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- | Aduhelm (aducanumab) / Neurimmune, Eisai, Leqembi (lecanemab-irmb) / Biogen, Eisai, Kisunla (donanemab-azbt) / Eli Lilly
Journal, IO biomarker: Chemical-Driven Amyloid Clearance for Therapeutics and Diagnostics of Alzheimer's Disease. (Pubmed Central) - Nov 19, 2024
In clinical practice, we anticipate that these findings will contribute to the development of patient-friendly therapeutic and diagnostic interventions, including self-administered and orally available options, thereby enhancing disease management and overall quality of life for individuals with AD. Furthermore, this research extends beyond AD, potentially offering insights into other neurodegenerative diseases characterized by protein aggregation.
- | Journal: Novel role of curcumin as inhibitor of ?-amyloid-induced lamin fragmentation. (Pubmed Central) - Nov 19, 2024
Collectively, these findings suggest that curcumin inhibits A?-induced cell death by preventing A? entry and lamin cleavage, providing potential new insights for AD treatment.
- | Journal: Facile synthesis of EGCG modified Au nanoparticles and their inhibitory effects on amyloid protein aggregation. (Pubmed Central) - Nov 16, 2024
This work provides a facile approach to synthesize the surface-functionalized Au NPs for enhanced inhibition of A? aggregation and amelioration of A?-induced cytotoxicity.
- | Preclinical, Journal, IO biomarker: Noradrenaline Protects Human Microglial Cells (HMC3) Against Apoptosis and DNA Damage Induced by LPS and A?1-42 Aggregates In Vitro. (Pubmed Central) - Nov 16, 2024
These findings indicate that NA holds promise as a therapeutic target to address microglial dysfunction and potentially slow the progression of AD. Its neuroprotective effects, particularly in reducing inflammation and regulating microglial activity, warrant further investigation into its broader role in mitigating neuroinflammation and preserving microglial function in AD.
- | Journal: Photocatalytic, (Pubmed Central) - Nov 16, 2024
In vitro investigations have shown that L-CNDs can pass through the BBB. Collectively, our findings reveal a unique technique for treating amyloid disorders using carbon nanodots with significant potential for future studies in this area.
- | Preclinical, Journal: Helicobacter pylori outer membrane vesicles directly promote A? aggregation and enhance A? toxicity in APP/PS1 mice. (Pubmed Central) - Nov 16, 2024
These findings reveal a mechanism of H. pylori OMVs in accelerating AD development in which the bacterial OMVs-originated lipid components play a key role in promoting A? aggregation and neurotoxicity.
- | Journal: Aromatic polyketides isolated from the marine-derived fungus Didymella aeria and their neuroprotective activity. (Pubmed Central) - Nov 15, 2024
Integrastatin B (3) showed potential activity for inhibition of A? aggregation and protection against H2O2-induced cell death.
- || Review, Journal: Application of carbon-based nanomaterials in Alzheimer's disease. (Pubmed Central) - Nov 15, 2024
The advent of carbon nanomaterials in nanotechnology has facilitated the development of novel treatment approaches for Alzheimer's disease. These strategies provide promising approaches for early diagnosis, effective intervention and neuroprotection of the disease.
- | hyoscine butylbromide oral / Generic mfg.
Preclinical, Journal: Discovery of novel thiosemicarbazone-acridine targeting butyrylcholinesterase with antioxidant, metal complexing and neuroprotector abilities as potential treatment of Alzheimer's disease: In vitro, in vivo, and in silico studies. (Pubmed Central) - Nov 14, 2024
It also exhibited neuroprotective effects in an in vitro oxidative stress model induced by H2O2. Finally, in vivo experiments confirmed that CL-13 effectively reversed scopolamine-induced cognitive impairment, without affecting locomotor activity in the mice.
- | Journal: Inhibition of A? Aggregation and Tau Phosphorylation with Functionalized Biomimetic Nanoparticles for Synergic Alzheimer's Disease Therapy. (Pubmed Central) - Nov 14, 2024
Compared with the single therapeutic drug, HM-DK@CM restored nerve damage and improved AD mice's learning and memory abilities by decreasing A? oligomer, p-Tau protein, and inflammation through various pathways for synergistic therapy, which has broad prospects for the effective treatment of AD.
- | Journal: A mitochondria targeting, de novo designed, aggregation-induced emission probe for selective detection of neurotoxic amyloid-? aggregates. (Pubmed Central) - Nov 13, 2024
aggregates and to monitor mitochondrial morphology change and dysfunction during A?-induced neurotoxicity, which may offer imperative direction for the advancement of compelling AIE biomarkers for targeted early stage A? diagnosis in the future.
- | Journal: A smart adaptable metal sequestering peptide conjugate to modulate A? fibrillar aggregation. (Pubmed Central) - Nov 13, 2024
aggregation. While such adaptable metal binders that can chelate various metals are new, AMSP inhibits aggregation through selective recognition and metal scavenging.
- | Journal: Guluronic acid disaccharide inhibits reactive oxygen species production and amyloid-? oligomer formation. (Pubmed Central) - Nov 13, 2024
All of these results proved that Di-GA could be a promising marine drug candidate in reducing copper-related ROS damage and A? oligomer toxicity associated with AD.
- || Review, Journal: Unveiling tomorrow: Carbonic anhydrase activators and inhibitors pioneering new frontiers in Alzheimer's disease. (Pubmed Central) - Nov 7, 2024
The current review sheds light on the clinical evidence for hCAs and the roles of inhibitors and activators in AD. Additionally, this review offers a fascinating outlook on the data that may aid medicinal chemists in designing and developing new leads that are more effective and selective for upcoming in vitro and in vivo studies, allowing for the discovery and introduction of novel drug candidates for the treatment of AD to the market and into the clinical pipeline.
- | Journal: Tau Protein and Tauopathies: Exploring Tau Protein-Protein and Microtubule Interactions, Cross-Interactions and Therapeutic Strategies. (Pubmed Central) - Nov 5, 2024
amyloid peptide. This review amalgamates current knowledge on Tau protein and evolving therapeutic strategies, providing a comprehensive resource for researchers seeking to deepen their understanding of the Tau protein and for scientists involved in the development of new peptide-based anti-aggregative Tau compounds.
- | Journal: Keep neuroinflammation in mind when addressing Alzheimer's disease: A microglia perspective. (Pubmed Central) - Nov 5, 2024
The research addresses the potential of blocking a sequence of events that lead to the progression of Alzheimer's disease (AD). Here, we discuss the significance of these results in neuroinflammation, highlighting the greater implications for how decoy peptides would be interesting for the research and development of new drugs for AD therapy.
- | Journal: Bifunctional Copper Chelators Capable of Reducing A? Aggregation and A?-Induced Oxidative Stress. (Pubmed Central) - Nov 4, 2024
Low cell toxicity and antioxidating properties, in conjunction with AFM and SICM-based biophysical provided on A?42-affected SH-SY5Y cells, support Alz-5 as a potential inhibitor of A? aggregation.
- | rofecoxib (TRM-201) / Tremeau Pharma
Journal: Rational Design, Synthesis, and Evaluation of Rofecoxib-Based Photosensitizers for the NIR Imaging and Photo-Oxidization of A? Aggregates. (Pubmed Central) - Nov 4, 2024
All these excellent characteristics of our dual-functional photosensitizers for simultaneous imaging and photo-oxidation of A? aggregates suggest their promising prospects in pathological research in AD.
- || Review, Journal: Structural and functional remodeling of neural networks in ?-amyloid driven hippocampal hyperactivity. (Pubmed Central) - Nov 2, 2024
In addition, we analyze the available therapies and trials that can potentially be used clinically to attenuate hippocampal hyperexcitability in AD. Overall, the present review sheds lights on the mechanism behind A?-induced hippocampal hyperactivity, and highlights that hippocampal hyperactivity could be a robust biomarker and therapeutic target in prodromal AD.
- | Journal: Microglia-derived Galectin-9 drives amyloid-? pathology in Alzheimer's disease. (Pubmed Central) - Nov 1, 2024
aggregation and seeding in AD. Thus, strategies aimed at inhibiting Gal-9 may hold promise as a disease-modifying therapy to alleviate AD pathology.
- | Journal: Evaluation of Anti-Alzheimer's Potential of Azo-Stilbene-Thioflavin-T derived Multifunctional Molecules: Synthesis, Metal and A? Species Binding and Cholinesterase Activity. (Pubmed Central) - Oct 30, 2024
peptides and acetylcholinesterase enzyme to understand the observed inhibitory effect on activity. Overall, the studies presented here establish the multifunctional nature of these molecules and qualify them as promising candidates for furthermore investigation in the quest for finding Alzheimer's disease treatment.
- | Journal: Copper Overload Promotes ?-amyloid Induced NLRP3/Caspase-1/GSDMD-Mediated Pyroptosis in Alzheimer's Disease. (Pubmed Central) - Oct 30, 2024
aggregation, and activates NLRP3 inflammasomes, further promoting the A? aggregation activated pyroptosis in AD cell models.
- || Review, Journal: Oxidative stress-mediated neuroinflammation in Alzheimer's disease. (Pubmed Central) - Oct 29, 2024
The management of neurodegenerative conditions in the context of dementia necessitates therapeutic interventions that specifically target the excessive production of inflammatory and oxidative agents. Furthermore, we shall deliberate upon the function of microglia and oxidative injury in the etiology of AD and the ensuing neurodegenerative processes.
- | Journal: Skeletal Isomerization of Ergosterol-5,8-peroxide Leading to the Discovery of Unprecedented Ergostanes and Collective Syntheses of 5,6-Epoxysterols and (+)-Sarocladione. (Pubmed Central) - Oct 29, 2024
The ?-amyloid aggregation inhibitory activity of synthetic sterols was evaluated for the first time to gain insights into the potential for dementia prevention. This study is valuable both for supplying rare sterols found in mushrooms for biological studies and for shedding light on the oxidative metabolic pathways of ergosterol.
- | Aduhelm (aducanumab) / Neurimmune, Eisai, Leqembi (lecanemab-irmb) / Biogen, Eisai
Journal: A?-targeting synNotch Receptor for Alzheimer's Disease: Expanding Applications to Extracellular Protein Aggregates. (Pubmed Central) - Oct 28, 2024
aggregates by synthesizing and secreting Aducanumab or Lecanemab. These findings broaden the potential applications of synNotch, extending its targets beyond membrane-bound proteins to extracellular protein aggregates, providing obvious benefits to research in this scientific arena.
- | Journal: Brazilian kefir fraction mitigates the Alzheimer-like phenotype in Drosophila melanogaster with ?-amyloid overexpression model. (Pubmed Central) - Oct 27, 2024
These findings broaden the potential applications of synNotch, extending its targets beyond membrane-bound proteins to extracellular protein aggregates, providing obvious benefits to research in this scientific arena. This study demonstrated that kefir fractions, particularly the peptidic fraction?<?10
- | Journal: Real-Time 3D Imaging and Inhibition Analysis of Human Serum Amyloid A Aggregations Using Quantum Dots. (Pubmed Central) - Oct 26, 2024
aggregation, also exhibited high inhibitory activity against 40 ?M hSAA. These results indicate that the MSHTS system is an effective tool for visualizing hSAA aggregation and for screening highly active inhibitors.
- || Review, Journal: Morphological and Molecular Profiling of Amyloid-? Species in Alzheimer's Pathogenesis. (Pubmed Central) - Oct 24, 2024
aggregation inhibitors, and anti-amyloid vaccines) are already under clinical trials. New drug discovery approaches based on "designed multiple ligands", "hybrid molecules", or "multitarget-directed ligands" are also being put forward and may contribute to tackling this highly debilitating and fatal form of human dementia.
- | Journal: Targeted imaging of lysosomal zinc ions with a tetrahedral DNA framework fluorescent reporter. (Pubmed Central) - Oct 23, 2024
aggregates and learning/memory impairments. Our study provides a generalizable strategy for organelle-specific theranostic applications.
- | Journal: Unveiling the effect of CaCl2 on amyloid ? aggregation via supercritical angle Raman and fluorescence spectroscopy and microscopy. (Pubmed Central) - Oct 23, 2024
Note that calcium ions have a larger influence on amyloid ?1-42 than on the 40 amino acid variant. We found that a small layer of calcium ions significantly protects the lipid membrane against the protein insertion process.
- | Journal: Distinct regional vulnerability to A? and iron accumulation in post mortem AD brains. (Pubmed Central) - Oct 17, 2024
Iron and A? levels in ex-vivo brains were simultaneously quantified.
- | Journal: An in situ-activated and chemi-excited photooxygenation system based on G-poly(thioacetal) for A?1-42 aggregates. (Pubmed Central) - Oct 17, 2024
A series of novel photosensitizers have been prepared and synthesized for use in the photodynamic oxidation of A?1-42 aggregates under white light activation. The nanoparticles (BD-6-QM/NPs) self-assembled from BD-6-QM, bis[2,4,5-trichloro-6-(pentoxycarbonyl) phenyl] ester (CPPO), and G-poly(thioacetal) not only exhibit H2O2-stimulated controlled release but also can be chemically triggered by H2O2 to generate singlet oxygen to inhibit A?1-42 aggregates, reducing the A?1-42-induced neurotoxicity.
- | simvastatin / Generic mfg., donepezil / Generic mfg.
Journal: Intranasal Carrier-Free Nanomodulator Addresses Both Symptomatology and Etiology of Alzheimer's Disease by Restoring Neuron Plasticity and Reprogramming Lesion Microenvironment. (Pubmed Central) - Oct 17, 2024
In the treatment of FAD4T transgenic mice, it highly improved spatial memory impairment and cognitive deficits while restoring the homeostasis of brain microenvironment. Collectively, our study presented a paradigm for both achieving efficient brain delivery and offering pleiotropic therapies for AD.
- || Review, Journal: Exploring the Benzazoles Derivatives as Pharmacophores for AChE, BACE1, and as Anti-A? Aggregation to Find Multitarget Compounds against Alzheimer's Disease. (Pubmed Central) - Oct 16, 2024
However, even though benzazoles have not been widely evaluated on BACE1, benzimidazoles evaluated in vitro showed an IC50 value in the nM range. Therefore, important chemical modifications could be considered to improve multitarget benzazoles' activity, such as substitutions in the aromatic ring with electron withdrawal at position five, or a linker 3 or 4 carbons in length, which would allow for better interaction with targets.
- | Journal: Seven undescribed meroterpenoids from Sargassum siliquastrum and their inhibitory activity against amyloid ? aggregation. (Pubmed Central) - Oct 15, 2024
Among the seven compounds isolated, sargasilide B had the strongest inhibitory activity. From the comparison of structure and activity, the geometric isomerism of olefins and length of isoprene side chains are important for the activity of meroterpenoids isolated from brown alga.
- | Journal: Effect of diffusivity of amyloid beta monomers on the formation of senile plaques. (Pubmed Central) - Oct 15, 2024
monomers and their production rate impact the concentration of A? aggregates.
- | chlorogenic acid / Jiuzhang Biotech
Preclinical, Journal: Exploring the therapeutic potential of Potentilla fragarioides var. major (Rosaceae) extract in Alzheimer's disease using in vitro and in vivo models: a multi-faceted approach. (Pubmed Central) - Oct 13, 2024
High-performance liquid chromatography confirmed that EEPF has five major components: neochlorogenic acid, chlorogenic acid, polydatin, isochlorogenic acid A, and buddleoside, with amounts ranging across 1.91-9.41 mg/g. EEPF may be a promising drug for treatment of AD and AD-related brain disorders.
- | treprostinil palmitil inhalation (INS1009) / Insmed
Preclinical, Journal: Near-Infrared Bodipy based Molecular Rotors for ?-Amyloid Imaging In Vivo. (Pubmed Central) - Oct 12, 2024
EEPF may be a promising drug for treatment of AD and AD-related brain disorders. Therefore, with this research
- | RAF265 / Novartis
Journal: A Drug Repositioning Approach Reveals Ergotamine May Be a Potential Drug for the Treatment of Alzheimer's Disease. (Pubmed Central) - Oct 11, 2024
In further analysis by molecular dynamics simulations, both drugs exhibited reasonable stability. Our work indicated that ergotamine and RAF-265 may be potential candidates for treating AD.
- | Journal: Islet amyloid polypeptide fibril catalyzes amyloid-? aggregation by promoting fibril nucleation rather than direct axial growth. (Pubmed Central) - Oct 11, 2024
and IAPP, shedding light on the cross-seeding mechanisms potentially linking T2D and AD. Our findings also underscore the importance of clearing IAPP deposits in T2D patients to mitigate AD risk.
- | Journal: Comment on "Extracellular Vesicles Slow Down A?(1-42) Aggregation by Interfering with the Amyloid Fibril Elongation Step". (Pubmed Central) - Oct 9, 2024
The commentary, in the light of included original experiments and cited literature, suggests that membrane proteins like PrPC are crucial to fully understand the role of EVs in A? aggregation, and Halipi et al.'s conclusions should be reexamined in light of these factors.
- | Journal: Deciphering the Morphological Difference of Amyloid-? Fibrils in Familial and Sporadic Alzheimer's Diseases. (Pubmed Central) - Oct 9, 2024
Genetic predisposition in fAD, on the other hand, might impair or overwhelm Bri2 functions, leading to a high population of fAD-associated fibril morphology. Together, our computational findings provide a theoretical framework for elucidating the AD subtypes entailed by distinct dominant amyloid fibril morphologies.
- | Preclinical, Journal: Thy1-ApoE4/C/EBP? double transgenic mice act as a sporadic model with Alzheimer's disease. (Pubmed Central) - Oct 4, 2024
Hence, Thy1-ApoE4/C/EBP? mouse model acts as a sporadic AD mouse model, reconstituting the major AD pathologies.
- | Journal: Amyloid beta 1-40 and 1-42 fibril ratios and maturation level cause conformational differences with minimal impact on autophagy and cytotoxicity. (Pubmed Central) - Oct 3, 2024
Overall, these insights underline the need for further exploration of the impact of conformationally different fibrils and the need to reliably produce disease relevant A? aggregates.
- | Journal: Discovering Effective Chiral Dipeptides against A?(1-42) Aggregation by the Computational Screening Strategy. (Pubmed Central) - Oct 3, 2024
aggregates. Totally, our strategy presents a viable approach to discover potential dipeptides with effective antiaggregation ability as potential therapeutic agents for Alzheimer's disease.
- | Journal: A Hydroxyquinoline Polymer with Excellent Amyloidosis Inhibition and Protein Delivery Ability to Combat Amyloid-?-Mediated Neurotoxicity. (Pubmed Central) - Oct 3, 2024
Intracellular delivery of SOD further enhanced the ability to maintain the ROS homeostasis. This polymer offers a multifaceted approach to treating diseases associated with amyloidosis.
- | Journal: Peptide-Based Strategies: Combating Alzheimer's Amyloid ? Aggregation through Ergonomic Design and Fibril Disruption. (Pubmed Central) - Oct 1, 2024
Thus, our studies highlight that incorporating a ?-amino acid not only imparts protection from proteolytic degradation and improved stability but also functions effectively as a ? breaker, redirecting the aggregation kinetics toward off-pathway fibrillation.
- || Leqembi (lecanemab-irmb) / Biogen, Eisai, Kisunla (donanemab-azbt) / Eli Lilly
Review, Journal: What's in It for Me? Contextualizing the Potential Clinical Impacts of Lecanemab, Donanemab, and Other Anti-?-amyloid Monoclonal Antibodies in Early Alzheimer's Disease. (Pubmed Central) - Sep 28, 2024
In the process of this exercise, we outline a generally useful concept termed Summative Treatment-Associated Benefit measuring Long-term Efficacy/Effectiveness Area as a metric of summative benefits of treatment over the life course of an individual. Second, we consider current real-world factors, such as conditions of FDA approval and other points involved in clinical decision-making that will influence and/or temper the actual impacts of this drug class.
- Leqembi (lecanemab-irmb) / Biogen, Eisai
[11C]PiB Brain Retention is not Affected by Antibody Binding to Amyloid-Beta (e-Poster Area) - Sep 27, 2024 - Abstract #EANM2024EANM_1470;
Nonetheless, [11C]PiB PET was not able to identify early treatment effects on soluble A? aggregates or A?1-42 levels.
- Breakthrough in 11C methylation of biologically interesting molecules: the case of [11C]PiB (Hall F) - Sep 27, 2024 - Abstract #EANM2024EANM_738;
aggregates or A?1-42 levels. The presented [11C]PiB example shows that the optimization of the platform has therefore the potential to create a methylation agent able to be used in a wide range of 11C-labeling tracers in a efficiently, reproducibly, and most importantly quickly way.