Article
Biochemistry & Molecular Biology
Hongtao Du, Jinzhi Song, Fang Ma, Hongxin Gao, Xinyan Zhao, Renjun Mao, Xiaolong He, Yan Yan
Summary: This study synthesised and characterised a series of novel harmine derivatives as potential ligands for AD treatment. Compounds 13 and 17d showed exceptional neuroprotective effects and potent inhibition against AChE and A beta aggregation. Kinetic studies and molecular modelling confirmed the interaction of compound 13 with both CAS and PAS of AChE.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Medicine, Research & Experimental
Sagheer Ahmed, Sidrah Tariq Khan, Muhammad Kazim Zargaham, Arif Ullah Khan, Saeed Khan, Abrar Hussain, Jalal Uddin, Ajmal Khan, Ahmed Al-Harrasi
Summary: Alzheimer's disease is the most common type of dementia affecting the later years of life and will be a major burden on the healthcare system. Despite scientific advancements, there are still no therapies available to stop or slow the progression of the disease. FDA has approved certain drugs for AD treatment, but research also suggests potential benefits from herbal compounds.
BIOMEDICINE & PHARMACOTHERAPY
(2021)
Article
Biochemistry & Molecular Biology
Yi-Yan Sie, Liang-Chieh Chen, Cai-Jhen Li, Yu-Hsiang Yuan, Sheng-Hung Hsiao, Mei-Hsien Lee, Ching-Chiung Wang, Wen-Chi Hou
Summary: Currently, there is no effective drug for delaying the cognitive impairment of Alzheimer's disease, which is one of the top 10 causes of death worldwide. Hydroxylated stilbenes, active compounds found in fruit and herbal plants, were evaluated for their effects on Alzheimer's disease-associated factors. Piceatannol (PIC) showed the most significant activities in scavenging radicals, inhibiting acetylcholinesterase and amyloid-beta aggregations, and improving learning behavior in animal tests.
Review
Chemistry, Multidisciplinary
Jiyeon Han, Zhi Du, Mi Hee Lim
Summary: Alzheimer's disease is the most common form of dementia characterized by memory loss and cognitive decline. Various pathological factors, including A beta aggregates, reactive oxygen species, metal ions, and acetylcholinesterase, contribute to the complexity of the disease. Developing small-molecule-based chemical tools targeting these factors could provide potential therapeutic strategies for Alzheimer's disease.
ACCOUNTS OF CHEMICAL RESEARCH
(2021)
Review
Biochemistry & Molecular Biology
Anna Bubley, Alexaner Erofeev, Peter Gorelkin, Elena Beloglazkina, Alexander Majouga, Olga Krasnovskaya
Summary: Alzheimer's disease (AD) is a neurodegenerative disorder characterized by Aβ aggregation, tau hyperphosphorylation, and loss of cholinergic neurons. AD is also associated with oxidative stress, metal dyshomeostasis, inflammation, and cell cycle dysregulation. In this review, THA-based hybrids are summarized as potential anti-AD agents, highlighting strategies for drug design that have led to cognitive improvements and reduced hepatotoxicity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Article
Geriatrics & Gerontology
Chan Liu, Zhipei Sang, Hong Pan, Qin Wu, Yu Qiu, Jingshan Shi
Summary: The study synthesized a novel multi-target-directed ligand (AP5) and used computational simulations and in vivo pharmacokinetic evaluations to confirm its potential. The results showed that AP5 can simultaneously bind to the peripheral and catalytic sites of AChE and has desirable pharmacokinetic characteristics and drug-likeness. AP5 can inhibit AChE activity and AChE-induced Aβ aggregation, reduce Aβ plaque deposition, suppress inflammation, and prevent neuronal and synaptic damage in Alzheimer's disease models.
FRONTIERS IN AGING NEUROSCIENCE
(2022)
Review
Chemistry, Medicinal
Yuanyuan Liu, Lin Cong, Chu Han, Bo Li, Rongji Dai
Summary: As the world's population ages, Alzheimer's disease has become a global concern. Despite some understanding of the disease's pathological features, there is still a lack of effective prevention and treatment drugs available.
MINI-REVIEWS IN MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Maria Elisabetta Clementi, Beatrice Sampaolese, Gabriele Di Sante, Francesco Ria, Rosa Di Liddo, Vincenzo Romano Spica, Fabrizio Michetti
Summary: The study demonstrated that the expression of S100B in astrocytoma cells plays a crucial role in the activation of reactive astrocytic processes, including cytotoxicity, ROS and NOS activation. Silencing S100B in astrocytoma cells effectively protected the cells from amyloid beta-peptide-induced damage, reducing cell death, oxygen radical generation and nitric oxide synthase activity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Pharmacology & Pharmacy
Debora A. Moreira, Sofia D. Santos, Victoria Leiro, Ana P. Pego
Summary: Alzheimer's disease (AD) affects over 30 million people worldwide and is characterized by the accumulation of amyloid beta peptide and hyperphosphorylated tau aggregates in the brain. Currently, there are limited approved drugs for AD treatment, and the majority of patients have no disease-modifying options. Nanobiomaterials, especially dendrimers, offer potential as multifunctional and multitargeted therapies for AD. Dendrimers have unique characteristics as drug carriers and also display anti-amyloidogenic properties. This review discusses the properties of dendrimers and derivatives that make them excellent AD nanotherapeutics, their use as drugs, and the challenges in their clinical application.
Article
Biochemistry & Molecular Biology
Marwa El-Hussieny, Mansoura A. Abd-El-Maksoud, Fouad M. Soliman, Marwa A. Fouad, Mohamed K. El-Ashrey
Summary: Alzheimer's disease is a neurodegenerative disease with no prevention or complete cure. In this study, researchers synthesized new triphenylphosphoranylidene derivatives and tested their biological activity against AChE and beta-amyloid proteins. The derivative 8c showed promising results as an AChE inhibitor, but lacked selectivity and had potential for structural modification to improve selectivity. Compound 8c also exhibited low cytotoxicity and showed good penetration into the blood-brain barrier and binding affinity with AChE.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Jofre Seira Curto, Maria Rosario Fernandez, Josep Cladera, Nuria Benseny-Cases, Natalia Sanchez de Groot
Summary: Homeostasis is crucial for cell function and disturbances in homeostasis can lead to health disorders. This study investigated how pH levels affect the aggregation of amyloid-beta-peptide (A beta) and the development of Alzheimer's disease. The results showed that the brain pH and different aggregated conformations play a role in the aggregation process. Furthermore, neutral pH and physiological salt concentrations were found to favor a slow aggregation with low cytotoxic effects.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Biochemistry & Molecular Biology
Hossein Ashrafian, Elaheh Hadi Zadeh, Rizwan Hasan Khan
Summary: Approximately 40 million people globally suffer from dementia, with Alzheimer's disease being the most common cause. Aggregation of Aβ outside of neuron cells and tau protein tangle formation inside cells are believed to play crucial roles. This paper reviews studies targeting the inhibition of these protein aggregations to suppress or postpone AD.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2021)
Article
Chemistry, Physical
Siddhartha Banerjee, Divya Baghel, Md Hasan Ul Iqbal, Ayanjeet Ghosh
Summary: Spontaneous aggregation of amyloid beta (Afi) proteins is a key pathological feature of Alzheimer's disease, but the structure of early-stage aggregates is not well understood. This study used atomic force microscopy-infrared nanospectroscopy to investigate the aggregation process of Afi 16-22 and found a structural transition from oligomers with parallel β-sheets to antiparallel fibrils.
JOURNAL OF PHYSICAL CHEMISTRY LETTERS
(2022)
Article
Plant Sciences
Yu Jin Kim, Eunjin Sohn, Hye-Sun Lim, Yoonju Kim, Joo-Hwan Kim, Soo-Jin Jeong
Summary: Bauhinia coccinea extracts were analyzed for chemical composition and studied for their effects on neuroprotection, antioxidation, and Alzheimer's disease marker molecules. The results showed that the extracts exhibit anti-AChE activation and A beta aggregation activities, suggesting them as potential sources for Alzheimer's disease medication.
Review
Chemistry, Medicinal
Yash P. Singh, Harish Kumar
Summary: Alzheimer's disease is a chronic neurodegenerative disease associated with aging, characterized by progressive memory loss and cognitive impairment. The current clinical treatment options for AD are limited and the use of tryptamine and its analogs as multifunctional agents shows promise for AD therapy.
DRUG DEVELOPMENT RESEARCH
(2023)
Article
Environmental Sciences
Yong-Xin Li, Yong Li, Jae-Young Je, Se-Kwon Kim
ENVIRONMENTAL TOXICOLOGY AND PHARMACOLOGY
(2015)
Article
Chemistry, Applied
Dai-Hung Ngo, Kyong-Hwa Kang, BoMi Ryu, Thanh-Sang Vo, Won-Kyo Jung, Hee-Guk Byun, Se-Kwon Kim
Review
Chemistry, Applied
Dai-Hung Ngo, Thanh-Sang Vo, Dai-Nghiep Ngo, Kyong-Hwa Kang, Jae-Young Je, Hoang Nguyen-Duc Pham, Hee-Guk Byun, Se-Kwon Kim
FOOD HYDROCOLLOIDS
(2015)
Article
Food Science & Technology
Quang Van Ta, Minseok Yoon, Hyejin Yang, Jiyoung Kim, Suengmok Cho, Kyong-Hwa Kang, Young-Sang Kim, Sun-Joo Park, Se-Kwon Kim
FOOD SCIENCE AND BIOTECHNOLOGY
(2015)
Article
Biochemistry & Molecular Biology
Panchanathan Manivasagan, Jayachandran Venkatesan, Kyong-Hwa Kang, Kannan Sivakumar, Sun-Joo Park, Se-Kwon Kim
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2015)
Article
Biochemistry & Molecular Biology
Panchanathan Manivasagan, Kyong-Hwa Kang, Dong Gyu Kim, Se-Kwon Kim
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2015)
Review
Biochemistry & Molecular Biology
Jayachandran Venkatesan, Ira Bhatnagar, Panchanathan Manivasagan, Kyong-Hwa Kang, Se-Kwon Kim
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2015)
Article
Microbiology
Ira Bhatnagar, Se-Kwon Kim
INTERNATIONAL JOURNAL OF MEDICAL MICROBIOLOGY
(2015)
Article
Biochemistry & Molecular Biology
BoMi Ryu, Byul-Nim Aim, Kyong-Hwa Kang, Young-Sang Kim, Yong-Xin Li, Chang-Suk Kong, Se-Kwon Kim, Dong Gyu Kim
JOURNAL OF PHOTOCHEMISTRY AND PHOTOBIOLOGY B-BIOLOGY
(2015)
Review
Biochemistry & Molecular Biology
S. Deepthi, J. Venkatesan, Se-Kwon Kim, Joel D. Bumgardner, R. Jayakumar
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2016)
Article
Biochemistry & Molecular Biology
Baboucarr Lowe, Jayachandran Venkatesan, Sukumaran Anil, Min Suk Shim, Se-Kwon Kim
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2016)
Article
Biochemistry & Molecular Biology
R. Nithya, Thandapani Gomathi, P. N. Sudha, Jayachandran Venkatesan, Sukumaran Anil, Se-Kwon Kim
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2016)
Review
Polymer Science
Jayachandran Venkatesan, Sukumaran Anil, Se-Kwon Kim, Min Suk Shim
Review
Microbiology
Panchanathan Manivasagan, Jayachandran Venkatesan, Kannan Sivakumar, Se-Kwon Kim
CRITICAL REVIEWS IN MICROBIOLOGY
(2015)
Review
Microbiology
Panchanathan Manivasagan, Jayachandran Venkatesan, Kannan Sivakumar, Se-Kwon Kim
CRITICAL REVIEWS IN MICROBIOLOGY
(2016)
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)
