Acetylcholinesterase Inhibitors in the Treatment of Neurodegenerative Diseases and the Role of Acetylcholinesterase in their Pathogenesis

International Journal of Molecular Sciences, Journal Year: 2021, Volume and Issue: 22(17), P. 9290 - 9290

Published: Aug. 27, 2021

Acetylcholinesterase (AChE) plays an important role in the pathogenesis of neurodegenerative diseases by influencing inflammatory response, apoptosis, oxidative stress and aggregation pathological proteins. There is a search for new compounds that can prevent occurrence slow down their course. The aim this review to present AChE pathomechanism diseases. In addition, aims reveal benefits using inhibitors treat these selected were also assessed terms potential use described disease entities. Designing searching drugs targeting may future allow discovery therapies will be effective treatment

Language: Английский

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Inflammatory Processes in Alzheimer’s Disease—Pathomechanism, Diagnosis and Treatment: A Review

International Journal of Molecular Sciences, Journal Year: 2023, Volume and Issue: 24(7), P. 6518 - 6518

Published: March 30, 2023

Alzheimer’s disease is one of the most commonly diagnosed cases senile dementia in world. It an incurable process, often leading to death. This multifactorial, and factor this inflammation. Numerous mediators secreted by inflammatory cells can cause neuronal degeneration. Neuritis may coexist with other mechanisms disease, contributing progression, also directly underlie AD. Although much has been established about processes pathogenesis AD, many aspects remain unexplained. The work devoted particular pathomechanism inflammation its role diagnosis treatment. An in-depth detailed understanding neuroinflammation help development diagnostic methods for early contribute new therapeutic strategies disease.

Language: Английский

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Chalcone and its analogs: Therapeutic and diagnostic applications in Alzheimer’s disease

Bioorganic Chemistry, Journal Year: 2021, Volume and Issue: 108, P. 104681 - 104681

Published: Jan. 29, 2021

Language: Английский

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Molecular hybridization: a powerful tool for multitarget drug discovery

Expert Opinion on Drug Discovery, Journal Year: 2024, Volume and Issue: 19(4), P. 451 - 470

Published: March 8, 2024

Introduction The current drug discovery paradigm of 'one drug, multiple targets' has gained attention from both the academic medicinal chemistry community and pharmaceutical industry. This is in response to urgent need for effective agents treat multifactorial chronic diseases. molecular hybridization strategy a useful tool that been widely explored, particularly last two decades, design multi-target drugs.

Language: Английский

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Quinones as Neuroprotective Agents

Antioxidants, Journal Year: 2023, Volume and Issue: 12(7), P. 1464 - 1464

Published: July 20, 2023

Quinones can in principle be viewed as a double-edged sword the treatment of neurodegenerative diseases, since they are often cytoprotective but also cytotoxic due to covalent and redox modification biomolecules. Nevertheless, low doses moderately electrophilic quinones generally cytoprotective, mainly their ability activate Keap1/Nrf2 pathway thus induce expression detoxifying enzymes. Some natural have relevant roles important physiological processes. One them is coenzyme Q

Language: Английский

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Drugtamer‐PROTAC Conjugation Strategy for Targeted PROTAC Delivery and Synergistic Antitumor Therapy

Advanced Science, Journal Year: 2024, Volume and Issue: 11(25)

Published: April 19, 2024

Abstract Proteolysis‐targeting chimeras (PROTACs) have emerged as a promising strategy for targeted protein degradation and drug discovery. To overcome the inherent limitations of conventional PROTACs, an innovative drugtamer‐PROTAC conjugation approach is developed to enhance tumor targeting antitumor potency. Specifically, smart prodrug designed by conjugating “drugtamer” nicotinamide phosphoribosyltransferase (NAMPT) PROTAC using microenvironment responsible linker. The consists fluorouridine nucleotide DNA‐like oligomer. Compared NAMPT combination + fluorouracil, AS‐2F‐NP demonstrates superior targeting, efficient cellular uptake, improved in vivo potency reduced side effects. This study provides precise delivery synergistic agents.

Language: Английский

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Green Tea Epigallocatechin-3-gallate (EGCG) Targeting Protein Misfolding in Drug Discovery for Neurodegenerative Diseases

Biomolecules, Journal Year: 2021, Volume and Issue: 11(5), P. 767 - 767

Published: May 20, 2021

The potential to treat neurodegenerative diseases (NDs) of the major bioactive compound green tea, epigallocatechin-3-gallate (EGCG), is well documented. Numerous findings now suggest that EGCG targets protein misfolding and aggregation, a common cause pathological mechanism in many NDs. Several studies have shown interacts with misfolded proteins such as amyloid beta-peptide (Aβ), linked Alzheimer’s disease (AD), α-synuclein, Parkinson’s (PD). To date, NDs constitute serious public health problem, causing financial burden for care systems worldwide. Although current treatments provide symptomatic relief, they do not stop or even slow progression these devastating disorders. Therefore, there an urgent need develop effective drugs incurable ailments. It expected targeting can serve therapeutic strategy since neurodegeneration. In this context, may offer great opportunities drug discovery review critically discusses role provides updated information on scientific evidence potentially be used fatal brain

Language: Английский

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Advancements in the development of multi-target directed ligands for the treatment of Alzheimer’s disease

Bioorganic & Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 61, P. 116742 - 116742

Published: April 5, 2022

Language: Английский

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Contemporary Medicinal Chemistry Strategies for the Discovery and Development of Novel HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors

Journal of Medicinal Chemistry, Journal Year: 2022, Volume and Issue: 65(5), P. 3729 - 3757

Published: Feb. 17, 2022

Currently, HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs) are a major component of the highly active anti-retroviral therapy (HAART) regimen. However, occurrence drug-resistant strains and adverse reactions after long-term usage have inevitably compromised clinical application NNRTIs. Therefore, development novel with distinct anti-resistance profiles better pharmacological properties is still an enormous challenge. Herein, we summarize state-of-the-art medicinal chemistry strategies for discovery potent NNRTIs, such as structure-based design strategies, contemporary computer-aided drug design, covalent-binding multi-target-directed ligands. The described here will facilitate identification promising

Language: Английский

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Multi-Target Mechanisms of Phytochemicals in Alzheimer’s Disease: Effects on Oxidative Stress, Neuroinflammation and Protein Aggregation

Journal of Personalized Medicine, Journal Year: 2022, Volume and Issue: 12(9), P. 1515 - 1515

Published: Sept. 15, 2022

Alzheimer's disease (AD) is a neurodegenerative characterized by tangle-shaped accumulation of beta-amyloid peptide fragments and Tau protein in brain neurons. The pathophysiological mechanism involves the presence Aβ-amyloid peptide, protein, oxidative stress, an exacerbated neuro-inflammatory response. This review aims to offer updated compendium most recent promising advances AD treatment through administration phytochemicals. literature survey was carried out electronic search following specialized databases PubMed/Medline, Embase, TRIP database, Google Scholar, Wiley, Web Science regarding published works that included molecular mechanisms signaling pathways targeted phytochemicals various experimental models vitro vivo. results studies showed use against has gained relevance due their antioxidant, anti-neuroinflammatory, anti-amyloid, anti-hyperphosphorylation properties protein. Some bioactive compounds from plants have been shown ability prevent stop progression Alzheimer's.

Language: Английский

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