Article
Chemistry, Multidisciplinary
Jing Wei, Keke Han, Xiuli You, Mengxia Zhang, Zhenhong Wei, Haina Zhang, Hu Cai
Summary: The synthesis of two three-dimensional organic-inorganic hybrid perovskite compounds using RbX as cosolvent and reducing molecular symmetry has been achieved. These compounds exhibit reversible phase transition, dielectric, second harmonic generation, and ferroelectric properties.
CHEMISTRY-A EUROPEAN JOURNAL
(2022)
Article
Chemistry, Multidisciplinary
Xiuli You, Wenjun Rao, Keke Han, Lingyu Wang, Mengxia Zhang, Zhenhong Wei
Summary: In this study, two compounds with high phase transition points were successfully synthesized by reacting different molecules 1,4-diazabicyclo[3.2.2]-nonane (3.2.2-dabcn) with different reactants. These compounds showed switchable phase transition and dielectric properties, and compound 1 also exhibited a reversible second-harmonic-generation effect.
NEW JOURNAL OF CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Niels Heise, Sander Friedrich, Veronika Temml, Daniela Schuster, Bianka Siewert, Rene Csuk
Summary: The study demonstrated that the acetylated triterpenoic acids could effectively inhibit the enzyme butyrylcholinesterase (BChE) while showing weak inhibition for acetylcholinesterase (AChE). Enzyme kinetics evaluation revealed hyperbolic inhibition for BChE, and molecular modeling explained the selectivity between AChE and BChE for these compounds.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Keke Han, Mengxia Zhang, Zhenhong Wei, Xing Ye, Wenjun Rao, Haina Zhang, Hu Cai
Summary: In this study, the reactions of 1,5-diazabicyclo[3.2.2]nonane (3.2.2-dabcn) with rubidium halides were investigated, resulting in the formation of two 3D molecular ferroelectrics.
CHEMICAL COMMUNICATIONS
(2022)
Article
Neurosciences
Melissa A. Tapia, Xiao-Tao Jin, Brenton R. Tucker, Leanne N. Thomas, Noah B. Walker, Veronica J. Kim, Steven E. Albertson, Naresh Damuka, Ivan Krizan, Seby Edassery, Jeffrey N. Savas, Kiran Kumar Solingapuram Sai, Sara R. Jones, Ryan M. Drenan
Summary: This study investigated the behavior and neurobiological effects of intermittent nicotine intake in rats. The results suggest that intermittent nicotine intake may lead to increased craving and enhanced response to nicotine-associated cues. Additionally, intermittent nicotine intake also caused increased nicotine binding in the brain and specific changes in the proteome of certain neural structures.
Article
Immunology
Alice Courties, Juliette Petit, Ariane Do, Manon Legris, Ines Kouki, Audrey Pigenet, Pradeep K. Sacitharan, Francois-Paul Ehkirch, Francis Berenbaum, Jeremie Sellam
Summary: This study investigated the role of non-neuronal cholinergic system in osteoarthritis (OA). The results showed that the cholinergic system, through alpha 7nAchR, can counteract the effects of inflammation on osteoblasts. Deletion of alpha 7nAchR may limit cartilage degradation in age-related OA. Therefore, enhancing the cholinergic system could be a potential therapeutic target, although it may depend on CHRFAM7A expression.
FRONTIERS IN IMMUNOLOGY
(2022)
Article
Cell Biology
Yujie Zhang, Yilin Sun, Yanfei Jia, Qian Zhang, Ping Zhu, Xiaoli Ma
Summary: Recent studies have shown that the overexpression of alpha 5 nicotinic acetylcholine receptor (alpha 5-nAChR) and survivin in lung adenocarcinoma (LUAD) is associated with worse clinical outcomes. Coexpression of alpha 5-nAChR and survivin in LUAD patients is indicative of a poorer prognosis. Targeting both alpha 5-nAChR and survivin may present a promising therapeutic strategy for the diagnosis of LUAD.
JOURNAL OF CELLULAR PHYSIOLOGY
(2021)
Article
Cell Biology
Irida Papapostolou, Daniela Ross-Kaschitza, Florian Bochen, Christine Peinelt, Maria Constanza Maldifassi
Summary: Nicotine in tobacco induces tumor-promoting effects and chemotherapy resistance through nicotinic acetylcholine receptors (nAChRs). This study investigates the role of a5 subunit in nicotine-induced cancer cell proliferation and migration in breast, colon, and prostate cancer cells. The results show that nicotine-induced proliferation and migration are mediated by a5.
Article
Oncology
Qian Zhang, Ying Jia, Pan Pan, Xiuping Zhang, Yanfei Jia, Ping Zhu, Xiaowei Chen, Yang Jiao, Guiyu Kang, Lulu Zhang, Xiaoli Ma
Summary: This study uncovers a new interaction between alpha 5-nAChR and Ly6E that inhibits cancer cell migration by modulating the TGF-beta 1/Smad signaling pathway in NSCLC.
Article
Chemistry, Medicinal
Si Pan, Yingxu Fan, Xiaopeng Zhu, Yi Xue, Sulan Luo, Xinquan Wang
Summary: The study elucidates the critical role of alpha 9-containing nicotinic acetylcholine receptors in neuropathic pain and reveals the key residues of alpha 9 alpha 10 nAChR that determine their high affinity for RgIA/RgIA4 through co-crystal structure and molecular dynamic simulations. This provides valuable insights for designing new therapeutic approaches for neuropathic pain.
Article
Neurosciences
Sergey G. Khasabov, Victoria M. Rogness, Montana B. Beeson, Lucy Vulchanova, Li-Lian Yuan, Donald A. Simone, Phu Tran
Summary: Loss of neuronal-specific TMEM35a (NACHO) leads to heightened pain sensitivity in mice and affects pain responses; NACHO in the spinal cord may be involved in increased neuroinflammation.
Article
Pharmacology & Pharmacy
Qiao-Qiao Han, Min Yin, Zi-Ying Wang, Hao Liu, Jun-Ping Ao, Yong-Xiang Wang
Summary: The study found that cynandione A suppresses neuropathic pain through an alpha 7-nAChR-dependent IL-10/beta-endorphin signaling pathway in spinal microglia.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Neurosciences
Shachi Shuchi Smita, Mashu Trivedi, Deepika Tripathi, Shashi Pandey-Rai, Rakesh Pandey
Summary: The study explores the potential of Asparagus racemosus extract (ARE) and its bioactive molecule Shatavarin IV (SIV) in improving cholinergic transmission, showing significant modulation in cholinergic function through increasing acetylcholine levels and nicotinic acetylcholine receptors activity. Further investigations suggest that ARE and SIV modulate synaptic ACh levels by blocking acetyl cholinesterase and regulating the synthesis of ACh, resulting in enhanced nAChR activity and lowering oxidative damage by diminishing ROS.
NEUROSCIENCE LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Qiang Li, Jingtan Li, Jingting Wang, Jing Wang, Tong Lu, Yanfei Jia, Haiji Sun, Xiaoli Ma
Summary: Evidence has shown a strong relationship between smoking and epithelial mesenchymal transition (EMT) in lung adenocarcinoma (LUAD). This study identifies a novel pathway involving alpha 5-nicotinic acetylcholine receptor (alpha 5-nAChR), PLEK2, and CFL1 in nicotine-induced LUAD progression. The alpha 5-nAChR/PLEK2/CFL1 pathway contributes to cell migration, invasion, and stemness in LUAD.
MOLECULAR CARCINOGENESIS
(2023)
Article
Toxicology
Max Epstein, Karan Bali, Thomas J. Piggot, A. Christopher Green, Christopher M. Timperley, Mike Bird, John E. H. Tattersall, Isabel Bermudez, Philip C. Biggin
Summary: Organophosphorus nerve agents are highly toxic chemical warfare agents that have been used since the 1930s. While there are several antidotes available, none directly target the toxic component of these agents. Research shows that nonoxime bispyridinium compounds can improve detoxification effects.
TOXICOLOGY LETTERS
(2021)
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)