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Multi-target-directed ligands to combat neurodegenerative diseases.
TLDR
The aims of the present article are to discuss the role of ligand modification in the discovery of clinically efficacious drugs and the role that ligands endowed with outstanding in vitro selectivity have in this area.
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Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush.
TLDR
Compounds that inhibit acetylcholinesterase and NMDA receptor activity and display antioxidant properties are presented, emerging as lead candidates for treating AD.
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Rational approach to discover multipotent anti-Alzheimer drugs.
TLDR
Lipocrine is the first compound that inhibits the catalytic activity of A ChE and AChE-induced amyloid-beta aggregation and protects against reactive oxygen species and emerged as a valuable pharmacological tool to investigate Alzheimer's disease and as a promising lead compound for new anti-Alzheimer drugs.
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Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease.
A design strategy to convert a dual-binding site AChE inhibitor into triple functional compounds with promising in vitro profile against multifactorial syndromes, such as Alzheimer's disease, is…
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A small molecule targeting the multifactorial nature of Alzheimer's disease.
TLDR
Nowadays,Mechanism-based drug-design approaches are mainly directed toward two proteins, amy-loidb (Ab) and tau, whereas phosphorylated tau is the main component of neurofibrillary tangles, the other hallmark lesion of AD.
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Alzheimer's disease: new approaches to drug discovery.
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Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.
TLDR
A new class of MTDLs based on a polyamine-quinone skeleton, whose lead (memoquin, 2) showed promising properties in preclinical investigations are described, and were tested in vitro against a number of isolated AD-related targets.
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Prejunctional muscarinic inhibitory control of acetylcholine release in the human isolated detrusor: involvement of the M4 receptor subtype
TLDR
The comparison of pre‐ and post‐junctional potencies and the relationship analysis with the affinity constants at human cloned muscarinic receptor subtypes indicates that the mus carinic autoreceptor inhibiting ACh release in human detrusor is an M4 receptor, while the receptor involved in muscular contraction belongs to the M3 subtype.
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Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
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Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects.
TLDR
The multifactorial mechanistic nature of cancer calls for the development of multifunctional therapeutic tools, i.e., single compounds able to interact with multiple altered pathogenetic pathways to induce apoptosis in tumor cell lines.
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