Liu, Shanshan Lin, Zelei Yu, Ge Li, Xinhua Wu, Yuanling Tang, Xiuwang Huang, Jianhua Xu, Yang Liu, Lixian Wu
Summary: This study systematically described the design, synthesis, and evaluation of HSP90 degraders based on the PROTAC strategy. The candidate compound 16b (BP3) was found to effectively degrade HSP90 and inhibit the growth of human breast cancer cells. The results suggest that the HSP90-targeting PROTAC strategy has potential novel applications in breast cancer therapy.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Oncology
Nozomu Nakagawa, Noriko Miyake, Nobuaki Ochi, Hiromichi Yamane, Masami Takeyama, Yasunari Nagasaki, Tomoko Ikeda, Etsuko Yokota, Takuya Fukazawa, Hidekazu Nakanishi, Daijiro Harada, Katsuyuki Kiura, Nagio Takigawa
Summary: Targeting ROR1 in combination with osimertinib may provide a novel therapeutic option for EGFR mutant lung cancer by suppressing cell growth, colony formation, and inducing apoptosis.
EXPERIMENTAL CELL RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
Baohua Xie, Bin Xu, Lilan Xin, Yizhou Wei, Xinyi Guo, Chune Dong
Summary: To address the potential off-target effects of antitumor drugs, a study developed hypoxia-responsive PROTACs targeting estrogen receptor a (ERa) for breast cancer treatment. The introduction of two hypoxia-activated groups, nitroimidazole and nitrobenzene, improved the safety of active PROTAC by reducing its toxicity in normal cells. The hypoxia-responsive PROTACs showed excellent responsiveness and degradation activity under hypoxic conditions, providing a new strategy for precise control of PROTAC drugs in breast cancer treatment.
BIOORGANIC CHEMISTRY
(2023)
Article
Neurosciences
Ting Yang, Xueping Li, Peng Xia, Xiaoju Wang, Jianqiang Lu, Lin Wang
Summary: This study evaluated the effect of rTMS combined with rPMS on stroke patients with arm paralysis after CSCNTS. The results showed that this combined treatment significantly reduced muscle tone and increased grip and pinch strength.
INTERNATIONAL JOURNAL OF NEUROSCIENCE
(2023)
Article
Geriatrics & Gerontology
Jiulong Song, Lijun Wei, Kai Cheng, Qiang Lin, Peng Xia, Xinwei Wang, Xiaoju Wang, Ting Yang, Baoyi Chen, Aimei Ding, Mingyi Sun, Anliang Chen, Xueping Li
Summary: The study found that modified Tai Chi exercises are effective in improving physical function and quality of life in elderly women with knee osteoarthritis (KOA).
FRONTIERS IN AGING NEUROSCIENCE
(2022)
Article
Chemistry, Multidisciplinary
Junjun Ma, Xiaoju Wang, Yonghuan Bian, Changyong Zhang, Chun Liu, Jianrui Niu, Jing Zhang, Ge Shen, Jie Liu
Summary: A spiral mosquito-repellent incense-shaped channel was designed and used in a flow electrode capacitive deionization system. Computational fluid dynamics analysis was conducted to study its hydrodynamic performance. The newly designed channel showed low flow resistance and minimal stagnant regions. The effects of flow rate and mass loading on desalination performance were investigated and compared to traditional runway and snake-shaped channels. The MR-shaped channel exhibited a higher salt removal rate. Vortices in the corners of the traditional channels aided in charge transfer.
ACS SUSTAINABLE CHEMISTRY & ENGINEERING
(2022)
Correction
Cell & Tissue Engineering
Xinwei Wang, Danbi Wang, Peng Xia, Kai Cheng, Qi Wang, Xiaoju Wang, Qiang Lin, Jiulong Song, Anliang Chen, Xueping Li
BONE & JOINT RESEARCH
(2022)
Article
Orthopedics
Peng Xia, Qi Wang, Jiulong Song, Xiaoju Wang, Xinwei Wang, Qiang Lin, Kai Cheng, Anliang Chen, Xueping Li
Summary: The study showed that LIPUS can promote MSC exosome release by activating autophagy, enhancing the positive effects of MSCs on OA cartilage repair. In vivo results demonstrated that LIPUS significantly improved the therapeutic efficacy of MSCs in OA cartilage repair, possibly through increasing autophagy-mediated exosome release.
Article
Psychology, Multidisciplinary
Jun Lei, Yaoyue Luo, Yude Xie, Xiaoju Wang
Summary: This study examined the association between VAI and depression in the American population using NHANES data. The results showed that for every 1 unit increase in VAI, the clinical depression increased by 14%. Patients with high VAI scores had the highest risk of developing depression.
FRONTIERS IN PSYCHOLOGY
(2022)
Article
Behavioral Sciences
Xiaoju Wang, Peng Xia, Jiulong Song, Ting Yang, Changjun Yu, Kai Cheng, Anliang Chen, Xueping Li
Summary: CES improves depression-like behavior of PSD rats through upregulation of GPX4-mediated BDNF expression in the hippocampus.
BEHAVIOURAL BRAIN RESEARCH
(2023)
Article
Engineering, Environmental
Jie Liu, Junjun Ma, Weizhang Zhong, Jianrui Niu, Zaixing Li, Xiaoju Wang, Ge Shen, Chun Liu
Summary: Membrane capacitive deionization (MCDI) is an efficient desalination technology. In this study, penicillin fermentation residue biochar (PFRB) was used as an electrode in the MCDI system, showing a high-capacity desalination performance. The PFRB electrode exhibited excellent electrochemical properties and stability.
FRONTIERS OF ENVIRONMENTAL SCIENCE & ENGINEERING
(2023)
Article
Engineering, Environmental
Ge Shen, Junjun Ma, Jianrui Niu, Ruina Zhang, Jing Zhang, Xiaoju Wang, Jie Liu, Jiarong Gu, Ruicheng Chen, Xiqing Li, Chun Liu
Summary: Capacitive deionization (CDI) is a novel electrochemical water-treatment technology that utilizes activated carbon (AC) as an electrode material. This study adopted ball milling to produce ball milled AC (BAC) with improved physical and electrochemical properties. BAC exhibited excellent pore structures and favorable surfaces for ion adsorption, leading to reduced electron transfer resistance and ion migration resistance. The average salt adsorption rates and energy-normalized removal salt were significantly enhanced in both membrane capacitive deionization (MCDI) and flow-electrode capacitive deionization (FCDI) using BAC as the electrode material.
FRONTIERS OF ENVIRONMENTAL SCIENCE & ENGINEERING
(2023)
Article
Chemistry, Inorganic & Nuclear
Xinxin Hang, Xiaoju Wang, Meilin Wang, Mengwei Chen, Yanfeng Bi
Summary: The integration of heterometallic units into coordination clusters can enhance their electrocatalytic performance. In this study, a series of coordination clusters were synthesized using different metal precursors and ligands, and they showed improved activity in the oxygen evolution reaction.
INORGANIC CHEMISTRY FRONTIERS
(2023)
Article
Environmental Sciences
Xiaoju Wang, Shanshan Hu, Haitao Mao, Xueyu Wei, Saraschandra Naraginti
Summary: Recently, there has been increasing attention on the development of efficient materials for degradation and detoxification of antibiotics in wastewater treatment. AgVO3, as a visible light active material, has been widely studied for environmental remediation. In this research, a novel heterojunction of AgVO3/rGO/BiVO4 was prepared through a hydrothermal method to improve its efficiency and stability. The results showed that the degradation efficiency of AgVO3/rGO/BiVO4 towards Norfloxacin (NFC) antibiotic was significantly higher compared to pure AgVO3 and BiVO4. The enhanced efficiency can be attributed to the formation of heterojunction and faster charge separation.
ENVIRONMENTAL RESEARCH
(2023)
Article
Chemistry, Multidisciplinary
Luyao Wang, Qingbo Wang, Emil Rosqvist, Jan-Henrik Smatt, Qiwen Yong, Lippo Lassila, Jouko Peltonen, Thomas Rosenau, Martti Toivakka, Stefan Willfoer, Patrik Eklund, Chunlin Xu, Xiaoju Wang
Summary: Fabricating bio-latex colloids with core-shell nanostructure is an effective method for obtaining films with enhanced mechanical characteristics. Nano-sized lignin is rising as a class of sustainable nanomaterials that can be incorporated into latex colloids. The correlation between surface chemistry of lignin nanoparticles (LNPs) and integration efficiency in latex colloids and from it thermally processed latex films is explored.
Article
Engineering, Biomedical
Qingbo Wang, Ozge Karadas, Oskar Backman, Luyao Wang, Tuomas Nareoja, Jessica M. Rosenholm, Chunlin Xu, Xiaoju Wang
Summary: In this study, a ternary-component aqueous emulsion was used to fabricate microgel assembly for 3D bioprinting. The emulsion consisted of methacrylated gelatin (GelMA) microgels, methacrylated galactoglucomannan (GGMMA), and dextran (Dex). The GGMMA and Dex provided stability to the emulsion, while GGMMA also facilitated the adhesion of GelMA microgels to form a porous hydrogel construct that supported cell growth and colonization.
ADVANCED HEALTHCARE MATERIALS
(2023)
Article
Medicine, General & Internal
Pei Zhang, Jing Liao, Xiaoju Wang, Zhengping Feng
Summary: The present study compared the effects of high glucose and glucose fluctuation on apoptosis and autophagy in MC3T3-E1 osteoblasts. The results showed that high glucose and glucose fluctuation decreased cell proliferation and activated autophagy. They also induced oxidative stress, mitochondrial damage, and apoptosis, with more significant differences observed in the glucose fluctuation group. Antioxidant treatment eliminated reactive oxygen species, inhibited autophagy and apoptosis, while autophagy inhibition enhanced apoptosis in the osteoblasts.
ARCHIVES OF MEDICAL SCIENCE
(2023)
Meeting Abstract
Oncology
Lanbo Xiao, Abhijit Parolia, Yuanyuan Qiao, Pushpinder Bawa Pushpinder, Sanjana Eyunni, Rahul Mannan, Sandra E. Carson, Yu Chang, Xiaoju Wang, Yuping Zhang, Josh Vo, Steven Kregel, Stephanie A. Simko, Andrew D. Delekta, Mustapha Jaber, Heng Zheng, Ingrid Apel, Lisa McMurry, Fengyun Su, Rui Wang, Sylvia Wang, Sanjita Sasmal, Leena K. Satyam, Subhendu Mukherjee, Chandrasekhar Abbinen, Kiran Aithal, Mital S. Bhakta, Jay Ghurye, Xuhong Cao, Nora M. Navone, Alexey Nesvizhskii, Rohit Mehra, Ulka Vaishampayan, Marco Blanchette, Yuzhuo Wang, Susanta Samajdar, Murali Ramachandra, Arul M. Chinnaiyan
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
